Note: Descriptions are shown in the official language in which they were submitted.
WO 2021/116854
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ORAL PRODUCTS WITH ACTIVE INGREDIENT COMBINATIONS
FIELD OF THE DISCLOSURE
The present disclosure relates to compositions intended for human use. The
compositions are
configured for oral use and deliver substances such as flavors and/or active
ingredients during use. Such
products may include tobacco or a product derived from tobacco, or may be
tobacco-free alternatives.
BACKGROUND
Tobacco may be enjoyed in a so-called "smokeless" form. Particularly popular
smokeless
tobacco products are employed by inserting some form of processed tobacco or
tobacco-containing
formulation into the mouth of the user. Conventional formats for such
smokeless tobacco products
include moist snuff, snus, and chewing tobacco, which are typically formed
almost entirely of particulate,
granular, or shredded tobacco, and which are either portioned by the user or
presented to the user in
individual portions, such as in single-use pouches or sachets. Other
traditional forms of smokeless
products include compressed or agglomerated forms, such as plugs, tablets, or
pellets. Alternative
product formats, such as tobacco-containing gums and mixtures of tobacco with
other plant materials, arc
also known. See for example, the types of smokeless tobacco formulations,
ingredients, and processing
methodologies set forth in US Pat. Nos. 1,376,586 to Schwartz; 4,513,756 to
Pittman et al.; 4,528,993 to
Sensabaugh, Jr. et al.; 4,624,269 to Story et al.; 4,991,599 to Tibbetts;
4,987,907 to Townsend; 5,092,352
to Sprinkle, III et al.; 5,387,416 to White et al.; 6,668,839 to Williams;
6,834,654 to Williams; 6,953,040
to Atchley et al.; 7,032,601 to Atchley et al.; and 7,694,686 to Atchley et
al.; US Pat. Pub. Nos.
2004/0020503 to Williams; 2005/0115580 to Quinter et al.; 2006/0191548 to
Strickland et al.;
2007/0062549 to Holton, Jr. et al.; 2007/0186941 to Holton, Jr. et al.;
2007/0186942 to Strickland et al.;
2008/0029110 to Dube et al.; 2008/0029116 to Robinson et al.; 2008/0173317 to
Robinson et al.;
2008/0209586 to Neilsen et al.; 2009/0065013 to Essen et al.; and 2010/0282267
to Atchley, as well as
W02004/095959 to Arnarp et al., each of which is incorporated herein by
reference.
Smokeless tobacco product configurations that combine tobacco material with
various binders
and fillers have been proposed more recently, with example product formats
including lozenges, pastilles,
gels, extruded forms, and the like. See, for example, the types of products
described in US Patent App.
Pub. Nos. 2008/0196730 to Engstrom et al.; 2008/0305216 to Crawford et al.;
2009/0293889 to Kumar et
al.; 2010/0291245 to Gao et al; 2011/0139164 to Mua et al.; 2012/0037175 to
Cantrell et al.;
2012/0055494 to Hunt et al.; 2012/0138073 to Cantrell et al.; 2012/0138074 to
Cantrell et al.;
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2013/0074855 to Holton, Jr.; 2013/0074856 to Holton, Jr.; 2013/0152953 to Mua
et al.; 2013/0274296 to
Jackson et al.; 2015/0068545 to Moldoveanu et al.; 2015/0101627 to Marshall et
al.; and 2015/0230515
to Lampe et al., each of which is incorporated herein by reference.
BRIEF SUMMARY
The present disclosure generally provides compositions configured for oral
use, the compositions
comprising at least one active ingredient and one or more fillers. The
compositions may be in chewable
form, tablet form, or in the form of a melt.
In one aspect, the disclosure provides a composition in chewable form,
configured for oral use,
the composition comprising: at least one active ingredient selected from the
group consisting of caffeine,
taurine, GABA, theanine, tryptophan, vitamin B6, vitamin B12 (or other B
vitamins), vitamin C, lemon
balm extract, ginseng, citicolinc, sunflower lecithin, and combinations
thereof; one or morc sugar
alcohols in an amount by weight of at least 50%, based on the total weight of
the composition; pectin; and
an organic acid, a gelation agent, or both, wherein the composition is a
homogenous mixture.
In one embodiment, the one or more sugar alcohols is a combination of isomalt
and maltitol. In
one embodiment, the composition comprises isomalt in an amount of from about
10 to about 25% by
weight, based on the total weight of the composition; maltitol in an amount of
from about 50 to about
75% by weight, based on the total weight of the composition; and pectin in an
amount of from about 1 to
about 3% by weight, based on the total weight of the composition.
In one embodiment, the organic acid is citric acid. In one embodiment, the
gelation agent is a
calcium salt. In one embodiments, the calcium salt is calcium diphosphate.
In one embodiment, the at least one active ingredient comprises caffeine.
In one embodiment, the at least one active ingredient comprises theanine.
In one embodiment, the at least one active ingredient comprises taurine.
In one embodiment, the at least one active ingredient comprises GABA.
In one embodiment, the at least one active ingredient comprises tryptophan.
In one embodiment, the at least one active ingredient comprises vitamin B6,
vitamin B12, or
both., such as vitamins B6 and B12 in a total amount by weight from about
0.008% to about 0.07%.
In one embodiment, the at least one active ingredient comprises vitamin C.
In one embodiment, the at least one active ingredient comprises ginseng.
In one embodiment, the at least one active ingredient comprises lemon balm
extract.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine,
theanine, and optionally ginseng. In one embodiment, the caffeine is present
in an amount of from about 1
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to about 4% by weight, based on the total weight of the composition; the
theanine is present in an amount
of from about 1 to about 4% by weight, based on the total weight of the
composition; and the ginseng,
when present, is in an amount of from about 0.1 to about 0.6% by weight, based
on the total weight of the
composition. In one embodiment, the composition further comprises citicoline
or sunflower lecithin.
In one embodiment, the at least one active ingredient comprises a combination
of theanine,
gamma-amino butyric acid (GABA), and optionally lemon balm extract. In one
embodiment, the theanine
is present in an amount of from about 1 to about 3% by weight, based on the
total weight of the
composition; the GABA is present in an amount of from about 1.5 to about 4% by
weight, based on the
total weight of the composition; and the lemon balm extract, when present, is
in an amount from about
0.25 to about 2% by weight, based on the total weight of the composition.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine,
taurine, and vitamin C. In one embodiment, the caffeine is present in an
amount of from about 1 to about
4% by weight, based on the total weight of the composition; the taurine is
present in an amount of from
about 1 to about 4% by weight, based on the total weight of the composition;
and the vitamin C is present
in an amount of from about 1 to about 3% by weight, based on the total weight
of the composition. In one
embodiment, the composition further comprises trisodium citrate. In one
embodiment, the composition
further comprises vitamin B6, vitamin B12, or both. In one embodiment, the at
least one active ingredient
comprises a combination of caffeine, taurine, and vitamin B6, vitamin B12, or
both.
In one embodiment, the composition further comprises at least one additional
component selected
from water, sweeteners, salts, flavors, buffers, emulsifiers, colorants,
processing aids, and combinations
thereof.
In one embodiment, the composition further comprises magnesium, such as
magnesium in an
amount by weight from about 0.1% to about 2%, or from about 0.2 to about 1%,
based on elemental
magnesium. In one embodiment, the magnesium is in the form of a magnesium
salt. In one embodiment,
the magnesium salt is magnesium gluconate.
In one embodiment, the composition is free of nicotine.
In one embodiment, the composition is free of tobacco.
In another aspect is provided a composition in tablet form configured for oral
use, the
composition comprising at least one active ingredient selected from the group
consisting of caffeine,
taurine, GABA, theanine, tryptophan, vitamin B6, vitamin B12 (or other B
vitamins), vitamin C, lemon
balm extract, ginseng, citicoline, sunflower lecithin, and combinations
thereof; a glucose-polysaccharide
blend; and a sugar alcohol; wherein the tablet form comprises the composition
as a homogenous mixture.
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In one embodiment, the glucose-polysaccharide blend is present in an amount of
from about 35 to
about 55% by weight, based on the total weight of the composition; and the
sugar alcohol is present in an
amount of from about 30 to about 45% by weight, based on the total weight of
the composition. In one
embodiment, the sugar alcohol is isomalt, erythritol, sorbitol, arabitol,
ribitol, maltitol, dulcitol, iditol,
mannitol, xylitol, lactitol, or a combination thereof. In one embodiment, the
sugar alcohol is isomalt.
In one embodiment, the at least one active ingredient comprises caffeine.
In one embodiment, the at least one active ingredient comprises theanine.
In one embodiment, the at least one active ingredient comprises taurine.
In one embodiment, the at least one active ingredient comprises tryptophan.
In one embodiment, the at least one active ingredient comprises GABA.
In one embodiment, the at least one active ingredient comprises vitamin B6,
vitamin B12, or
both, such as vitamins B6 and B12 in a total amount by weight from about
0.008% to about 0.07%.
In one embodiment, the at least one active ingredient comprises vitamin C.
In one embodiment, the at least one active ingredient comprises ginseng.
In one embodiment, the at least one active ingredient comprises lemon balm
extract.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine,
theanine, and optionally ginseng. In one embodiment, the caffeine is present
in an amount of from about 3
to about 5% by weight, based on the total weight of the composition; the
theanine is present in an amount
of from about 3 to about 5% by weight, based on the total weight of the
composition; and the ginseng,
when present, is in an amount from about 0.4 to about 0.6% by weight, based on
the total weight of the
composition. in one embodiment, the composition further comprises citicoline
or sunflower lecithin.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine and
vitamin B6, vitamin B12, or both. In one embodiment, the at least one active
ingredient comprises a
combination of caffeine and taurine. In one embodiment, the at least one
active ingredient comprises a
combination of caffeine, taurine, and vitamin B6, vitamin B12, or both.
In one embodiment, the at least one active ingredient comprises a combination
of theanine,
gamma-amino butyric acid (GABA), and optionally lemon balm extract. In one
embodiment, the theanine
is present in an amount of from about 3 to about 5% by weight, based on the
total weight of the
composition; the GABA is present in an amount of from about 4 to about 6% by
weight, based on the
total weight of the composition; and the lemon balm extract when present is in
an amount from about 3 to
about 4% by weight, based on the total weight of the composition.
In one embodiment, the at least one active ingredient comprises theanine and
tryptophan. In one
embodiment, the at least one active ingredient comprises theanine and vitamin
B6, B12, or a combination
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thereof. In one embodiment, the at least one active ingredient comprises
theanine, tryptophan, and vitamin
B6, B12, or a combination thereof.
In one embodiment, the at least one active ingredient comprises caffeine and
taurine. In one
embodiment, the at least one active ingredient comprises a combination of
caffeine, taurine, and vitamin
C. In one embodiment, the caffeine is present in an amount of from about 3 to
about 5% by weight, based
on the total weight of the composition; the taurine is present in an amount of
from about 4 to about 6% by
weight, based on the total weight of the composition; and the vitamin C is
present in an amount of from
about 4 to about 6% by weight, based on the total weight of the composition.
In one embodiment, the
composition further comprises trisodium citrate.
In one embodiment, the composition further comprises at least one additional
component selected
from sweeteners, salts, flavors, buffers, emulsifiers, colorants, processing
aids, and combinations thereof.
In one embodiment, the composition further comprises magnesium, such as
magnesium in an
amount by weight from about 0.1% to about 2%, or from about 0.2 to about 1%,
based on elemental
magnesium. In one embodiment, the magnesium is in the form of a magnesium
salt. In one embodiment,
the magnesium salt is magnesium gluconate.
In one embodiment, the composition is free of nicotine.
In one embodiment, the composition is free of tobacco.
In another aspect is provided a composition in meltable form, configured for
oral use, the
composition comprising: at least one active ingredient selected from the group
consisting of caffeine,
taurine, GABA, theanine, tryptophan, vitamin B6, vitamin B12 (or other B
vitamins), vitamin C, lemon
balm extract, ginseng, citicoline, sun flower lecithin, and combinations
thereof; a sugar alcohol; and a
lipid; wherein the meltable form comprises the composition as a homogenous
mixture.
In one embodiment, the sugar alcohol is present in an amount of from about 35
to about 55% by
weight, based on the total weight of the composition; and the lipid in an
amount of from about 35 to about
50% by weight, based on the total weight of the composition. In one
embodiment, the lipid has a melting
point of about 29 C or above. In one embodiment, the lipid has a melting point
from about 36 C to about
45 C. In one embodiment, the lipid is an oil selected from the group
consisting of palm oil, palm kernel
oil, soybean oil, sunflower oil, coconut oil, cottonseed oil, and combinations
thereof, wherein the oil may
be hydrogenated, partially hydrogenated, or non-hydrogenated.
In one embodiment, the sugar alcohol is isomalt, erythritol, sorbitol,
arabitol, ribitol, maltitol,
dulcitol, iditol, mannitol, xylitol, lactitol, or a combination thereof. In
one embodiment, the sugar alcohol
is isomalt.
In one embodiment, the at least one active ingredient comprises caffeine.
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In one embodiment, the at least one active ingredient comprises theanine.
In one embodiment, the at least one active ingredient comprises taurine.
In one embodiment, the at least one active ingredient comprises GABA.
In one embodiment, the at least one active ingredient comprises tryptophan.
In one embodiment, the at least one active ingredient comprises vitamin B6,
vitamin B12, or
both; such as vitamins B6 and B12 in a total amount by weight from about
0.008% to about 0.07%.
In one embodiment, the at least one active ingredient comprises vitamin C.
In one embodiment, the at least one active ingredient comprises ginseng.
In one embodiment, the at least one active ingredient comprises lemon balm
extract.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine,
theanine, and optionally, ginseng. In one embodiment, the caffeine is present
in an amount of from about
2 to about 6% by weight, based on the total weight of the composition;
theanine is present in an amount
of from about 2 to about 4% by weight, based on the total weight of the
composition; and the ginseng
when present is in an amount from about 0.3 to about 0.5% by weight, based on
the total weight of the
composition.
In one embodiment, the composition further comprises citicolinc or sunflower
lecithin.
In one embodiment, at least a portion of the caffeine is present in
encapsulated form.
In one embodiment, the at least one active ingredient comprises a combination
of theanine,
gamma-amino butyric acid (GABA), and optionally lemon balm extract. In one
embodiment, the theanine
is present in an amount of from about 2 to about 4% by weight, based on the
total weight of the
composition; the GABA is present in an amount of from about 3.5 to about 4.5%
by weight, based on the
total weight of the composition; and the lemon balm extract when present is in
an amount of from about
1.5 to about 2.5% by weight, based on the total weight of the composition.
In one embodiment, the at least one active ingredient comprises theanine and
tryptophan. In one
embodiment, the at least one active ingredient comprises theanine and vitamin
B6, B12, or a combination
thereof. In one embodiment, the at least one active ingredient comprises
theanine, tryptophan, and vitamin
B6, B12, or a combination thereof.
In one embodiment, the at least one active ingredient comprises a combination
of caffeine,
taurine, and vitamin C. In one embodiment, the caffeine is present in an
amount of from about 2 to about
6% by weight, based on the total weight of the composition; the taurine is
present in an amount of from
about 3.5 to about 4.5% by weight, based on the total weight of the
composition; and the vitamin C is
present in an amount of from about 3.5 to about 4.5% by weight, based on the
total weight of the
composition.
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In one embodiment, at least a portion of the caffeine is present in
encapsulated form.
In one embodiment, the composition further comprises sodium citrate.
In one embodiment, the composition further comprises at least one additional
component selected
from sweeteners, salts, flavors, buffers, emulsifiers, colorants, processing
aids, and combinations thereof.
In one embodiment, the composition further comprises magnesium, such as
magnesium in an
amount by weight from about 0.1% to about 2%, or from about 0.2 to about 1%,
based on elemental
magnesium. In one embodiment, the magnesium is in the form of a magnesium
salt. In one embodiment,
the magnesium salt is magnesium gluconate.
In one embodiment, the composition is free of nicotine.
In one embodiment, the composition is free of tobacco.
In another aspect is provided a composition in chewable, tablet, or melting
form as disclosed
herein, wherein the at least one active ingredient is a combination of:
a) caffeine in an amount of from about 1.5 to about 5% by weight, based on the
total weight
of the composition;
taurine in an amount of from about 1.5 to about 6% by weight, based on the
total weight
of the composition;
vitamin C in an amount of from about 2 to about 6% by weight, based on the
total weight
of the composition; and
sodium citrate in an amount of from about 1 to about 3% by weight, based on
the total
weight of the composition;
b) theanine in an amount of from about 1 to about 5% by weight, based on the
total weight
of the composition;
GABA in an amount of from about 1.5 to about 6% by weight, based on the total
weight
of the composition; and
lemon balm extract in an amount of from about 1 to about 4% by weight, based
on the
total weight of the composition; or
c) caffeine in an amount of from about 1.5 to about 6% by weight, based on the
total weight
of the composition;
theanine in an amount of from about 1.5 to about 5% by weight, based on the
total weight
of the composition;
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ginseng in an amount of from about 0.2 to about 0.6% by weight, based on the
total
weight of the composition; and optionally,
citicoline or sunflower lecithin in an amount of from about 0.3 to about 1.5%
by weight,
based on the total weight of the composition.
The disclosure includes, without limitations, the following embodiments.
Embodiment 1: A composition in chewable form, configured for oral use, the
composition
comprising: at least one active ingredient selected from the group consisting
of caffeine, taurine, GABA,
theanine, tryptophan, vitamin B6, vitamin B12, vitamin C, lemon balm extract,
ginseng, citicoline,
sunflower lecithin, and combinations thereof; one or more sugar alcohols in an
amount by weight of at
least 50%, based on the total weight of the composition; pectin; and an
organic acid, a gelation agent, or
both; wherein the composition is a homogenous mixture.
Embodiment 2: The composition of embodiment 1, wherein the one or more sugar
alcohols is a
combination of isomalt and maltitol.
Embodiment 3: The composition of embodiment 1 or 2, comprising isomalt in an
amount of from
about 10 to about 25% by weight, based on the total weight of the composition;
maltitol in an amount of
from about 50 to about 75% by weight, based on the total weight of the
composition; and pectin in an
amount of from about 1 to about 3% by weight, based on the total weight of the
composition.
Embodiment 4: The composition of any one of embodiments 1 to 3, wherein the
organic acid is
citric acid.
Embodiment 5: The composition of any one of embodiments 1 to 4, wherein the at
least one
active ingredient comprises a combination of caffeine, theanine, and
optionally ginseng.
Embodiment 6: The composition of any one of embodiments 1 to 5, wherein: the
caffeine is
present in an amount of from about 1 to about 4% by weight, based on the total
weight of the
composition; thcaninc is present in an amount of from about 1 to about 4% by
weight, based on the total
weight of the composition; and the ginseng is present in an amount of from
about 0.1 to about 0.6% by
weight, based on the total weight of the composition.
Embodiment 7: The composition of any one of embodiments 1 to 6, further
comprising citicoline
or sunflower lecithin.
Embodiment 8: The composition of any one of embodiments 1 to 4, wherein the at
least one
active ingredient comprises a combination of theanine, gamma-amino butyric
acid (GABA), and
optionally lemon balm extract.
Embodiment 9: The composition of any one of embodiments 1 to 8, wherein: the
theanine is
present in an amount of from about 1 to about 3% by weight, based on the total
weight of the
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composition; the GABA is present in an amount of from about 1.5 to about 4% by
weight, based on the
total weight of the composition; and the lemon balm extract when present is in
an amount of from about
0.25 to about 2% by weight, based on the total weight of the composition.
Embodiment 10: The composition of any one of embodiments 1 to 4, wherein the
at least one
active ingredient comprises: theanine; theanine and tryptophan; or theanine
and one or more of vitamins
B6 and B12; and optionally tryptophan.
Embodiment 11: The composition of any one of embodiments 1 to 4, comprising
theanine and
one or both of vitamins B6 and vitamin B12.
Embodiment 12: The composition of any one of embodiments 1 to 4, wherein the
at least one
active ingredient comprises a combination of caffeine, taurine, and vitamin C.
Embodiment 13: The composition of any one of embodiments 1 to 12, wherein: the
caffeine is
present in an amount of from about 1 to about 4% by weight, based on the total
weight of the
composition; the taurine is present in an amount of from about 1 to about 4%
by weight, based on the
total weight of the composition; and the vitamin C is present in an amount of
from about 1 to about 3% by
weight, based on the total weight of the composition.
Embodiment 14: The composition of any one of embodiments 1 to 13, further
comprising
trisodium citrate.
Embodiment 15: The composition of any one of embodiments 1 to 14, further
comprising at least
one additional component selected from water, sweeteners, salts, flavors,
buffers, emulsifiers, colorants,
processing aids, and combinations thereof.
Embodiment 16: The composition of any one of embodiments 1 to 15, wherein the
composition is
free of nicotine.
Embodiment 17: The composition of any one of embodiments 1 to 16, wherein the
composition is
free of tobacco.
Embodiment 18: A composition in tablet form configured for oral use, the
composition
comprising: at least one active ingredient selected from the group consisting
of caffeine, taurine, GABA,
theanine, tryptophan, vitamin B6, vitamin B12, vitamin C, lemon balm extract,
ginseng, citicoline,
sunflower lecithin, and combinations thereof; a glucose-polysaccharide blend;
and a sugar alcohol;
wherein the tablet form comprises the composition as a homogenous mixture.
Embodiment 19: The composition of embodiment 18, wherein: the glucose-
polysaccharide blend
is present in an amount of from about 35 to about 55% by weight, based on the
total weight of the
composition; and the sugar alcohol is present in an amount of from about 30 to
about 45% by weight,
based on the total weight of the composition.
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Embodiment 20: The composition of embodiment 18 or 19, wherein the sugar
alcohol is isomalt,
erythritol, sorbitol, arabitol, ribitol, maltitol, dulcitol, iditol, mannitol,
xylitol, lactitol, or a combination
thereof.
Embodiment 21: The composition of any one of embodiments 18 to 20, wherein the
sugar alcohol
is isomalt.
Embodiment 22: The composition of any one of embodiments 18 to 21, wherein the
at least one
active ingredient comprises a combination of caffeine, theanine, and
optionally ginseng.
Embodiment 23: The composition of any one of embodiments 18 to 22, wherein:
the caffeine is
present in an amount of from about 3 to about 5% by weight, based on the total
weight of the
composition; theanine is present in an amount of from about 3 to about 5% by
weight, based on the total
weight of the composition; and the ginseng is present in an amount of from
about 0.4 to about 0.6% by
weight, based on the total weight of the composition.
Embodiment 24: The composition of any one of embodiments 18 to 23, further
comprising
citicoline or sunflower lecithin
Embodiment 25: The composition of any one of embodiments 18 to 21, wherein the
at least one
active ingredient comprises a combination of theanine, gamma-amino butyric
acid (GABA), and
optionally lemon balm extract.
Embodiment 26: The composition of any one of embodiments 18 to 25, wherein:
the theanine is
present in an amount of from about 3 to about 5% by weight, based on the total
weight of the
composition; the GABA is present in an amount of from about 4 to about 6% by
weight, based on the
total weight of the composition; and the lemon balm extract is present in an
amount of from about 3 to
about 4% by weight, based on the total weight of the composition.
Embodiment 27: The composition of any one of embodiments 18 to 21, wherein the
at least one
active ingredient comprises a combination of caffeine, taurine, and vitamin C.
Embodiment 28: The composition of embodiment 27, wherein: the caffeine is
present in an
amount of from about 3 to about 5% by weight, based on the total weight of the
composition; the taurine
is present in an amount of from about 4 to about 6% by weight, based on the
total weight of the
composition; and the vitamin C is present in an amount of from about 4 to
about 6% by weight, based on
the total weight of the composition.
Embodiment 29: The composition of embodiment 28, further comprising trisodium
citrate.
Embodiment 30: The composition of any one of embodiments 18 to 21, wherein the
at least one
active ingredient comprises: theanine; theanine and tryptophan; or theanine
and one or more of vitamins
B6 and B12; and optionally tryptophan.
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Embodiment 31: The composition of any one of embodiments 18 to 21, comprising
theanine and
one or both of vitamins B6 and vitamin B12.
Embodiment 32: The composition of any one of embodiments 18 to 31, further
comprising at
least one additional component selected from sweeteners, salts, flavors,
buffers, emulsifiers, colorants,
processing aids, and combinations thereof.
Embodiment 33: The composition of any one of embodiments 18 to 32, wherein the
composition
is free of nicotine.
Embodiment 34: The composition of any one of embodiments 18 to 33, wherein the
composition
is free of tobacco.
Embodiment 35: A composition in meltable form, configured for oral use, the
composition
comprising: at least one active ingredient selected from the group consisting
of caffeine, taurine, GABA,
tryptophan, theanine, vitamin B6, vitamin B12, vitamin C, lemon balm extract,
ginseng, citicoline,
sunflower lecithin, and combinations thereof; a sugar alcohol; and a lipid;
wherein the meltable form
comprises the composition as a homogenous mixture.
Embodiment 36: The composition of embodiment 35, wherein: the sugar alcohol is
present in an
amount of from about 35 to about 55% by weight, based on the total weight of
the composition: and the
lipid in an amount of from about 35 to about 50% by weight, based on the total
weight of the
composition.
Embodiment 37: The composition of embodiment 35 or 36, wherein the lipid has a
melting point
of about 29 C or above.
Embodiment 38: The composition of any one of embodiments 35 to 37, wherein the
lipid has a
melting point from about 36 C to about 45 C.
Embodiment 39: The composition of any one of embodiments 35 to 38, wherein the
lipid is an oil
selected from the group consisting of palm oil, palm kernel oil, soybean oil,
sunflower oil, cottonseed oil,
coconut oil, and combinations thereof, wherein the oil may be hydrogenated,
partially hydrogenated, or
non-hydrogenated.
Embodiment 40: The composition of any one of embodiments 35 to 38, wherein the
sugar alcohol
is isomalt, erythritol, sorbitol, arabitol, ribitol, maltitol, dulcitol,
iditol, mannitol, xylitol, lactitol, or a
combination thereof.
Embodiment 41: The composition of any one of embodiments 35 to 40, wherein the
sugar alcohol
is isomalt.
Embodiment 42: The composition of any one of embodiments 35 to 41, wherein the
at least one
active ingredient comprises a combination of caffeine, theanine, and
optionally, ginseng.
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Embodiment 43: The composition of embodiment 42, wherein: the caffeine is
present in an
amount of from about 2 to about 6% by weight, based on the total weight of the
composition; theanine is
present in an amount of from about 2 to about 4% by weight, based on the total
weight of the
composition; and the ginseng, when present, is in an amount from about 0.3 to
about 0.5% by weight,
based on the total weight of the composition.
Embodiment 44: The composition of embodiment 43, further comprising citicoline
or sunflower
lecithin.
Embodiment 45: The composition of embodiment 42, wherein at least a portion of
the caffeine is
present in encapsulated form.
Embodiment 46: The composition of any one of embodiments 35 to 41, wherein the
at least one
active ingredient comprises a combination of theanine, gamma-amino butyric
acid (GABA), and
optionally lemon balm extract.
Embodiment 47: The composition of embodiment 46, wherein: the theanine is
present in an
amount of from about 2 to about 4% by weight, based on the total weight of the
composition; the GABA
is present in an amount of from about 3.5 to about 4.5% by weight, based on
the total weight of the
composition; and the lemon balm extract when present is in an amount from
about 1.5 to about 2.5% by
weight, based on thc total weight of the composition.
Embodiment 48: The composition of any one of embodiments 35 to 41, wherein the
at least one
active ingredient comprises a combination of caffeine, taurine, and vitamin C.
Embodiment 49: The composition of embodiment 48, wherein: the caffeine is
present in an
amount of from about 2 to about 6% by weight, based on the total weight of the
composition; the taurine
is present in an amount of from about 3.5 to about 4.5% by weight, based on
the total weight of the
composition; and the vitamin C is present in an amount of from about 3.5 to
about 4.5% by weight, based
on the total weight of the composition.
Embodiment 50: The composition of embodiment 48, wherein at least a portion of
the caffeine is
present in encapsulated form.
Embodiment 51: The composition of embodiment 48, further comprising trisodium
citrate.
Embodiment 52: The composition of any one of embodiments 35 to 41, wherein the
at least one
active ingredient comprises: theanine; theanine and tryptophan; or theanine
and one or more of vitamins
B6 and B12; and optionally tryptophan.
Embodiment 52: The composition of any one of embodiments 35 to 41, comprising
theanine and
one or both of vitamins B6 and vitamin B12.
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Embodiment 53: The composition of any one of embodiments 35 to 52, further
comprising at
least one additional component selected from sweeteners, salts, flavors,
buffers, emulsifiers, colorants,
processing aids, and combinations thereof.
Embodiment 54: The composition of any one of embodiments 35 to 53, wherein the
composition
is free of nicotine.
Embodiment 55: The composition of any one of embodiments 35 to 54, wherein the
composition
is free of tobacco.
Embodiment 56: The composition of any one of embodiments 1, 18, or 35, wherein
the at least
one active ingredient is a combination of:
a) caffeine in an amount of from about 1.5 to about 5% by weight, based on the
total weight of
the composition;
taurine in an amount of from about 1.5 to about 6% by weight, based on the
total weight of the
composition;
vitamin C in an amount of from about 2 to about 6% by weight, based on the
total weight of the
composition; and
sodium citrate in an amount of from about 1 to about 3% by weight, based on
the total weight
of the composition;
b) theanine in an amount of from about 1 to about 5% by weight, based on the
total weight of
the composition;
GABA in an amount of from about 1.5 to about 6% by weight, based on the total
weight of
the composition; and
lemon balm extract in an amount of from about 1 to about 4% by weight, based
on the total
weight of the composition; or
c) caffeine in an amount of from about 1.5 to about 6% by weight, based on the
total weight of
the composition;
theanine in an amount of from about 1.5 to about 5% by weight, based on the
total weight of
the composition;
ginseng in an amount of from about 0.2 to about 0.6% by weight, based on the
total weight of
the composition; and optionally,
citicoline or sunflower lecithin in an amount of from about 0.3 to about 1.5%
by weight,
based on the total weight of the composition.
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Embodiment 57: The composition of any one of embodiments 1-56, further
comprising
magnesium, such as magnesium in an amount by weight from about 0.1% to about
2%, or from about 0.2
to about 1%, based on elemental magnesium.
These and other features, aspects, and advantages of the disclosure will be
apparent from a
reading of the following detailed description. The invention includes any
combination of two, three, four,
or more of the above-noted embodiments as well as combinations of any two,
three, four, or more features
or elements set forth in this disclosure, regardless of whether such features
or elements are expressly
combined in a specific embodiment description herein. This disclosure is
intended to be read holistically
such that any separable features or elements of the disclosed invention, in
any of its various aspects and
embodiments, should be viewed as intended to be combinable unless the context
clearly dictates
otherwise.
DETAILED DESCRIPTION
The present disclosure provides compositions configured for oral use, the
compositions
Ii comprising at least one active ingredient and one or more fillers. The
one or more fillers generally
comprise a sugar alcohol or a combination of sugar alcohols. The at least one
active ingredient may
include one or more botanical materials, stimulants, amino acids, vitamins,
antioxidants, nicotine
components, cannabinoids, cannabimimetics, teipenes, pharmaceutical agents, or
combinations thereof.
The compositions may be in chewable form, tablet form, or in the form of a
melt.
The present disclosure will now be described more fully hereinafter with
reference to example
embodiments thereof. These example embodiments are described so that this
disclosure will be thorough
and complete, and will fully convey the scope of the disclosure to those
skilled in the art. Indeed, the
disclosure may be embodied in many different forms and should not be construed
as limited to the
embodiments set forth herein; rather, these embodiments are provided so that
this disclosure will satisfy
applicable legal requirements As used in this specification and the claims,
the singular forms "a," "an,"
and "the" include plural referents unless the context clearly dictates
otherwise. Reference to "dry weight
percent" or "dry weight basis" refers to weight on the basis of dry
ingredients (i.e., all ingredients except
water). Reference to "wet weight" refers to the weight of the composition
including water. Unless
otherwise indicated, reference to "weight percent" of a composition reflects
the total wet weight of the
composition (i.e., including water).
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The compositions as described herein comprise at least one active ingredient
and one or more
fillers. In some embodiments, the compositions may further comprise binders,
organic acids, water,
sweeteners, salts, flavors, buffers, emulsifiers, colorants, processing aids,
and combinations thereof. The
relative amounts of the various components within the composition may vary,
and typically are selected
so as to provide the desired sensory and performance characteristics to the
oral composition. The example
individual components of the composition are described herein below.
Filler
The compositions as described herein comprise one or more fillers. Fillers may
fulfill multiple
functions, such as enhancing certain organoleptic properties such as texture
and mouthfeel, enhancing
cohesiveness or compressibility of the product, and the like.
The amount of filler can vary, but is typically greater than about 20%, and up
to about 75% of the
composition by weight, based on the total weight of the composition. A typical
range of filler within the
composition can be from about 20 to about 75% by total weight of the
composition, for example, from
about 20, about 25, or about 30, to about 35, about 40, about 45, or about 50%
by weight (e.g., about 20
to about 50%, or about 25 to about 45% by weight). In certain embodiments, the
amount of filler is at
least about 20% by weight, such as at least about 25%, or at least about 30%,
or at least about 35%, or at
least about 40%, based on the total weight of the composition.
Generally, fillers are porous particulate materials and are cellulose-based.
For example, suitable
fillers are any non-tobacco plant material or derivative thereof, including
cellulose materials derived from
such sources. Examples of cellulosic non-tobacco plant material include cereal
grains (e.g., maize, oat,
barley, rye, buckwheat, and the like), sugar beet (e.g., FIBREX brand filler
available from International
Fiber Corporation), bran fiber, and mixtures thereof. Non-limiting examples of
derivatives of non-tobacco
plant material include starches (e.g., from potato, wheat, rice, corn),
natural cellulose, and modified
cellulosic materials. Additional examples of potential fillers include
maltodextrin, dextrose, calcium
carbonate, calcium phosphate, lactose, mannitol, xylitol, and sorbitol.
Combinations of fillers can also be
used.
"Starch" as used herein may refer to pure starch from any source, modified
starch, or starch
derivatives. Starch is present, typically in granular form, in almost all
green plants and in various types of
plant tissues and organs (e.g., seeds, leaves, rhizomes, roots, tubers,
shoots, fruits, grains, and sterns).
Starch can vary in composition, as well as in granular shape and size. Often,
starch from different sources
has different chemical and physical characteristics. A specific starch can be
selected for inclusion in the
composition based on the ability of the starch material to impart a specific
organoleptic property to
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composition. Starches derived from various sources can be used. For example,
major sources of starch
include cereal grains (e.g., rice, wheat, and maize) and root vegetables
(e.g., potatoes and cassava). Other
examples of sources of starch include acorns, arrowroot, arracacha, bananas,
barley, beans (e.g., favas,
lentils, mung beans, peas, chickpeas), breadfruit, buckwheat, canna,
chestnuts, colacasia, katakuri, kudzu,
malanga, millet, oats, oca, Polynesian arrowroot, sago, sorghum, sweet potato,
quinoa, rye, tapioca, taro,
tobacco, water chestnuts, and yams. Certain starches are modified starches. A
modified starch has
undergone one or more structural modifications, often designed to alter its
high heat properties. Some
starches have been developed by genetic modifications, and are considered to
be "genetically modified"
starches. Other starches are obtained and subsequently modified by chemical,
enzymatic, or physical
means. For example, modified starches can be starches that have been subjected
to chemical reactions,
such as esterification, etherification, oxidation, depolymerization (thinning)
by acid catalysis or oxidation
in the presence of base, bleaching, transglycosylation and depolymerization
(e.g., dextrinization in the
presence of a catalyst), cross-linking, acetylation, hydroxypropylation,
and/or partial hydrolysis.
Enzymatic treatment includes subjecting native starches to enzyme isolates or
concentrates, microbial
enzymes, and/or enzymes native to plant materials, e.g.. amylase present in
corn kernels to modify corn
starch. Other starches are modified by heat treatments, such as
pregelatinization, dextrinization, and/or
cold water swelling processes. Certain modified starches include monostarch
phosphate, distarch
glycerol, distarch phosphate esterified with sodium trimetaphosphate,
phosphate distarch phosphate,
acetylated distarch phosphate, starch acetate esterified with acetic
anhydride, starch acetate esterified with
vinyl acetate, acetylated distarch adipate, acetylated distarch glycerol,
hydroxypropyl starch,
hydroxypropyl distarch glycerol, and starch sodium octenyl succinate.
Additional examples of potential fillers include maltodextrin, dextrose,
calcium carbonate,
calcium phosphate, lactose, and sugar alcohols. Combinations of fillers can
also be used. In some
embodiments, the filler comprises or is a mixture of glucose and starch-
derived polysaccharides. One
such suitable mixture of glucose and starch-derived polysaccharides is EMDEX ,
available from JRS
PHARMA LP, USA, 2981 Route 22, Patterson, NY 12563-2359.
In some embodiments, the filler comprises one or more sugar alcohols. Sugar
alcohols are polyols
derived from monosaccharides or disaceharides that have a partially or fully
hydrogenated form. Sugar
alcohols have, for example, about 4 to about 20 carbon atoms and include
erythritol, arabitol, ribitol,
isomalt, maltitol, dulcitol, iditol, mannitol, xylitol, lactitol, sorbitol,
and combinations thereof (e.g.,
hydrogenated starch hydrolysates). Isomalt is an equimolar mixture of two
disaccharides, each composed
of two sugars as follows: glucose and mannitol (a-D-glucopyranosido-1,6-
mannitol); and glucose and
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sorbitol (a-D-glucopyranosido-1,6-sorbitol). In some embodiments, the one or
more sugar alcohols
comprise isomalt. In some embodiments, the one or more sugar alcohols is
isomalt.
In some embodiments, the filler comprises a combination of isomalt and EMDEX .
In some
embodiments, the one or more sugar alcohols is a combination of isomalt and
EMDEX .
In some embodiments, the one or more sugar alcohols is a combination of two or
even three sugar
alcohols. In some embodiments, the combination of sugar alcohols comprises or
is isomalt and maltitol.
The total amount of sugar alcohols can vary, but is typically greater than
about 30%, and up to
about 95% of the composition by weight, based on the total weight of the
composition. A typical range of
sugar alcohols within the composition can be for example, from about 35, about
40, about 45, about 50, or
about 55, to about 60, about 65, about 70, about 75, about 80, about 85, about
90, or about 95%, by
weight. In certain embodiments, the amount of sugar alcohol is at least about
50% by weight. such as is
at least about 55% by weight, or at least about 60%, or at least about 65%, or
at least about 70%, or at
least about 75%, or at least about 80%, or at least about 85%, based on the
total weight of the
composition
IS In particular embodiments, the sugar alcohol is isomalt in an amount
of from about 35 to about
55% by weight, based on the total weight of the composition, such as from
about 35, about 40, or about
45, to about 50 or about 55 % by weight.
In particular embodiments, the sugar alcohol is a combination of isomalt in an
amount of from
about 10 to about 25% by weight, such as about 10, about 15, about 20, or
about 25% by weight; and
maltitol in an amount of from about 50 to about 75% by weight, such as about
50, about 55, about 60,
about 65%, about 70, about 75% by weight.
In particular embodiments, the filler is a combination of isomalt in an amount
of from about 30 to
about 50% by weight, based on the total weight of the composition, such as
about 30, about 35, about 40,
about 45, or about 50% by weight; and a glucose-polysaccharide blend (e.g.,
EMDEX ) in an amount of
from about 35 to about 55% by weight, based on the total weight of the
composition, such as about 35,
about 40, about 45, or about 50% by weight.
Lipid
In some embodiments, the composition comprises a lipid. Such compositions may,
in some
embodiments, be described as "meltable" or "melting" compositions, described
further herein below.
When present, the lipid of the composition is typically a fat, oil, or wax
substance derived from animal or
plant material (e.g., plant-derived fats), and typically comprises mostly
triglycerides along with lesser
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amounts of free fatty acids and mono- or diglycerides. In certain embodiments,
the lipid is a solid or semi-
solid at room temperature (i.e., 25 C) and capable of at least partially
liquefying when subjected to the
temperature of the oral cavity of the user (i.e., "melting"). Example plant-
derived fats are comprised
primarily of saturated or unsaturated fatty acid chains (most of which are
bound within triglyceride
structures) having a carbon length of about 10 to about 26 carbon atoms, or
about 14 to about 20 carbon
atoms, or about 14 to about 18 carbon atoms.
In some embodiments, the lipid comprises an oil and, in particular, a food
grade oil, including
fractionated oils. Such oils include, but are not limited to, vegetable oils
(e.g., acai oil, almond oil,
amaranth oil, apricot oil, apple seed oil, argan oil, avocado oil, babassu
oil, beech nut oil, ben oil, bitter
gourd oil, black seed oil, blackcurrant seed oil, borage seed oil, borne
tallow nut oil, bottle gourd oil,
brazil nut oil, buffalo gourd oil, butternut squash seed oil, cape chestnut
oil, canola oil, carob cashew oil,
cocoa butter, cocklebur oil, coconut oil, corn oil, cothune oil, coriander
seed oil, cottonseed oil, date seed
oil, dika oil, egus seed oil, evening primrose oil, false flax oil, flaxseed
oil, grape seed oil, grapefruit seed
oil, hazelnut oil, hemp oil, kapok seed oil, kenaf seed oil, lallemantia oil,
lemon oil, linseed oil,
macadamia oil, mafura oil, marula oil, meadowfoam seed oil, mongongo nut oil,
mustard oil, niger seed
oil, nutmeg butter, okra seed oil, olive oil, orange oil, palm oil, papaya
seed oil, peanut oil, pecan oil,
perilla seed oil, persimmon seed oil, pcqui oil, pili nut oil, pine nut oil,
pistachio oil, pomegranate seed
oil, poppyseed oil, pracaxi oil, prune kernel oil, pumpkin seed oil, quinoa
oil, ramtil oil, rapeseed oil, rice
bran oil, royle oil, sacha inchi oil, safflower oil, sapote oil, seje oil,
sesame oil, shea butter, soybean oil,
sunflower oil, taramira oil, tea seed oil, thistle oil, tigernut oil, tobacco
seed oil, tomato seed oil, walnut
oil, watermelon seed oil, wheat germ oil, and combinations thereof), animal
oils (e.g., cattle fat, buffalo
fat, sheep fat, goat fat, pig fat, lard, camel fat, tallow, liquid margarine,
fish oil, fish liver oil, whale oil,
seal oil, and combinations thereof), and mineral oils.
In certain embodiments, the plant-derived fats of the present disclosure
include palm oil,
(including fractionated palm oil) palm kernel oil, soybean oil, cottonseed
oil, and mixtures thereof. In one
embodiment, the lipid is a blend of palm oil and palm kernel oil. The lipid
can be, for example,
hydrogenated, partially hydrogenated, or non-hydrogenated. Example embodiments
of lipids can be
purchased under the brand names CEBES , CISAO , or CONFAO , available from
AarhusKarlshamn
USA Inc.
The melting point of the lipid is typically about 29 C or above, such as about
29 C to about 49 C,
or about 36 C to about 45 C, or about 38 C to about 41 C. In some
embodiments, use of lipids with a
melting point of less than about 36 C is not advantageous due to possible
melting during product storage
or handling. One test for determining the melting point of lipids is the
Mettler dropping point method
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(ASTM D3954-15, Standard Test Method for Dropping Point of Waxes, ASTM
International, West
Conshohocken, PA, 2015, www.astm.org.).
When present, the amount of lipid within the composition may vary. in certain
embodiments, the
amount of lipid is at least about 10 percent, at least about 20 percent, or at
least about 30 percent, on a dry
weight basis of the composition. In certain embodiments, the amount of lipid
is less than about 70
percent, less than about 60 percent, or less than about 50 weight percent, on
a dry weight basis. Example
lipid weight ranges include about 10 to about 70 dry weight percent, such as
about 35 to about 50 dry
weight percent. In some embodiments, the amount of lipid is about 35, about
40, about 45, or about 50
percent by weight of the total composition.
In some embodiments, the composition comprises a lipid. In one embodiment, the
lipid is an oil
selected from the group consisting of palm oil, palm kernel oil, soybean oil,
sunflower oil, cottonseed oil,
coconut oil, and combinations thereof, wherein the oil may be hydrogenated,
partially hydrogenated, or
non-hydrogenated. In one embodiment, the lipid is a trans-hydrogenated filling
fat of medium hardness
such as Confao 5, available from AarhusKarisharan USA Inc., 131 Marsh Street,
Port Newark, NJ
(M-14.
Active ingredient
The composition as disclosed herein includes one or more active ingredients.
As used herein, an
"active ingredient" refers to one or more substances belonging to any of the
following categories: API
(active pharmaceutical ingredient), food additives, natural medicaments, and
naturally occurring
substances that can have an effect on humans. Example active ingredients
include any ingredient known
to impact one or more biological functions within the body, such as
ingredients that furnish
pharmacological activity or other direct effect in the diagnosis, cure,
mitigation, treatment, or prevention
of disease, or which affect the structure or any function of the body of
humans (e.g., provide a stimulating
action on the central nervous system, have an energizing effect, an
antipyretic or analgesic action, or an
otherwise useful effect on the body). In some embodiments, the active
ingredient may be of the type
generally referred to as dietary supplements, nutraceuticals,
''phytochemicals" or "functional foods."
These types of additives are sometimes defined in the art as encompassing
substances typically available
from naturally-occurring sources (e.g., botanical materials) that provide one
or more advantageous
biological effects (e.g., health promotion, disease prevention, or other
medicinal properties), but are not
classified or regulated as drugs.
Non-limiting examples of active ingredients include those falling in the
categories of botanical
ingredients, stimulants, amino acids, nicotine components, and/or
pharmaceutical, nutraceutical, and
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medicinal ingredients (e.g., vitamins, such as A, B3, B6, B12, and C, and/or
cannabinoids, such as
tetrahydrocannabinol (THC) and cannabidiol (CBD)). Each of these categories is
further described herein
below. The particular choice of active ingredients will vary depending upon
the desired flavor, texture,
and desired characteristics of the particular product.
The particular percentages of active ingredients present will vary depending
upon the desired
characteristics of the particular product. Typically, an active ingredient or
combination thereof is present
in a total concentration of at least about 0.001% by weight of the
composition, such as in a range from
about 0.001% to about 20%. In some embodiments, the active ingredient or
combination of active
ingredients is present in a concentration from about 0.1% w/w to about 10% by
weight, such as, e.g., from
about from about 0.5% w/w to about 10%, from about 1% to about 10%, from about
1% to about 5% by
weight, based on the total weight of the composition. In some embodiments, the
active ingredient or
combination of active ingredients is present in a concentration of from about
0.001%, about 0.01%, about
0.1% , or about 1%, up to about 20% by weight, such as, e.g., from about from
about 0.001%, about
0.002%, about 0.003%, about 0.004%, about 0.005%, about 0.006%, about 0.007%,
about 0.008%, about
0.009%, about 0.01%, about 0.02%, about 0.03%, about 0.04%, about 0.05%, about
0.06%, about 0.07%,
about 0.08%, about 0.09%, about 0.1%, about 0.2%, about 0.3%, about 0.4%,
about 0.5% about 0.6%,
about 0.7%, about 0.8%, or about 0.9%, to about 1%, about 2%, about 3%, about
4%, about 5%, about
6%, about 7%, about 8%, about 9%, about 10%, about 11%, about 12%, about 13%,
about 14%, about
15%, about 16%, about 17%, about 18%, about 19%, or about 20% by weight, based
on the total weight
of the composition. Further suitable ranges for specific active ingredients
are provided herein below.
Botanical
In some embodiments, the active ingredient comprises a botanical ingredient.
As used herein, the
term "botanical ingredient" or "botanical" refers to any plant material or
fungal-derived material,
including plant material in its natural form and plant material derived from
natural plant materials, such as
extracts or isolates from plant materials or treated plant materials (e.g.,
plant materials subjected to heat
treatment, fermentation, bleaching, or other treatment processes capable of
altering the physical and/or
chemical nature of the material). For the purposes of the present disclosure,
a "botanical" includes, but is
not limited to, "herbal materials," which refer to seed-producing plants that
do not develop persistent
woody tissue and are often valued for their medicinal or sensory
characteristics (e.g., teas or tisanes).
Reference to botanical material as "non-tobacco" is intended to exclude
tobacco materials (i.e., does not
include any Nicoiiana species). In some embodiments, the compositions as
disclosed herein can be
characterized as free of any tobacco material (e.g., any embodiment as
disclosed herein may be
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completely or substantially free of any tobacco material). By "substantially
free" is meant that no tobacco
material has been intentionally added. For example, certain embodiments can be
characterized as having
less than 0.001% by weight of tobacco, or less than 0.0001%, or even 0% by
weight of tobacco.
When present, a botanical is typically at a concentration of from about 0.01%
w/w to about 10%
by weight, such as, e.g., from about from about 0.01% w/w, about 0.05%, about
0.1%, or about 0.5%, to
about 1%, about 2%, about 3%, about 4%, about 5%, about 6%, about 7%, about
8%, about 9%, or about
10%, about 11%, about 12%, about 13%, about 14%, or about 15% by weight, based
on the total weight
of the composition.
The botanical materials useful in the present disclosure may comprise, without
limitation, any of
the compounds and sources set forth herein, including mixtures thereof.
Certain botanical materials of
this type are sometimes referred to as dietary supplements, nutraceuticals,
"phytochemicals" or
"functional foods." Certain botanicals, as the plant material or an extract
thereof, have found use in
traditional herbal medicine, and are described further herein. Non-limiting
examples of botanicals or
botanical-derived materials include ashwagandha, Bacopa monniera, baobab,
basil, Centella as/at/ca,
Chai-hu, chamomile, cherry blossom, chlorophyll, cinnamon, citrus, cloves,
cocoa, cordyceps, curcumin,
damiana, Dorstenia arijolia, Dorstenia odorata, essential oils, eucalyptus,
fennel, Galphirnia glauca,
ginger, Ginkgo biloba, ginseng (e.g., Panax ginseng), green tea, Griffonia
simplicifolia, guarana,
cannabis, hemp, hops, jasmine, Kaempferia parviflora (Thai ginseng), kava,
lavender, lemon balm,
lemongrass, licorice, lutein, maca, matcha, Nardostachys chinensis, oil-based
extract of Viola odorata,
peppermint, quercetin, resveratrol, Rhizome gastrodiae, Rhodio la, Moib os ,
rose essential oil, rosemary,
Sceletium tortuosum, Schisandra, Skullcap, spearmint extract, Spikenard,
terpenes, tisanes, turmeric,
Turnera aphrodisiaca, valerian, white mulberry, and Yerba mate.
In some embodiments, the active ingredient comprises lemon balm. Lemon balm
(Melissa
officinalis) is a mildly lemon-scented herb from the same family as mint
(Lamiaceae). The herb is native to
Europe, North Africa, and West Asia. The tea of lemon balm, as well as the
essential oil and the extract, are
used in traditional and alternative medicine. In some embodiments, the active
ingredient comprises lemon
balm extract. In some embodiments, the lemon balm extract is present in an
amount of from about 1 to
about 4% by weight, based on the total weight of the composition.
In some embodiments, the active ingredient comprises ginseng. Ginseng is the
root of plants of the
genus Panax, which are characterized by the presence of unique steroid saponin
phytochemicals
(ginsenosides) and gintonin. Ginseng finds use as a dietary supplement in
energy drinks or herbal teas, and in
traditional medicine. Cultivated species include Korean ginseng (P. ginseng),
South China ginseng (P.
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nologinseng), and American ginseng (P. quinquefollus). American ginseng and
Korean ginseng vary in the
type and quantity of various ginsenosides present. In some embodiments, the
ginseng is American ginseng or
Korean ginseng. In specific embodiments, the active ingredient comprises
Korean ginseng_ in some
embodiments, ginseng is present in an amount of from about 0.4 to about 0.6%
by weight, based on the total
weight of the composition.
Stiinttlants
In some embodiments, the active ingredient comprises one or more stimulants.
As used herein,
the term "stimulant" refers to a material that increases activity of the
central nervous system and/or the
body, for example, enhancing focus, cognition, vigor, mood, alertness, and the
like. Non-limiting
examples of stimulants include caffeine, theacrine, theobromine, and
theophylline. Theacrine
tetrametlyiuric acid) is a purine alkaloid which is structurally related to
caffeine, and possesses stimulant,
analifesic, and anti-inflammatory effects. Present stimulants may be natural,
naturally derived, or wholly
synthetic. For example, certain botanical materials (guarana, tea, coffee,
cocoa, and the like) may possess
a stimulant effect by virtue of the presence of e.g., caffeine or related
alkaloids, and accordingly are
"natural" stimulants. By "naturally derived" is meant the stimulant (e.g.,
caffeine, theacrine) is in a
purified form, outside its natural (e.g., botanical) matrix. For example,
caffeine can be obtained by
extraction and purification from botanical sources (e.g., tea). By "wholly
synthetic", it is meant that the
stimulant has been obtained by chemical synthesis. In some embodiments, the
active ingredient comprises
caffeine. In some embodiments, the caffeine is present in an encapsulated
form. On example of an
encapsulated caffeine is Vitashure , available from Balchem Corp., 52 Sunrise
Park Road, New
Hampton, NY, 10958.
When present, a stimulant or combination of stimulants (e.g., caffeine,
theacrine, and
combinations thereof) is typically at a concentration of from about 0.1% w/w
to about 15% by weight,
such as, e.g., from about from about 0.1% w/w, about 0.2%, about 0.3%, about
0.4%, about 0.5% about
0.6%, about 0.7%, about 0.8%, or about 0.9%, to about 1%, about 2%, about 3%,
about 4%, about 5%,
about 6%, about 7%, about 8%, about 9%, about 10%, about 11%, about 12%, about
13%, about 14%, or
about 15% by weight, based on the total weight of the composition. In some
embodiments, the
composition comprises caffeine in an amount of from about 1.5 to about 6% by
weight, based on the total
weight of the composition;
_Amino acids
In some embodiments, the active ingredient comprises an amino acid. As used
herein, the term
"amino acid" refers to an organic compound that contains amine (-NFI1) and
carboxyl (-COOH) or
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sulfonic acid (SO3H) functional groups, along with a side chain (R group),
which is specific to each
amino acid. Amino acids may be proteinogenic or non-proteinogenic. By
"proteinogenic" is meant that
the amino acid is one of the twenty naturally occurring amino acids found in
proteins. The proteinogenic
amino acids include alanine, arginine, asparagine, aspartie acid, cysteine,
glutamine, glutamic acid,
glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine,
proline, serine, threonine,
tryptopha.n, tyrosine, and valine. By "non-proteinogenic" is meant that either
the amino acid is not found
naturally in protein, or is not directly produced by cellular machinery (e.g.,
is the product of post-
tranlational modification). Non-limiting examples of non-proteinogenic amino
acids include gamma-
aminobutyric acid (GABA), taurine (2-aminoethanesulfonic acid), theanine (L-T-
Outainylethylamido,
hydroxyproline, and beta-alanine. In some embodiments, the active ingredient
comprises theanine. In
some embodiments, the active ingredient comprises GABA. In some embodiments,
the active ingredient
comprises a combination of theanine and GABA. In some embodiments, the active
ingredient is a
combination of theanine, GABA, and lemon balm. In some embodiments, the active
ingredient comprises
a combination of theanine and tryptophan. In some embodiments, the active
ingredient comprises a
combination of theanine and one or more B vitamins. In some embodiments, the
active ingredient is a
combination of caffeine, theanine, and optionally, ginseng. In some
embodiments, the active ingredient
comprises taurinc. In some embodiments, the active ingredient is a combination
of caffeine and taurinc.
Without being bound by any theory of operation, it is believed that certain
amino acids, such as
theanine, tryptopban, GABA, or taurine, can have beneficial impact on mood,
anxiety level, focus, or
cognitive performance, particularly when combined with other active
ingredients, such as caffeine or
certain botanicals.
When present, an amino acid or combination of amino acids (e.g., theanine,
taurine, GABA,
tryptophan, and combinations thereof) is typically at a concentration of from
about 0.01% w/w to about
15% by weight, such as, e.g., from about from about 0.1% w/w, about 0.2%,
about 0.3%, about 0.4%,
about 0.5% about 0.6%, about 0.7%, about 0.8%, or about 0.9%, to about 1%,
about 2%, about 3%, about
4%, about 5%, about 6%, about 7%, about 8%, about 9%, about 10%, about 11%,
about 12%, about 13%,
about 14%, or about 15% by weight, based on the total weight of the
composition.
In one embodiment, the at least one active ingredient comprises tryptophan in
an amount by
weight from about 0.03% to about 1%, or from about 0.05% to about 0.5%.
Vitamins
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In some embodiments, the active ingredient comprises a vitamin or combination
of vitamins. As
used herein, the term "vitamin" refers to an organic molecule (or related set
of molecules) that is an
essential micronutrient needed for the proper functioning of metabolism in a
mammal_ There are thirteen
vitamins required by human metabolism, which are: vitamin A (as all-trans-
retinol, all-trans-retinyl-
esters, as well as all-trans-beta-carotene and other provitamin A
carotenoids), vitamin B1 (thiamine),
vitamin B2 (riboflavin), vitamin B3 (niacin), vitamin B5 (pantothenic acid),
vitamin B6 (pyridoxine),
vitamin B7 (biotin), vitamin B9 (folic acid or folate), vitamin B12
(cobalamins), vitamin C (ascorbic
acid), vitamin D (calciferols), vitamin E (tocopherols and tocotrienols), and
vitamin K (quinones). In
some embodiments, the active ingredient comprises vitamin C. In some
embodiments, the active
ingredient is a combination of vitamin C, caffeine, and taurine. In some
embodiments, the active
ingredient comprises one or more of vitamin B6 and B12. In some embodiments,
the active ingredient
comprises theanine and one or more of vitamin B6 and B12. When present, a
vitamin or combination of
vitamins (e.g., vitamin B6, vitamin B12, vitamin E, vitamin C, or a
combination thereof) is typically at a
concentration of from about 0.0001% to about 6% by weight, such as, e.g., from
about 0.0001, about
0.001, about 0.01%, about 0.02%, about 0.03%, about 0.04%, about 0.05%, about
0.06%, about 0.07%,
about 0.08%, about 0.09%, or about 0.1% w/w, to about 0.2%, about 0.3%, about
0.4%, about 0.5%,
about 0.6%, about 0.7%, about 0.8%, about 0.9%, about 1%, about 2%, about 3%,
about 4%, about 5%,
or about 6% by weight, based on the total weight of the composition.
In some embodiments, the active ingredient comprises vitamin B6 in an amount
from about
0.008% to about 0.06% by weight, or from about 0.01% to about 0.04% by weight.
In some embodiments, the active ingredient comprises vitamin B12 in an amount
from about
0.0001% to about 0.007% by weight, or from about 0.0005% to about 0.001% by
weight.
In some embodiments, the active ingredient comprises a combination of vitamin
B6 and vitamin
B12 in a total amount by weight from about 0.008% to about 0.07%.
Antioxidants
In some embodiments, the active ingredient comprises one or more antioxidants.
As used herein,
the term "antioxidant" refers to a substance which prevents or suppresses
oxidation by terminating free
radical reactions, and may delay or prevent some types of cellular damage.
Antioxidants may be naturally
occurring or synthetic. Naturally occurring antioxidants include those found
in foods and botanical
materials. Non-limiting examples of antioxidants include certain botanical
materials, vitamins,
polyphenols, and phenol derivatives.
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Examples of botanical materials which are associated with antioxidant
characteristics include
without limitation acai berry, alfalfa, allspice, mulatto seed, apricot oil,
basil, bee balm, wild bergamot,
black pepper, blueberries, borage seed oil, bugleweed, cacao, calamus root,
catnip, catuaba, cayenne
pepper, chaga mushroom, chervil, cinnamon, dark chocolate, potato peel, grape
seed, ginseng, gingko
biloba, Saint John's Wort, saw palmetto, green tea, black tea, black cohosh,
cayenne, chamomile, cloves,
cocoa powder, cranberry, dandelion, grapefruit, honeybush, echinacea, garlic,
evening primrose,
feverfew, ginger, goldenseal, hawthorn, hibiscus flower, jiaogulan, kava,
lavender, licorice, marjoram,
milk thistle, mints (menthe), oolong tea, beet root, orange, oregano, papaya,
pennyroyal, peppermint, red
clover, rooibos (red or green), rosehip, rosemary, sage, clary sage, savory,
spearmint, spirulina, slippery
elm bark, sorghum bran hi-tannin, sorghum grain hi-tannin, sumac bran, comfrey
leaf and root, goji
berries, gutu kola, thyme, turmeric, uva ursi, valerian, wild yam root,
wintergreen, yacon root, yellow
dock, yerba mate, yerba santa, bacopa monniera, withania somnifera, Lion's
mane, and silybum
marianum. Such botanical materials may be provided in fresh or dry form,
essential oils, or may be in the
form of an extracts. The botanical materials (as well as their extracts) often
include compounds from
various classes known to provide antioxidant effects, such as minerals,
vitamins, isoflavones,
phvtoesterols, allyl sulfides, dithiolthiones, isothiocyanates, indoles,
lignans, flavonoids, polyphenols, and
carotcnoids. Examples of compounds found in botanical extracts or oils include
ascorbic acid, peanut
endocarb, resveratrol, sulforaphane, beta-carotene, lycopene, lutein, co-
enzyme Q, carnitine, quercetin,
kaempferol, and the like. See, e.g., Santhosh et al., Phytomedicine, 12(2005)
216-220, which is
incorporated herein by reference.
Non-limiting examples of other suitable antioxidants include citric acid_
Vitamin E or a derivative
thereof, a tocopherol, epicatechol, epigallocatechol, epigallocatechol
gallate, erythorbic acid, sodium
erythorbate, 4-hexylresorcinol, theaflavin, the aflavin monogallate A or B,
theaflavin digallate, phenolic
acids, glycosides, quercitrin, isoquercitrin, hyperoside, polyphenols,
catechols, resveratrols, oleuropein,
butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), tertiary
butylhydroquinone (TBHQ),
and combinations thereof.
When present, an antioxidant is typically at a concentration of from about
0.001% w/w to about
10% by weight, such as, e.g., from about from about 0.001%, about 0.005%,
about 0.01% w/w, about
0.05%, about 0.1%, or about 0.5%, to about 1%, about 2%, about 3%, about 4%,
about 5%, about 6%,
about 7%, about 8%, about 9%, or about 10%, based on the total weight of the
composition.
Nicotine component
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In certain embodiments, the active ingredient comprises a nicotine component.
By "nicotine
component" is meant any suitable form of nicotine (e.g., free base or salt)
for providing oral absorption of
at least a portion of the nicotine present Typically, the nicotine component
is selected from the group
consisting of nicotine free base and a nicotine salt. In some embodiments, the
nicotine component is
nicotine in its free base form, which easily can be adsorbed in for example, a
microciystalline cellulose
material to form a microcrystalline cellulose-nicotine carrier complex. See,
for example, the discussion of
nicotine in free base form in US Pat. Pub. No. 2004/0191322 to Hansson, which
is incorporated herein by
reference.
In some embodiments, at least a portion of the nicotine component can be
employed in the form
of a salt. Salts of nicotine can be provided using the types of ingredients
and techniques set forth in US
Pat. No. 2,033,909 to Cox et al. and Perfetti, Beitrage Tabakforschung Int.,
12: 43-54 (1983), which are
incorporated herein by reference. Additionally, salts of nicotine arc
available from sources such as Pfaltz
and Bauer, Inc. and K&K Laboratories, Division of ICN Biochemicals, Inc.
Typically, the nicotine
component is selected from the group consisting of nicotine free base, a
nicotine salt such as
hydrochloride, dihydrochloride, monotartrate, bitartrate, sulfate, salicylate,
and nicotine zinc chloride.
In some embodiments, at least a portion of the nicotine can be in the form of
a resin complex of
nicotine, where nicotine is bound in an ion-exchange resin, such as nicotine
polacrilex, which is nicotine
bound to, for example, a polymethacrilic acid, such as Amberlite IRP64,
Purolite C115HMR, or Doshion
P551. See, for example, US Pat. No. 3,901,248 to Lichtneckert et al., which is
incorporated herein by
reference. Another example is a nicotine-polyacrylic carbomer complex, such as
with Carbopol 974P. In
some embodiments, nicotine may be present in the form of a nicotine
polyacrylic complex.
Typically, the nicotine component (calculated as the free base) when present,
is in a concentration
of at least about 0.001% by weight of the composition, such as in a range from
about 0.001% to about
10%. In some embodiments, the nicotine component is present in a concentration
from about 0.1% w/w to
about 10% by weight, such as, e.g., from about from about 0.1% w/w, about
0.2%, about 0.3%, about
0.4%, about 0.5% about 0.6%, about 0.7%, about 0.8%, or about 0.9%, to about
1%, about 2%, about 3%,
about 4%, about 5%, about 6%, about 7%, about 8%, about 9%, or about 10% by
weight, calculated as the
free base and based on the total weight of the composition. In some
embodiments, the nicotine
component is present in a concentration from about 0.1% w/w to about 3% by
weight, such as, e.g., from
about from about 0.1% w/w to about 2.5%, from about 0.1% to about 2.0%, from
about 0.1% to about
1.5%, or from about 0.1% to about 1% by weight, calculated as the free base
and based on the total
weight of the composition.
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In some embodiments, the products or compositions of the disclosure can be
characterized as free
of any nicotine component (e.g., any embodiment as disclosed herein may be
completely or substantially
free of any nicotine component). By "substantially free" is meant that no
nicotine has been intentionally
added, beyond trace amounts that may be naturally present in e.g., a botanical
material. For example,
certain embodiments can be characterized as having less than 0.001% by weight
of nicotine, or less than
0.0001%, or even 0% by weight of nicotine, calculated as the free base.
In some embodiments, the active ingredient comprises a nicotine component
(e.g., any product or
composition of the disclosure, in addition to comprising any active ingredient
or combination of active
ingredients as disclosed herein, may further comprise a nicotine component).
Cannabinoids
In some embodiments, the active ingredient comprises one or more cannabinoids.
As used herein,
the term "cannabinoid" refers to a class of diverse chemical compounds that
acts on cannabinoid
receptors, also known as the endocannabinoid system, in cells that alter
neurotransmitter release in the
brain. Ligands for these receptor proteins include the endocannabinoids
produced naturally in the body by
Ii animals; phytocannabinoids, found in cannabis; and synthetic
cannabinoids, manufactured artificially.
Cannabinoids found in cannabis include, without limitation: cannabigerol
(CBG), cannabichromene
(CBC), cannabidiol (CBD), tetrahydrocannabinol (THC), cannabinol (CBN),
cannabinodiol (CBDL),
cannabicyclol (CBL), cannabivarin (CBV), tetrahydrocannabivarin (THCV),
cannabidivarin (CBDV),
cannabichromevarin (CBCV), cannabigerovarin (CBGV), cannabigerol 1110110111
ethyl ether (CBGM),
cannabinerolic acid, cannabidiolic acid (CBDA), cannabinol propyl variant
(CBNV), cannabitriol (CBO),
tetrahydrocannabinolic acid (THCA), and tetrahydrocannabivarinic acid (THCV
A). In certain
embodiments, the cannabinoid is selected from tetrahydrocannabinol (THC), the
primary psychoactive
compound in cannabis, and cannabidiol (CBD) another major constituent of the
plant, but which is devoid
of psychoactivity. All of the above compounds can be used in the form of an
isolate from plant material or
synthetically derived.
Alternatively, the active ingredient can be a cannabimimetic, which is a class
of compounds
derived from plants other than cannabis that have biological effects on the
endocannabinoid system
similar to cannabinoids. Examples include yangonin, alpha-amyrin or beta-
amyrin (also classified as
terpenes), cyanidin, curcum in (tumeric), catechin, quercetin, salvinorin A, N-
acylethanolamines, and N-
alkylamide lipids.
When present, a cannabinoid (e.g., CBD) or cannabimimetic is typically in a
concentration of at
least about 0.1% by weight of the composition, such as in a range from about
0.1% to about 30%, such as,
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e.g., from about from about 0.1%, about 0.2%, about 0.3%, about 0.4%, about
0.5% about 0.6%, about
0.7%, about 0.8%, or about 0.9%, to about 1%, about 2%, about 3%, about 4%,
about 5%, about 6%,
about 7%, about 8%, about 9%, about 10%, about 15%, about 20%, or about 30% by
weight, based on the
total weight of the composition.
Terpenes
Active ingredients suitable for use in the present disclosure can also be
classified as terpenes,
many of which are associated with biological effects, such as calming effects.
Terpenes are understood to
have the general formula of (C5H8)11 and include monoterpenes, sesquiterpenes,
and diterpenes. Terpenes
can be acyclic, monocyclic or bicyclic in structure. Some terpenes provide an
entourage effect when used
in combination with eannabinoids or cannabimimetics. Examples include beta-
caryophyllene, linalool,
limonene, beta-citronellol, linalyl acetate, pinene (alpha or beta), geraniol,
carvone, eucalyptol, menthone,
iso-menthone, piperitone, myrcene, beta-bourbonene, and germacrene, which may
be used singly or in
combination.
Pharmaceutical in,gredients
In some embodiments, the active ingredient comprises an active pharmaceutical
ingredient (API).
The API can be any known agent adapted for therapeutic, prophylactic, or
diagnostic use. These can
include, for example, synthetic organic compounds, proteins and peptides,
polysaccharides and other
sugars, lipids, phospholipids, inorganic compounds (e.g., magnesium, selenium,
zinc, nitrate),
neurotransmitters or precursors thereof (e.g., seroton in, 5-
hydroxytryptophan, oxitriptan, acetylcholine,
dopamine, melatonin), and nucleic acid sequences, having therapeutic,
prophylactic, or diagnostic
activity. Non-limiting examples of APIs include analgesics and antipyretics
(e.g., acetylsalicylic acid,
acetaminophen, 3-(4-isobutylphenyl)propanoic acid), phosphatidylserine,
myoinositol, docosahexaenoic
acid (DHA, Omega-3), arachidonic acid (AA, Omega-6), S-adenosylmethionine
(SAM), beta-hydroxy-
beta-methylbutyrate (HMB), citicoline (cytidine-5'-diphosphate-choline), and
cotinine. in some
embodiments, the active ingredient comprises citicoline. In some embodiments,
the active ingredient is a
combination of citicoline, caffeine, theanine, and ginseng. In some
embodiments, the active ingredient
comprises sunflower lecithin. In some embodiments, the active ingredient is a
combination of sunflower
lecithin, caffeine, theanine, and ginseng.
The amount of API may vary. For example, when present, an API is typically at
a concentration
of from about 0.001% w/w to about 10% by weight, such as, e.g., from about
from about 0.01%, about
0.02%, about 0.03%, about 0.04%, about 0.05%, about 0.06%, about 0.07%, about
0.08%, about 0.09%,
about 0.1% w/w, about 0.2%, about 0.3%, about 0.4%, about 0.5% about 0.6%,
about 0.7%, about 0.8%,
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about 0.9%, or about 1%, to about 2%, about 3%, about 4%, about 5%, about 6%,
about 7%, about 8%,
about 9%, or about 10% by weight, based on the total weight of the
composition.
In some embodiments, the composition is substantially free of any API. By
''substantially free of
any API" means that the composition does not contain, and specifically
excludes, the presence of any API
as defined herein, such as any Food and Drug Administration (FDA) approved
therapeutic agent intended
to treat any medical condition.
In certain embodiments, the active ingredient is selected from the group
consisting of caffeine,
taurine, GABA, theanine, tryptophan, vitamin B6, vitamin B12, vitamin C, lemon
balm extract, ginseng,
citicolinc, sunflower lecithin, and combinations thereof. For example, the
active ingredient can include a
combination of caffeine, theanine, and optionally ginseng. In another
embodiment, the active ingredient
includes a combination of theanine, gamma-amino butyric acid (GABA), and
optionally lemon balm
extract. In a further embodiment, the active ingredient includes theanine,
theanine and tryptophan,
theanine and one or more of B vitamin B6 and vitamin B12, or tryptophan,
theanine and one or more of B
vitamin B6 and vitamin B12. In a still further embodiment, the active
ingredient includes a combination
of caffeine, taurine, and vitamin C, optionally further including one or more
B vitaimins (e.g., vitamin B6
or B12). A magnesium salt (e.g., magnesium gluconate) could be added to any of
the above
combinations, particularly combinations also including theanine.
Water
The moisture content (e.g., water content) of the composition, prior to use by
a consumer of the
product, may vary according to the desired properties. Typically, the
composition, prior to insertion into
the mouth of the user, is less than about 60% by weight of water, and
generally is from about 1 to about
60% by weight of water, for example, from about 5 to about 55%, about 10 to
about 50%, about 20 to
about 45%, or about 25 to about 40% water by weight, including water amounts
of at least about 5% by
weight, at least about 10% by weight, at least about 15% by weight, and at
least about 20% by weight.
Salts
In some embodiments, the composition comprises a salt (e.g., an alkali metal
salt), typically
employed in an amount sufficient to provide desired sensory attributes to the
composition. Non-limiting
examples of suitable salts include sodium chloride, potassium chloride,
ammonium chloride, flour salt,
sodium acetate, sodium citrate, calcium citrate, and the like. In some
embodiments, the salt is sodium
chloride, ammonium chloride, or a combination thereof. In some embodiments,
the salt is trisodium
citrate, calcium citrate, or a combination thereof.
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When present, a representative amount of salt is about 0.1% by weight or more,
about 0.5% by
weight or more, about 1.0% by weight or more, or about 1.5% by weight or more,
but will typically make
up about 10% or less of the total weight of the composition, or about 7.5% or
less, or about 5% or less
(e.g., from about 0.1 to about 5% by weight).
Sweeteners
In order to improve the sensory properties of the composition according to the
disclosure, one or
more sweeteners may be added. The sweeteners can be any sweetener or
combination of sweeteners, in
natural or artificial form, or as a combination of natural and artificial
sweeteners. Examples of natural
sweeteners include fructose, sucrose, glucose, maltose, isomaltulosc, mannosc,
galactose, lactose, stcvia,
honey, and the like. Examples of artificial sweeteners include sucralose,
maltodextrin, saccharin,
aspartame, acesulfame K, neotame, and the like. In some embodiments, the
sweetener comprises one or
more sugar alcohols. Sugar alcohols are polyols derived from monosaccharides
or disaccharides that
have a partially or fully hydrogenated form. Sugar alcohols have, for example,
about 4 to about 20
carbon atoms and include erythritol, arabitol, ribitol, isomalt, maltitol,
dulcitol, iditol, mannitol, xylitol,
lactitol, sorbitol, and combinations thereof (e.g., hydrogenated starch
hydrolysates). In some
embodiments, the sweetener is sucralose, acesulfame K, or a combination
thereof.
When present, a sweetener or combination of sweeteners may make up from about
0.01 to about
20% or more of the of the composition by weight, for example, from about 0.01
to about 0.1, from about
0.1 to about 1%, from about 1 to about 5%, from about 5 to about 10%, or from
about 10 to about 20% by
weight, based on the total weight of the composition. In some embodiments, a
combination of sweeteners
is present at a concentration of from about 0.01% to about 0.1% by weight of
the composition, such as
about 0.01, about 0.02, about 0.03, about 0.04, about 0.05, about 0.06, about
0.07, about 0.08, about 0.09,
or about 0.1% by weight of the composition. In some embodiments, a combination
of sweeteners is
present at a concentration of from about 0.1% to about 0.5% by weight of the
composition, such as about
0.1, about 0.2, about 0.3, about 0.4, or about 0.5% by weight of the
composition. In some embodiments, a
combination of sweeteners is present at a concentration of from about 1% to
about 3% by weight of the
composition.
Flavoring agents
In some embodiments, the composition comprises a flavoring agent. As used
herein, a "flavoring
agent," "flavor" or "flavorant" is any flavorful or aromatic substance capable
of altering the sensory
characteristics associated with the oral product. Examples of sensory
characteristics that can be modified
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by the flavoring agent include taste, mouthfeel, moistness, coolness/heat,
and/or fragrance/aroma.
Flavoring agents may be natural or synthetic, and the character of the flavors
imparted thereby may be
described, without limitation, as fresh, sweet, herbal, confectionary, floral,
fruity, or spicy_ Specific types
of flavors include, but are not limited to, vanilla, coffee, chocolate/cocoa,
cream, mint, spearmint,
menthol, peppermint, wintergreen, eucalyptus, lavender, cardamom, nutmeg,
cinnamon, clove, cascarilla,
sandalwood, honey, jasmine, ginger, anise, sage, licorice, lemon, orange,
apple, peach, lime, cherry,
strawberry, trigeminal sensates, terpenes, and any combinations thereof. See
also, Leffingwell et al.,
Tobacco Flavoring for Smoking Products, R. J. Reynolds Tobacco Company (1972),
which is
incorporated herein by reference. Flavoring agents also may include components
that are considered
moistening, cooling or smoothening agents, such as eucalyptus. These flavors
may be provided neat (i.e.,
alone) or in a composite, and may be employed as concentrates or flavor
packages (e.g., spearmint and
menthol, orange and cinnamon; lime, pineapple, and the like). Representative
types of components also
are set forth in US Pat. No. 5,387,416 to White et al.; US Pat. App. Pub. No.
2005/0244521 to Strickland
et al.; and PCT Application Pub. No. WO 05/041699 to Quinter et al., each of
which is incorporated
herein by reference. In some instances, the flavoring agent may be provided in
a spray-dried form or a
liquid form.
The amount of flavoring agent utilized in the composition can vary, but is
typically up to about
10% by weight, and certain embodiments are characterized by a flavoring agent
content of at least about
0.1% by weight, such as about 0.5 to about 10%, about 1 to about 5%, or about
2 to about 4% weight,
based on the total weight of the composition.
Taste modifiers
In order to improve the organoleptic properties of a composition as disclosed
herein, the
composition may include one or more taste modifying agents ("taste modifiers")
which may serve to
mask, alter, block, or improve e.g., the flavor of a composition as described
herein. Non-limiting
examples of such taste modifiers include analgesic or anesthetic herbs,
spices, and flavors which produce
a perceived cooling (e.g., menthol, eucalyptus, mint), warming (e.g.,
cinnamon), or painful (e.g.,
capsaicin) sensation. Certain taste modifiers fall into more than one
overlapping category.
In some embodiments, the taste modifier modifies one or more of bitter, sweet,
salty, or sour
tastes. In some embodiments, the taste modifier targets pain receptors. In
some embodiments, the
composition comprises an active ingredient having a bitter taste, and a taste
modifier which masks or
blocks the perception of the bitter taste. In some embodiments, the taste
modifier is a substance which
targets pain receptors (e.g., vanilloid receptors) in the user's mouth to mask
e.g., a bitter taste of another
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component (e.g., an active ingredient). Suitable taste modifiers include, but
are not limited to, capsaicin,
gamma-amino butyric acid (GABA), adenosine monophosphate (AMP), lactisole, or
a combination
thereof
When present, a representative amount of taste modifier is about 0.01% by
weight or more, about
0.1% by weight or more, or about 1.0% by weight or more, but will typically
make up less than about
10% by weight of the total weight of the composition, (e.g., from about 0.01%,
about 0.05%, about 0.1%,
or about 0.5%, to about 1%, about 5%, or about 10% by weight of the total
weight of the composition).
Binders
A binder (or combination of binders) may be employed in certain embodiments,
in amounts
sufficient to provide the desired physical attributes and physical integrity
to the composition, and binders
also often function as thickening or gelling agents. Typical binders can be
organic or inorganic, or a
combination thereof. Representative binders include cellulose derivatives
(e.g., cellulose ethers),
povidone, sodium alginate, starch-based binders, pectin, gums, carrageenan,
pullulan, zein, and the like,
and combinations thereof. In some embodiments, the binder comprises pectin or
carrageenan or
combinations thereof.
The amount of binder utilized in the composition can vary based on the binder
and the desired
composition properties, but is typically up to about 30% by weight, and
certain embodiments are
characterized by a binder content of at least about 0.1% by weight, such as
about 0.5 to about 30% by
weight, or about 1 to about 10% by weight, based on the total weight of the
composition.
In certain embodiments, the binder includes a gum, for example, a natural gum.
As used herein, a
natural gum refers to polysaccharide materials of natural origin that have
binding properties, and which
are also useful as a thickening or gelling agents. Representative natural gums
derived from plants, which
are typically water soluble to some degree, include xanthan gum, guar gum, gum
arabic, ghatti gum, gum
tragacanth, karaya gum, locust bean gum, gellan gum, and combinations thereof.
When present, natural
gum binder materials are typically present in an amount of up to about 5% by
weight, for example, from
about 0.1, about 0.2, about 0.3, about 0.4, about 0.5, about 0.6, about 0.7,
about 0.8, about 0.9, or about
1%, to about 2, about 3, about 4, or about 5% by weight, based on the total
weight of the composition.
In some embodiments, the binder comprises pectin. Pectins are natural polymers
related to
carbohydrates and which are acidic heteropolysaccharides (polysaccharides
comprising multiple
monosaccharide units). As opposed to carbohydrates, the pectin C-6 position
contains a carboxylic acid
(or corresponding methyl ester or carboxamide) group instead of a
hydroxymethyl group. The principal
subunit is known as galacturonic acid, which can be copolymerized with L-
rhamnose. Other sugars are
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featured as side-chain substituents. Pectin acts as a thickening and gelling
agent. Pectin isolated from
sources such as apple pomace, citrus peels, sugarbeet waste from sugar
manufacturing, sunflower heads
discarded from seed harvesting, mango waste, and other commercially available
pectins may be used. in
combination with certain sugars, under acidic conditions (e.g., a pH of from
about 2.5 to about 5), or in
the presence of a gelation agent (calcium or other divalent alkaline earth
elements), pectins may provide a
gel or gum consistency to compositions as disclosed herein. In some
embodiments, the binder comprises
low methoxy pectin. Suitable low methoxy pectins include, for example, "GENU
pectin type LM-104
AS", available from CP Kelco, Atlanta, GA, USA. In some embodiments, the
binder comprises low
methoxy pectin in combination with a gelation agent. In some embodiments, the
gelation agent comprises
calcium ions, such as, but not limited to, calcium diphosphate. In some
embodiments, the binder
comprises a high methoxy pectin in combination with an organic acid, described
herein below. In some
embodiments, the binder comprises a high methoxy pectin in combination with
citric acid.
When present, a pectin binder is typically present in an amount of up to about
3% by weight, for
example, from about 0.1, about 0.2, about 0.3, about 0.4, about 0.5, about
0.6, about 0.7, about 0.8, about
0.9, or about 1, to about 1.1, about 1.2, about 1.3, about 1.4, about 1.5,
about 1.6, about 1.7, about 1.8.
about 1.9, about 2, about 2.1, about 2.2, about 2.3. about 2.4, about 2.5,
about 2.6, about 2.7, about 2.8,
about 2.9, or about 3% by weight, based on the total weight of the
composition.
Organic acid
In some embodiments, the composition comprises an organic acid. As used
herein, the term
"organic acid" refers to an organic (i.e., carbon-based) compound that is
characterized by acidic
properties. Typically, organic acids are relatively weak acids (i.e., they do
not dissociate completely in the
presence of water), such as carboxylic acids (-CO2H) or sulfonic acids (-
S020H). As used herein,
reference to organic acid means an organic acid that is intentionally added.
In this regard, an organic acid
may be intentionally added as a specific mixture ingredient as opposed to
merely being inherently present
as a component of another mixture ingredient (e.g., the small amount of
organic acid which may
inherently be present in a mixture ingredient such as a tobacco material). In
some embodiments, the one
or more organic acids are added neat (i.e., in their free acid, native solid
or liquid form) or as a solution in,
e.g., water. In some embodiments, the one or more organic acids are added in
the form of a salt, as
described herein below.
Suitable organic acids will typically have a range of lipophilicities (i.e., a
polarity giving an
appropriate balance of water and organic solubility). Lipophilicity is
conveniently measured in terms of
logP, the partition coefficient of a molecule between an aqueous and
lipophilic phase, usually water and
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octanol, respectively. Typically, lipophilicities of organic acids may be
between about -2 and about 6.5.
In some embodiments, the organic acid may be more soluble in water than in
octanol (i.e., having a
negative logP value, such as from about -2 to about -1). in some embodiments,
the organic acid may be
about equally soluble in octanol than in water (i.e., having a logP value of
about 0). In some
embodiments, the organic acid may be more soluble in octanol than in water
(i.e., having a positive logP
value, such as from about 1 to about 6.5). In some embodiments, the organic
acid has a logP value of
from about 1.5 to about 5.0, e.g., from about 1.5, about 2.0, about 2.5, or
about 3.0, to about 3.5, about
4.0, about 4.5, or about 5Ø
In some embodiments, the organic acid is a carboxylic acid or a sulfonic acid.
The carboxylic
acid or sulfonic acid functional group may be attached to any alkyl,
cycloalkyl, heterocycloalkyl, aryl, or
heteroaryl group having, for example, from one to twenty carbon atoms (Ci-
C20). In some embodiments,
the organic acid is an alkyl, cycloalkyl, heterocycloalkyl, aryl, or
heteroaryl carboxylic or sulfonic acid.
As used herein. "alkyl" refers to any straight chain or branched chain
hydrocarbon. The alkyl
group may be saturated (i.e., having all sp3 carbon atoms), or may be
unsaturated (i.e., having at least one
site of unsathration). As used herein, the term "unsaturated" refers to the
presence of a carbon-carbon, sp2
double bond in one or more positions within the alkyl group. Unsaturated alkyl
groups may be mono- or
polyunsaturated. Representative straight chain alkyl groups include, but are
not limited to, methyl, ethyl,
n-propyl, n-butyl, n-pentyl, and n-hexyl. Branched chain alkyl groups include,
but are not limited to,
isopropyl, sec-butyl, isobutyl, tert-butyl, isopentyl, and 2-methylbutyl.
Representative unsaturated alkyl
groups include, but are not limited to, ethylene or vinyl, ally-1, 1-butenyl,
2-butenyl, isobutylenyl, 1-
pentenyl, 2-pentenyl, 3-methy1-1-butenyl, 2-methy-1-2-butenyl, 2,3-dimethy1-2-
butenyl, and the like. An
alkyl group can be unsubstituted or substituted.
"Cycloalkyl" as used herein refers to a carbocyclic group, which may be mono-
or bicyclic.
Cycloalkyl groups include rings having 3 to 7 carbon atoms as a monocycle or 7
to 12 carbon atoms as a
bicycle. Examples of monocyclic cycloalkyl groups include cyclopropyl,
cyclobutyl, cyclopcntyl,
cyclohexyl, cycloheptyl, and cyclooctyl. A cycloalkyl group can be
unsubstituted or substituted, and may
include one or more sites of unsaturation (e.g., cyclopentenyl or
cyclohexenyl).
The term "aryl" as used herein refers to a carbocyclic aromatic group.
Examples of aryl groups
include, but are not limited to, phenyl and naphthyl. An aryl group can be
unsubstituted or substituted.
"fieteroaryl" and "heterocycloalkyl" as used herein refer to an aromatic or
non-aromatic ring
system, respectively, in which one or more ring atoms is a heteroatom, e.g.
nitrogen, oxygen, and sulfur.
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The heteroaryl or heterocycloalkyl group comprises up to 20 carbon atoms and
from 1 to 3 heteroatoms
selected from N, 0, and S. A heteroaryl or heterocycloalkyl may be a monocycle
having 3 to 7 ring
members (for example, 2 to 6 carbon atoms and 1 to 3 heteroatoms selected from
N, 0, and 5) or a
bicycle having 7 to 10 ring members (for example, 4 to 9 carbon atoms and 1 to
3 heteroatoms selected
from N, 0, and S), for example: a bicyclo[4,5], [5,5], [5,6], or [6,6] system.
Examples of heteroaryl
groups include by way of example and not limitation, pyridyl, thiazolyl,
tetrahydrothiophenyl,
pyrimidinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl,
benzofuranyl, thianaphthalenyl,
indolyl, indolenyl, quinolinyl, isoquinolinyl, benzimidazolyl, isoxazolyl,
pyrazinyl, pyridazinyl,
indolizinyl, isoindolyl, 3H-indoly-1, 1H-indazolyl, purinyl, 4H-quinolizinyl,
phthalazinyl, naphthyridinyl,
quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4 aH-c arb azolyl,
carbazolyl, phen an thridinyl, acridinyl,
pyrimidinyl, phenanthrolinyl, phenazinyl, phenothiazinyl, furazanyl,
phenoxazinyl, isochromanyl,
chromanyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl,
benzotriazolyl, benzisoxazolyl, and
isatinoyl. Examples of heterocycloalkyls include by way of example and not
limitation, dihydroypyridyl,
tetrahydropyridyl (piperidyl), tetrahydrothiophenyl, piperidinyl, 4-
piperidonyl, pyrrolidinyl, 2-
pyrrolidonyl, tetrahydrofuranyl, tetrahydropyranyl, bis-tetrahydropyranyl,
tetrahydroquinolinyl,
tetrahydroisoquinolinyl, decahvdroquinolinyl, octahydroisoquinolinyl,
piperazinyl, quinuclidinyl, and
morpholinyl. Heteroaryl and heterocycloalkyl groups can be unsubstituted or
substituted.
"Substituted" as used herein and as applied to any of the above alkyl, aryl,
cycloalkyl, heteroaryl,
beterocyclyl, means that one or more hydrogen atoms are each independently
replaced with a substituent.
Typical substituents include, but are not limited to, -Cl, Br, F, alkyl, -OH, -
OCH3, NH2, -NHCH3, -
N(CH3)2, -CN, -NC(=0)CH3, -C(-0)-, -C(=0)NH2, and -C(=0)N(CH3)2. Wherever a
group is described
as "optionally substituted," that group can be substituted with one or more of
the above substituents,
independently selected for each occasion. In some embodiments, the substituent
may be one or more
methyl groups or one or more hydroxyl groups.
In some embodiments, the organic acid is an alkyl carboxylic acid. Non-
limiting examples of
alkyl carboxylic acids include formic acid, acetic acid, propionic acid,
octanoic acid, nonanoic acid,
decanoic acid, undecanoic acid, dodecanoic acid, stearic acid, oleic acid,
linoleic acid, linolenic acid, and
the like. In some embodiments, the organic acid is an alkyl sulfonic acid. Non-
limiting examples of alkyl
sulfonic acids include propanesulfonic acid and octanesulfonic acid.
In some embodiments, the alkyl carboxylic or sulfonic acid is substituted with
one or more
hydroxyl groups. Non-limiting examples include glycolic acid, 4-hydroxybutyric
acid, and lactic acid.
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In some embodiments, an organic acid may include more than one carboxylic acid
group or more
than one sulfonic acid group (e.g., two, three, or more carboxylic acid
groups). Non-limiting examples
include oxalic acid, fumaric acid, maleic acid, and glutaric acid. In organic
acids containing multiple
carboxylic acids (e.g., from two to four carboxylic acid groups), one or more
of the carboxylic acid
groups may be esterified. Non-limiting examples include succinic acid
monoethyl ester, monomethyl
fumarate, monomethyl or dimethyl citrate, and the like.
In some embodiments, the organic acid may include more than one carboxylic
acid group and one
or more hydroxyl groups. Non-limiting examples of such acids include tartaric
acid, citric acid, and the
like. In some embodiments, the organic acid is citric acid, sodium citrate,
calcium citrate, or a
combination thereof.
In some embodiments, the organic acid is an awl carboxylic acid or an awl
sulfonic acid. Non-
limiting examples of aryl carboxylic and sulfonic acids include benzoic acid,
toluic acids, salicylic acid,
benzenesulfonic acid, andp-toluenesulfonic acid.
Additional non-limiting examples of suitable organic acids include 2,2-
dichloroacetic acid, 2-
hydroxyethanesulfonic acid, 2-oxoglutaric acid, 4-acetamidobenzoic acid, 4-
aminosalicylic acid, acetic
acid, adipic acid, ascorbic acid (L), aspartic acid (L), camphoric acid (+),
camphor-10-sulfonic acid (+),
capric acid, caproic acid, caprylic acid, cinnamic acid, cyclamic acid,
decanoic acid, dodecylsulfuric acid,
ethane-1,2-disulfonic acid, ethanesulfonic acid, formic acid, fumaric acid,
galactaric acid, gentisic acid,
glucoheptonic acid, gluconic acid, glucuronic acid, glutamic acid,
glycerophosphoric acid, glycolic acid,
hippuric acid, isobutyric acid, lactobionic acid, lauric acid, malonic acid,
mandelic acid, methanesulfonic
acid, naphthalene-1,5-disulfonic acid, naphthalene-2-sulfonic acid, oleic
acid, palmitic acid, pamoic acid,
pyroglutamic acid, sebacic acid, stearic acid, and undecylenic acid.
In some embodiments, the one or more organic acids is a single organic acid.
In some
embodiments, the one or more organic acids is a combination of several acids,
such as two, three, or more
organic acids
The amount of organic acid present in the composition may vary. Generally, the
mixture
comprises from about 0.1 to about 10% by weight of organic acid, present as
one or more organic acids,
based on the total weight of the composition. In some embodiments, the
composition comprises about
0.1%, about 0.2%, about 0.3%, about 0.4%, about 0.5%, about 0.6%, about 0.7%,
about 0.8%, about
0.9%, about 1%, about 2%, about 3%, about 4%, about 5%, about 6%, about 7%,
about 8%, about 9%, or
about 10% organic acid by weight, based on the total weight of the
composition. In some embodiments,
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the composition comprises from about 0.1 to about 0.5% by weight of organic
acid, for example, about
0.1, about 0.15, about 0.2, about 0.25, about 0.3, about 0.35, about 0.4,
about 0.45, or about 0.5% by
weight, based on the total weight of the composition. In some embodiments, the
composition comprises
from about 0.25 to about 0.35% by weight of organic acid, for example, from
about 0.25, about 0.26,
about 0.27, about 0.28, about 0.29, or about 0.3, to about 0.31, about 0.32,
about 0.33, about 0.34, or
about 0.35% by weight, based on the total weight of the composition. In the
case where a salt of an
organic acid is added (e.g., sodium citrate), the percent by weight is
calculated based on the weight of the
free acid, not including any counter-ion which may be present.
Organic acids (e.g., citric acid) may be added neat (i.e., as a solid) or in
solution, for example, in
water. In some embodiments, the organic acid is added as a 50% aqueous
solution.
Buffering agents
In certain embodiments, the composition of the present disclosure can comprise
pH adjusters or
buffering agents. Examples of pH adjusters and buffering agents that can be
used include, but are not
limited to, metal hydroxides (e.g., alkali metal hydroxides such as sodium
hydroxide and potassium
hydroxide), and other alkali metal buffers such as metal carbonates (e.g.,
potassium carbonate or sodium
carbonate), or metal bicarbonates such as sodium bicarbonate, and the like.
Non-limiting examples of
suitable buffers include alkali metals acetates, glycinates,
phosphates, glycerophosphates, citrates,
carbonates, hydrogen carbonates, borates, or mixtures thereof. In some
embodiments, the buffer is
sodium bicarbonate.
Where present, the buffering agent is typically present in an amount less than
about 5% by
weight, based on the weight of the composition, for example, from about 0.1%
to about 5%, such as, e.g.,
from about 0.1% to about 1%, or from about 0.1% to about 0.5% by weight, based
on the total weight of
the composition.
Colorants
A colorant may be employed in amounts sufficient to provide the desired
physical attributes to
the composition. Examples of colorants include various dyes and pigments, such
as caramel coloring and
titanium dioxide. Natural colorants such as curcumin, beet juice extract,
spirulina; also a variety of
synthetic pigments may also be used. The amount of colorant utilized in the
composition can vary, but
when present is typically up to about 3% by weight, such as from about 0.1%,
about 0.5%, or about 1%,
to about 3% by weight, based on the total weight of the composition.
Humectants
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In certain embodiments, one or more humectants may be employed in the
composition.
Examples of humectants include, but are not limited to, glycerin, propylene
glycol, and the like. Where
included, the hutnectant is typically provided in an amount sufficient to
provide desired moisture
attributes to the composition. Further, in some instances, the humectant may
impart desirable flow
characteristics to the composition for depositing in a mold. When present, a
humectant will typically
make up about 5% or less of the weight of the composition (e.g., from about
0.1 to about 5% by weight),
for example, from about 0.1% to about 1% by weight, or about 1% to about 5% by
weight, based on the
total weight of the composition.
Oral care additives
In sonic embodiments, the composition comprises an oral care ingredient (or
mixture of such
ingredients). Oral care ingredients provide the ability to inhibit tooth decay
or loss, inhibit gum disease,
relieve mouth pain, whiten teeth, or otherwise inhibit tooth staining, elicit
salivary stimulation, inhibit
breath malodor, freshen breath, or the like. For example, effective amounts of
ingredients such as thyme
oil, eucalyptus oil and zinc (e.g., such as the ingredients of formulations
commercially available as
ZYTEX from Discus Dental) can be incorporated into the composition. Other
examples of ingredients
that can be incorporated in desired effective amounts within the present
composition can include those
that are incorporated within the types of oral care compositions set forth in
Takahashi et al., Oral
Microbiology and Immunology, 19(1), 61-64 (2004); U.S. Pat. No. 6,083,527 to
Thistle; and US Pat.
Appl. Pub. Nos. 2006/0210488 to Jakubowski and 2006/02228308 to Cummins et al.
Other exemplary
ingredients of tobacco containing-formulation include those contained in
formulations marketed as
MALTISORB by Roquette and DENTIZYME by NatraRx. When present, a
representative amount of
oral care additive is at least about 1%, often at least about 3%, and
frequently at least about 5% of the
total dry weight of the composition. The amount of oral care additive within
the composition will not
typically exceed about 30%, often will not exceed about 25%, and frequently
will not exceed about 20%,
of the total dry weight of the composition.
Processing aids
If necessary for downstream processing of the composition, such as
granulation, mixing, or
molding, a flow aid can also be added to the composition in order to enhance
flowability of the
composition. In some embodiments, the composition (e.g., melt and chew forms)
may be surface treated
with anti-stick agents, such as oils, silicones, and the like. Exemplary flow
aids include microcrystalline
cellulose, silica, polyethylene glycol, stearic acid, calcium stearate,
magnesium stearate, zinc stearate,
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sodium stearyl fumarate, canauba wax, and combinations thereof. In some
embodiments, the flow aid is
sodium stearyl fumarate.
When present, a representative amount of flow aid may make up at least about
0.5 percent or at
least about 1 percent, of the total dry weight of the composition. Preferably,
the amount of flow aid within
the composition will not exceed about 5 percent, and frequently will not
exceed about 3 percent, of the
total dry weight of the composition.
Emulsifier
In certain embodiments, an emulsifier may be added. In some embodiments, the
emulsifier is
lecithin. For example, lecithin (e.g., soy lecithin or sunflower lecithin) may
be added to the composition
to provide smoother textural properties to the composition and to improve
flowability and mixing of e.g.,
a lipid with the remaining components of the composition. Emulsifiers (e.g.,
lecithin) can be used in an
amount of about 0.01 to about 5% by dry weight of the composition, such as
from about 0.1 to about
2.5%, or from about 0.1 to about 1.0% based on the total weight of the
composition.
Other additives
Other additives can be included in the disclosed composition. For example, the
composition can
be processed, blended, formulated, combined, and/or mixed with other materials
or ingredients. The
additives can be artificial, or can be obtained or derived from 'herbal or
biological sources. Examples of
further types of additives include thickening or gelling agents (e.g., fish
gelatin), emulsifiers,
preservatives (e.g., potassium sorbate and the like), disintegration aids,
zinc or magnesium salts selected
to be relatively water soluble for compositions with greater water solubility
(e.g., magnesium or zinc
gluconate) or selected to be relatively water insoluble for compositions with
reduced water solubility
(e.g., magnesium or zinc oxide), or combinations thereof. See, for example,
those representative
components, combination of components, relative amounts of those components,
and manners and
methods for employing those components, set forth in US Pat. No. 9,237,769 to
Mua et al., US Pat. No.
7,861,728 to Holton, Jr. et al., US Pat. App. Pub. No. 2010/0291245 to Gao et
al., and US Pat. App. Pub.
No. 2007/0062549 to Holton, Jr. et al., each of which is incorporated herein
by reference. Typical
inclusion ranges for such additional additives can vary depending on the
nature and function of the
additive and the intended effect on the final composition, with an example
range of up to about 10% by
weight, based on total weight of the composition (e.g., about 0.1 to about 5%
by weight).
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In some embodiments, the composition comprises a magnesium salt. A non-
limiting example of a
suitable magnesium salt is magnesium gluconate. In some embodiments, the
composition comprises
magnesium in an amount by weight from about 0.1% to about 2%, or from about 01
to about 1%, based
on elemental magnesium.
The aforementioned additives can be employed together (e.g., as additive
formulations) or
separately (e.g., individual additive components can be added at different
stages involved in the
preparation of the final composition). Furthermore, the aforementioned types
of additives may be
encapsulated as provided in the final product or composition. Exemplary
encapsulated additives are
described, for example, in W02010/132444 to Atchley, which has been previously
incorporated by
reference herein.
Configured for oral use
Provided herein is a composition configured for oral use. The term "configured
for oral use" as
used herein means that the composition is provided in a form such that during
use, saliva in the mouth of
the user causes one or more of the components of the composition (e.g.,
flavoring agents and/or active
ingredients) to pass into the mouth of the user. In certain embodiments, the
composition is adapted to
deliver components to a user through mucous membranes in the user's mouth, the
user's digestive system,
or both, and, in some instances, said component is an active ingredient
(including, but not limited to, for
example, a stimulant, vitamin, an amino acid, a botanical, or combinations
thereof) that can be absorbed
through the mucous membranes in the mouth or absorbed through the digestive
tract when the product is
used.
Compositions configured for oral use as described herein may take various
forms, including gels,
pastilles, gums, chews, melts, tablets, lozenges, powders, and pouches. Gels
can be soft or hard. Certain
compositions configured for oral use are in the form of pastilles. As used
herein, the term "pastille" refers
to a dissolvable oral composition made by solidifying a liquid or gel
composition so that the final
composition is a somewhat hardened solid gel The rigidity of the gel is highly
variable Certain
compositions of the disclosure are in the form of solids. Certain compositions
can exhibit, for example,
one or more of the following characteristics: crispy, granular, chewy, syrupy,
pasty, fluffy, smooth, and/or
creamy. In certain embodiments, the desired textural property can be selected
from the group consisting
of adhesiveness, cohesiveness, density, dryness, fracturability, graininess,
gumminess, hardness,
heaviness, moisture absorption, moisture release, mouthcoating, roughness,
slipperiness, smoothness,
viscosity, wetness, and combinations thereof.
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The compositions as disclosed herein can be formed into a variety of shapes,
including pills,
tablets, spheres, strips, films, sheets, coins, cubes, beads, ovoids, obloids,
cylinders, bean-shaped, sticks,
or rods. Cross-sectional shapes of the composition can vary, and example cross-
sectional shapes include
circles, squares, ovals, rectangles, and the like. Such shapes can be formed
in a variety of manners using
equipment such as moving belts, nips, extruders, granulation devices,
compaction devices, and the like.
The compositions of the present disclosure may be dissolvable. As used herein,
the terms
"dissolve," "dissolving," and "dissolvable" refer to compositions having
aqueous-soluble components that
interact with moisture in the oral cavity and enter into solution, thereby
causing gradual consumption of
the composition. According to one aspect, the dissolvable composition is
capable of lasting in the user's
mouth for a given period of time until it completely dissolves. Dissolution
rates can vary over a wide
range, from about 1 minute or less to about 60 minutes. For example, fast
release compositions typically
dissolve and/or release the desired component(s) (e.g., active ingredient,
flavor, and the like) in about 2
minutes or less, often about 1 minute or less (e.g., about 50 seconds or less,
about 40 seconds or less,
about 30 seconds or less, or about 20 seconds or less). Dissolution can occur
by any means, such as
melting, mechanical disruption (e.g., chewing), enzymatic or other chemical
degradation, or by disruption
of the interaction between the components of the composition. In other
embodiments, the products do not
dissolve during the product's residence in the user's mouth.
In some embodiments, the composition can be chewable, meaning the composition
has a mild
resilience or "bounce" upon chewing, and possesses a desirable degree of
malleability. A composition in
chewable form may be entirely dissolving, or may be in the form of a non-
dissolving gum in which only
certain components (e.g., active ingredients, flavor, sweetener) dissolve,
leaving behind a non-dissolving
matrix. Chewable embodiments generally include a binder, such as a natural gum
or pectin. In some
embodiments, the composition in chewable form comprises pectin and an organic
acid, along with one or
more sugar alcohols in an amount by weight of at least 50%, based on the total
weight of the composition.
Generally, the pectin is present in an amount of from about 1 to about 3% by
weight, based on the total
weight of the composition.
In some embodiments, the composition can be meltable as discussed, for
example, in US Patent
App. Pub. No. 2012/0037175 to Cantrell et al., incorporated by reference
herein in its entirety. As used
herein, "melt," "melting," and ¶meltable" refer to the ability of the
composition to change from a solid
state to a liquid state. That is, melting occurs when a substance (e.g., a
composition as disclosed herein)
changes from solid to liquid, usually by the application of heat. The
application of heat in regard to a
composition as disclosed herein is provided by the internal temperature of a
user's mouth. Thus, the term
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µ`meltable" refers to a composition that is capable of liquefying in the mouth
of the user as the
composition changes phase from solid to liquid, and is intended to distinguish
compositions that merely
disintegrate in the oral cavity through loss of cohesiveness within the
composition that merely dissolve in
the oral cavity as aqueous-soluble components of the composition interact with
moisture. Generally,
meltable compositions comprise a lipid as described herein above. In some
embodiments, the composition
in meltable form comprises a lipid in an amount of from about 35 to about 50%
by weight, based on the
total weight of the composition, and a sugar alcohol in an amount of from
about 35 to about 55% by
weight, based on the total weight of the composition. In some embodiments, the
sugar alcohol is isomalt,
erythritol, sorbitol, arabitol, ribitol, maltitol, dulcitol, iditol, mannitol,
xylitol, lactitol, or a combination
thereof. In some embodiments, the sugar alcohol is isomalt.
In certain embodiments, the composition is in the form of a compressed or
molded pellet.
Example pellet weights range from about 250 mg to about 1500 mg, such as about
250 mg to about 700
mg, or from about 700 mg to about 1500 mg. The pellet can have any of a
variety of shapes, including
traditional pill or tablet shapes. Generally, the composition in tablet form
comprises a glucose-
polysaccharide blend and a sugar alcohol. In some embodiments, the glucose-
polysaccharide blend is
present in an amount of from about 35 to about 50% by weight, based on the
total weight of the
composition; and the sugar alcohol is present in an amount of from about 30 to
about 45% by weight,
based on the total weight of the composition. In some embodiments, the sugar
alcohol is isomalt,
erythritol, sorbitol, arabitol, ribitol, maltitol, dulcitol, iditol. mannitol,
xylitol, lactitol, or a combination
thereof. In some embodiments, the sugar alcohol is isomalt.
Preparation of the composition
The manner by which the various components of the composition (e.g., filler,
active ingredient,
and the like) are combined may vary. As such, the overall composition with
e.g., powdered composition
components may be relatively uniform in nature (e.g., homogenous). The
components noted above,
which may be in liquid or dry solid form, can be admixed in a pretreatment
step prior to mixture with any
remaining components of the composition, or simply mixed together with all
other liquid or dry
ingredients. The compositions of the disclosure are prepared, for example, by
dry-blending dry
ingredients, such as filler, sweeteners, salts, and the like. In certain
embodiments, water can be added to
the dry blend at this stage. Additionally, it is optional to add, such as by
spraying, active ingredients
and/or flavoring agents to the dry blend, followed by mixing.
The various components of the composition may be contacted, combined, or mixed
together
using any mixing technique or equipment known in the art. Any mixing method
that brings the
composition ingredients into intimate contact can be used, such as a mixing
apparatus featuring an
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impeller or other structure capable of agitation. Examples of mixing equipment
include casing drums,
conditioning cylinders or drums, liquid spray apparatus, conical-type
blenders, ribbon blenders, mixers
available as FKM130, FKM600, FKM1200, FKM2000 and FKM3000 from Littleford Day,
Inc., Plough
Share types of mixer cylinders, Hobart mixers; and the like. See also, for
example, the types of
methodologies set forth in US Pat. Nos. 4,148,325 to Solomon et al.; 6,510,855
to Korte et al.; and
6,834,654 to Williams, each of which is incorporated herein by reference. In
some embodiments, the
components forining the composition are prepared such that the mixture thereof
may be used in a starch
molding process for forming the composition. Manners and methods for
formulating compositions will
be apparent to those skilled in the art. See, for example, the types of
methodologies set forth in US Pat.
No. 4,148,325 to Solomon et al.; US Pat. No. 6,510,855 to Korte et al.; and US
Pat. No. 6,834,654 to
Williams, US Pat. Nos. 4,725,440 to Ridgway et al., and 6,077,524 to Bolder et
al., each of which is
incorporated herein by reference.
In some embodiments, the composition is in the form of a compressed pellet or
tablet. In one
embodiment, the process for making the pellet or tablet involves first mixing
the bulk filler (e.g.,
EMDEX) and the active ingredients. The remaining composition ingredients
(e.g., sugar alcohol and any
other desired components, such as binders, colorants, sweeteners, flavors, and
the like) are then added.
Optionally, a colorant can may be added to one of the composition components
in a separate step prior to
mixing with the remaining components of the composition. The mixing of the
composition can be
accomplished using any mixing device. The final composition is then compressed
into pellet or tablet
form using conventional tableting techniques and optionally coated. Compressed
composition pellets can
be produced by compacting the composition, including any associated
formulation components, in the
form of a pellet, and optionally coating each pellet with an overcoat
material. Example compaction
devices, such as compaction presses, are available as Colton 2216 and Colton
2247 from Vector
Corporation and as 1200i, 2200i, 3200, 2090, 3090 and 4090 from Fette
Compacting. Devices for
providing outer coating layers to compacted pelletized compositions are
available as CompuLab 24,
CompuLab 36, Accela-Cota 48 and Accela-Cota 60 from Thomas Engineering. When
present, a coating
typically comprises a film-forming polymer, such as a cellulosic polymer, an
optional plasticizer, and
optional flavorants, colorants, salts, sweeteners or other additives of the
types set forth herein. The
coating compositions are usually aqueous in nature and can be applied using
any pellet or tablet coating
technique known in the art, such as pan coating. Example film-forming polymers
include cellulosic
polymers such as methylcellulose, hydroxypropyl cellulose (HPC), hydroxypropyl
methylcellulose
(HPMC), hydroxyethyl cellulose, and carboxy methylcellulose. Example
plasticizers include aqueous
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solutions or emulsions of glyceryl monostearate and triethyl citrate.
Additional potential coatings include
food grade shellac, waxes such as carnuaba wax, and combinations thereof.
In some embodiments, the composition is in chewable form. For the preparation
of the
composition in chewable form, generally, pectin binder is pre-blended with a
portion of the isomalt.
Water is added, and the mixture heated to boiling with stirring. Maltitol
syrup and any remaining isomalt
are added to the boiling mixture, along with the active ingredients (e.g.,
caffeine, taurine, and vitamin C),
followed by trisodium citrate. The mixture is cooked to 78 brix. Heat is
removed, and sweetener (e.g.,
sucralose and acesulfame K) and flavorant added, along with the colorant and
citric acid solution (or
dicalcium phosphate), and the mixture thoroughly combined. The composition is
deposited into starch
molds for storage at ambient temperature.
In some embodiments, the composition is in meltable form. For preparation of
meltable
compositions, the lipid is typically heated to slightly above the melting
temperature such that the lipid is
liquefied. Optionally, active ingredients, flavoring agents, and/or lecithin
can be added to the liquefied
lipid at this stage. Thereafter, all or a portion of the liquefied lipid can
be blended with the dry blend and
mixed until the composition reaches the desired level of homogeneity or until
the desired textural
properties are achieved. The mixture is milled (e.g., in a dry roll mill)
until the particle size is less than
about 20 microns. The milled isomalt-palm oil is combined with any remaining
lipid, and the dry
ingredients and flavor mixed in. The base is generally warmed to a fluid
consistency. The composition
can be divided into discrete portions, such as by pouring the composition into
a sheet-like structure,
cooling, and then cutting the structure into individual portions, or by
depositing the composition into
molds and allowing to cool.
Many modifications and other embodiments of the invention will come to mind to
one skilled in
the art to which this invention pertains having the benefit of the teachings
presented in the foregoing
description. Therefore, it is to be understood that the invention is not to be
limited to the specific
embodiments disclosed and that modifications and other embodiments are
intended to be included within
the scope of the appended claims. Although specific terms are employed herein,
they are used in a
generic and descriptive sense only and not for purposes of limitation.
EXAMPLES
Aspects of the present invention are more fully illustrated by the following
examples, which are
set forth to illustrate certain aspects of the present invention and are not
to be construed as limiting
thereof.
Example 1. Tablet comprising theanine, GABA, and lemon balm.
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A composition according to an embodiment of the present disclosure in tablet
form was prepared
from a composition containing a mixture of fillers, a mixture of theanine,
GABA (gamma-aminobutyric
acid), and lemon balm as the active ingredient, and additional components as
disclosed herein (salt,
sweeteners, processing aid). The fillers, sweetener, salt, active ingredients,
and processing aid were
combined and mixed thoroughly. The mixture was compressed and tableted using a
Fette 1200i tablet
press. The tablets were coated with wax and shellac. The ingredients of the
composition and their
concentrations in the composition in weight % are provided in Table 1. The
tablets each weighed 1000
mg.
Table 1. Tablet ingredients
Ingredient %w/w
isom alt 32-48
Emdex* 35-55
theanine 3-5
GABA 4-6
lemon balm extract 3-4
sweetener 0.1-0.5
salt 0.2-0.4
sodium stearyl fumarate 0.5-1.5
flavorant 1-1.5
Carnauba wax 0.05-0.15
shellac 0.2-0.4
Example 2. Tablet comprising caffeine, taurine, and vitamin C.
A composition according to an embodiment of the present disclosure in tablet
form was prepared
from a composition containing a mixture of fillers, a mixture of caffeine,
taurine, and vitamin C as the
active ingredient, and additional components as disclosed herein (salt,
sweeteners, buffer, processing aid)
using the method of Example 1. The ingredients of the composition and their
concentrations in the
composition in weight % are provided in Table 2. The tablets each weighed 1000
mg.
Table 2. Tablet ingredients
Ingredient %w/w
i so m alt 30-40
Emdexl) 35-55
sweetener 0.1-0.5
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caffeine 3-5
taurine 4-6
vitamin C 4-6
trisodium citrate 2-3
salt 0.1-0.5
colorant 1-2
flavorant 1-1.5
sodium stearyl fumarate 0.5-1.5
Carnauba wax 0.05-0.15
shellac 0.2-0.4
Example 3. Tablet comprising caffeine, theanine, sunflower lecithin, and
ginseng.
A composition according to an embodiment of the present disclosure in tablet
form was prepared
from a composition containing a mixture of fillers, a mixture of caffeine,
theaninc, sunflower lecithin, and
ginseng as the active ingredient, and additional components as disclosed
herein (salt, sweeteners, buffer,
processing aid) using the method of Example 1 . The ingredients of the
composition and their
concentrations in the composition in weight % are provided in Table 3. The
tablets each weighed 1000
mg.
Table 3. Tablet ingredients
Ingredient %w/vv
isomalt 32-48
Emdex4) 35-55
sweetener 0.1-0.5
caffeine 3-5
theanine 3-5
sunflower lecithin 0.5-1.5
ginseng extract 0.4-0.6
trisodium citrate 2-3
salt 0.1-0.5
colorant 1-2
flavorant 1-1.5
sodium stearyl fumarate 0.5-1.5
Carnauba wax 0.05-0.15
shellac 0.2-0.4
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Example 4. Chewable comprising caffeine, tontine, and vitamin C.
A composition according to an embodiment of the present disclosure in chewable
form was
prepared from a composition containing a mixture of fillers, a mixture of
caffeine, taurine, and vitamin C
as the active ingredient, and additional components as disclosed herein (salt,
sweeteners, flavoring agent,
water, binder, citric acid, gelation agent). The ingredients of the
composition and their concentrations in
the composition in weight% are provided in Table 4.
The pectin binder was pre-blended with a portion of the isomalt. Water was
added, and the
mixture heated to boiling with stirring. Maltitol syn.tp and any remaining
isomalt were added to the
boiling mixture, along with the active ingredients (e.g., caffeine, taurine,
and vitamin C), followed by
trisodium citrate. The mixture was cooked to 78 brix. Heat was removed, and
sweetener (e.g., sucralose
and acesulfame K, colorant and flavorant were added, along with the citric
acid and dicalcium phosphate,
and the mixture thoroughly combined, and the composition deposited into starch
molds for storage at
ambient temperature. The chews each weighed 2600 mg.
Table 4. Chewable ingredients
Ingredient %w/w
isomalt 12-20
maltitol syrup 48-72
caffeine 1-2
taurine 1.5-2.5
vitamin C 1.5-2.5
water 12-18
dicalcium phosphate 0.4-0.6
citric acid 0.5-1.5
trisodium citrate 0.5-1.5
flavorant 0.6-0.9
pectin 1-2
sweetener 0.05-0.5
colorant 0.05-0.15
Example 5. Chewable comprising theanine, GABA, and lemon balm.
A composition according to an embodiment of the present disclosure in chewable
form was
prepared from a composition containing a mixture of fillers, a mixture of
theanine, GABA, and lemon
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balm as the active ingredient, and additional components as disclosed herein
(salt, sweeteners, flavoring
agent, water, binder, citric acid, gelation agent) using the method of Example
4. The ingredients of the
composition and their concentrations in the composition in weight % are
provided in Table 5. The chews
each weighed 2600 mg.
Table 5. Chewable ingredients
Ingredient %w/w
isomalt 12-20
maltitol syrup 48-72
theanine 1.2-1.8
GABA 1.5-2.5
lemon balm extract 0.5-1.5
water 12-20
citric acid 0.5-1.5
dicalcium phosphate 0.4-0.6
pectin 2-3
sweetener 0.05-0.5
flavor 0.5-0.7
Example 6. Chewable comprising caffeine, theanine, and ginseng.
A composition according to an embodiment of the present disclosure in chewable
form was
prepared from a composition containing a mixture of fillers, a mixture of
caffeine, theanine, and ginseng
as the active ingredient, and additional components as disclosed herein (salt,
sweeteners, flavoring agent,
water, binder, citric acid, gelation agent) using the method of Example 4. The
ingredients of the
composition and their concentrations in the composition in weight % are
provided in Table 6. The chews
each weighed 2600 mg.
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Table 6. Chewable ingredients
Ingredient %w/w
isomalt 12-20
maltitol syrup 48-72
caffeine 1.2-1.8
thcaninc 1.2-1.8
Ginseng extract 0.1-0.3
water 12-18
citric acid 0.4-0.6
pectin 1.2-1.8
sunflower lecithin 0.3-0.5
sweetener 0.05-0.5
colorant 0.05-0.15
flavor 0.5-1.5
Trisodium citrate 0.8-1.2
Dicalcium phosphate 0.2-0.4
Example 7. Meltable comprising theanine, GABA, and lemon balm.
A composition according to an embodiment of the present disclosure in meltable
form was
prepared from a composition containing a filler, a lipid, a mixture of
theanine, GABA, and lemon balm as
the active ingredient, and additional components as disclosed herein (salt,
sweeteners, flavoring agent).
The ingredients of the composition and their concentrations in the composition
in weight % are provided
in Table 7.
A portion of the palm oil was melted and mixed with the isomalt in a mixer.
The mixture was
transferred to a dry roll mill and milled until the particle size was less
than 20 microns. In a mixer, the
milled isomalt-palm oil was combined with the remaining portion of palm oil.
The base was warmed to a
fluid consistency. Sunflower oil, the dry ingredients, and flavor were mixed
in. The isomalt-palm oil-
ingredient mixture was transferred to a heated depositing funnel. The
appropriate weight of the samples
was deposited into a shape mold. If needed, the mold was placed on a vibrator
to ensure even filling. The
product was allowed to cool and solidify, then removed from the mold. The
melts each weighed 1300 mg.
Table 7. Meltable ingredients
Ingredient %w/w
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isomalt 35-55
Lipid (e.g., palm oil) 32-48
theanine 2.5-3.5
GABA 3.5-4.5
lemon balm extract 1.5-2.5
salt 0.5-1.5
sunflower lecithin 0.25-0.5
Sunflower oil 2-3.5
sweetener 0.05-0.5
flavor 0.5-1.5
Example 8. Meltable comprising theanine, caffeine, and ginseng.
A composition according to an embodiment of the present disclosure in meltable
form was
prepared from a composition containing a filler, a lipid, a mixture of
theanine, caffeine, and ginseng as
the active ingredient, and additional components as disclosed herein (salt,
sweeteners, flavoring agent,
buffer) using the method of Example 7. The ingredients of the composition and
their concentrations in the
composition in weight % are provided in Table 8. The melts each weighed 1300
mg.
Table 8. Meltable ingredients
Ingredient %w/w
isomalt 35-55
lipid (e.g., palm oil) 35-50
caffeine 3-4
theanine 2.5-3.5
Ginseng extract 0.3-0.5
sunflower lecithin 0.5-1
Sunflower oil 2-4
colorant 0.4-0.6
trisodium citrate 1-2.5
salt 0.5-1.5
flavor 0.5-1.5
sweetener 0.05-0.5
Example 9. Meltable comprising taurine, caffeine, and vitamin C.
A composition according to an embodiment of the present disclosure in meltable
form was
prepared from a composition containing a filler, a lipid, a mixture of
taurine, caffeine, and vitamin C as
the active ingredient, and additional components as disclosed herein (salt,
sweeteners, flavoring agent,
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buffer, emulsifier) using the method of Example 7. The ingredients of the
composition and their
concentrations in the composition in weight % are provided in Table 9. The
melts each weighed 1300 mg.
Table 9. Meltable ingredients
Ingredient %w/w
isomalt 35-55
lipid (e.g., palm oil) 35-50
taurine 3.5-4.5
caffeine 2.5-3.5
trisodium citrate 1-2.5
vitamin C 3.5-4.5
salt 0.5-1.5
sweetener 0.05-0.5
sunflower lecithin 0.3-0.5
flavor 0.5-1.5
Sunflower oil 25-3.5
colorant 0.4-0.6
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