Note: Descriptions are shown in the official language in which they were submitted.
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ORAL CARE COMPOSITION
BACKGROUND
[0001] Gum bleeding is associated with many common oral conditions, such as
gingivitis. Gum
bleeding may be caused by a buildup of plaque, a soft, sticky, colorless film
of bacteria that
forms on the teeth and gums, and produces toxins that may inflame or infect
the gum tissue to
cause gingivitis. Gingivitis is the initial stage of gum disease and, if left
untreated, may cause
periodontitis.
[0002] Among other uses, antibacterial agents have been used in oral care
products to reduce
plaque and gingivitis, and hence reduce gum bleeding. However, the
antibacterial efficacy of
compounds may be affected by other active ingredients in the oral care
product, or by limits on
the amounts of an antibacterial agent that can be used.
[0003] Accordingly, it would be useful to develop oral care compositions, such
as toothpastes
and mouthwashes, configured to provide improved antibacterial efficacy.
Additionally, it would
be useful to develop oral care composition with natural or botanically-based
active ingredients.
BRIEF SUMMARY
[0004] This summary is intended merely to introduce a simplified summary of
some aspects of
one or more embodiments of the present disclosure. Further areas of
applicability of the present
invention will become apparent from the detailed description provided
hereinafter. This summary
is not an extensive overview, nor is it intended to identify key or critical
elements of the present
teachings, nor to delineate the scope of the disclosure. Rather, its purpose
is merely to present one
or more concepts in simplified form as a prelude to the detailed description
below.
[0005] The foregoing and/or other aspects and utilities embodied in the
present disclosure may be
achieved by providing an oral care composition, including from 0.04 weight %
to 2.80 weight %
of a mixture of antibacterial agents, based on a total weight of the oral care
composition, wherein
the mixture of antibacterial agents includes oleanic acid and eugenol at a 2:1
to 3:1 weight ratio.
[0006] Eugenol may include one or more of eugenol, methyl eugenol, iso-
eugenol, or mixtures
thereof.
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[0007] The oral care composition may include from 0.10 weight % to 1.0 weight
% of the mixture
of antibacterial agents.
[0008] The mixture of antibacterial agents may include oleanic acid and
eugenol at a 2:1 weight
ratio.
[0009] The mixture of antibacterial agents may consist essentially of oleanic
acid and eugenol at
a2:1 weight ratio.
[0010] The oral care composition may include from 0.02 weight % to 2.0 weight
% of oleanic
acid, based on the total weight of the oral care composition; and from 0.01
weight % to 1.0 weight
% of eugenol, based on the total weight of the oral care composition.
[0011] The oral care composition may include from 0.05 weight % to 0.50 weight
% of oleanic
acid; and from 0.025 weight % to 0.25 weight % of eugenol.
[0012] The oral care composition may include 0.10 weight % of oleanic acid;
and 0.05 weight %
of eugenol.
[0013] Other than the mixture of antibacterial agents, the oral care
composition may lack another
antibacterial agent.
[0014] The foregoing and/or other aspects and utilities embodied in the
present disclosure may
also be achieved by providing a method for increasing the antibacterial effect
of an oral care
composition, including adding a mixture of antibacterial agents to the oral
care composition,
wherein the mixture of antibacterial agents includes oleanic acid and eugenol
at a 2:1 to 3:1 weight
ratio.
[0015] Eugenol may include one or more of eugenol, methyl eugenol, iso-
eugenol, or mixtures
thereof.
[0016] The mixture of antibacterial agents may include oleanic acid and
eugenol at a 2:1 weight
ratio.
[0017] The mixture of antibacterial agents may consist essentially of oleanic
acid and eugenol at
a2:1 weight ratio.
[0018] Other than the mixture of antibacterial agents, the oral care
composition may lack another
antibacterial agent.
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DETAILED DESCRIPTION
[0019] Reference will now be made in detail to the various embodiments in the
present disclosure.
The embodiments are described below to provide a more complete understanding
of the
components, processes, compositions, and apparatuses disclosed herein. Any
examples given are
intended to be illustrative, and not restrictive. However, it will be apparent
to one of ordinary skill
in the art that the invention may be practiced without these specific details.
In other instances,
well-known methods, procedures, and components have not been described in
detail so as not to
unnecessarily obscure aspects of the embodiments.
[0020] Throughout the specification and claims, the following terms take the
meanings explicitly
associated herein, unless the context clearly dictates otherwise. Phrases such
as "in an
embodiment," "in certain embodiments," and "in some embodiments" as used
herein do not
necessarily refer to the same embodiment(s), though they may. Furthermore, the
phrases "in
another embodiment" and "in some other embodiments" as used herein do not
necessarily refer to
a different embodiment, although they may. As described below, various
embodiments may be
readily combined, without departing from the scope or spirit of the present
disclosure.
[0021] As used herein, the term "or" is an inclusive operator, and is
equivalent to the term
"and/or," unless the context clearly dictates otherwise. The term "based on"
is not exclusive and
allows for being based on additional factors not described, unless the context
clearly dictates
otherwise. In the specification, the recitation of "at least one of A, B, and
C," includes
embodiments containing A, B, or C, multiple examples of A, B, or C, or
combinations of A/B,
A/C, B/C, A/B/B/ B/B/C, A/B/C, etc. In addition, throughout the specification,
the meaning of
"a," "an," and "the" include plural references. The meaning of "in" includes
"in" and "on."
[0022] It will also be understood that, although the terms first, second, etc.
may be used herein to
describe various elements, these elements should not be limited by these
terms. These terms are
only used to distinguish one element from another. For example, a first
object, component, or step
could be termed a second object, component, or step, and, similarly, a second
object, component,
or step could be termed a first object, component, or step, without departing
from the scope of the
invention. The first object, component, or step, and the second object,
component, or step, are
both, objects, components, or steps, respectively, but they are not to be
considered the same object,
component, or step. It will be further understood that the terms "includes,"
"including,"
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"comprises" and/or "comprising," when used in this specification, specify the
presence of stated
features, steps, operations, elements, and/or components, but do not preclude
the presence or
addition of one or more other features, steps, operations, elements,
components, and/or groups
thereof. Further, as used herein, the term "if" may be construed to mean
"when" or "upon" or "in
response to determining" or "in response to detecting," depending on the
context.
[0023] All physical properties that are defined hereinafter are measured at 20
to 25 Celsius
unless otherwise specified.
[0024] When referring to any numerical range of values herein, such ranges are
understood to
include each and every number and/or fraction between the stated range minimum
and maximum,
as well as the endpoints. For example, a range of 0.5-6% would expressly
include all intermediate
values of, for example, 0.6%, 0.7%, and 0.9%, all the way up to and including
5.95%, 5.97%, and
5.99%, among many others. The same applies to each other numerical property
and/or elemental
range set forth herein, unless the context clearly dictates otherwise.
[0025] Additionally, all numerical values are "about" or "approximately" the
indicated value, and
take into account experimental error and variations that would be expected by
a person having
ordinary skill in the art. It should be appreciated that all numerical values
and ranges disclosed
herein are approximate values and ranges, whether "about" is used in
conjunction therewith.
[0026] Unless otherwise specified, all percentages and amounts expressed
herein and elsewhere
in the specification should be understood to refer to percentages by weight.
The amounts given
are based on the active weight of the material.
[0027] With regard to procedures, methods, techniques, and workflows that are
in accordance with
some embodiments, some operations in the procedures, methods, techniques, and
workflows
disclosed herein may be combined and/or the order of some operations may be
changed.
[0028] The inventors have surprisingly discovered a new, synergistic, mixture
of antibacterial
agents that lead to improve antibacterial efficacy. An oral care composition
as disclosed herein
includes a mixture of antibacterial agents. The mixture of antibacterial
agents provides an
improved antibacterial effect. The mixture of antibacterial agents includes
oleanic acid and
eugenol. In particular, the mixture of antibacterial agents includes oleanic
acid and eugenol at a
2:1 to 3:1 ratio by weight. For example, the mixture of antibacterial agents
may include oleanic
acid and eugenol at a 2:1 ratio by weight.
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[0029] In some embodiments, the mixture of antibacterial agents consists
essentially of oleanic
acid and eugenol. For example, the mixture of antibacterial agents may consist
essentially of
oleanic acid and eugenol at a 2:1 to 3:1 ratio by weight. For example, the
mixture of antibacterial
agents may consist essentially of oleanic acid and eugenol at a 2:1 ratio by
weight.
[0030] In some embodiments, the mixture of antibacterial agents is derived
from or based upon
compounds or extracts isolated from plants.
[0031] Formula 1 illustrates a chemical structure of oleanic acid. Oleanic or
oleanolic acid (30-
hydroxy-olea-12-en-28-oic) is a pentacyclic triterpenoid that is widely
distributed in plants. For
example, oleanic acid may be extracted from a number of medicinal plants, such
as Calendula
officinalis L. (marigold), Ligustrum lucidum Ait (oleaceae), and Hemsleya
Chinensis Cogn.
Formula 1:
, 1
, -
...--'
,....----õ, ,---
SCOOH
"--
HO."',;(.1t ---
/ \H
[0032] Formula 2 illustrates a chemical structure of eugenol. Eugenol (4-ally1-
2-methoxyphenol),
is a naturally occurring phenol essential oil extracted from, for example,
cloves, nutmeg,
cinnamon, basil, and bay leaf. Eugenol may also be provided as methyl eugenol
or iso-eugenol.
Formula 2:
OH
:
Ts-
1,
CH2
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[0033] As described above, the inventors have surprisingly discovered that the
combination of
oleanic acid and eugenol has increased antibacterial effects. In some
embodiments, the
antibacterial effects of oleanic acid combined with eugenol are greater than
those of oleanic acid
or eugenol separately. In other embodiments, the antibacterial effects of
oleanic acid combined
with eugenol at a 2:1 ratio are greater than those of oleanic acid combined
with eugenol at other
ratios, such as 3:1 or greater.
[0034] In certain embodiments, the mixture of antibacterial agents including
oleanic acid and
eugenol is the only antibacterial agent present in the oral care composition.
In other embodiments,
the oral care composition includes no other antibacterial agents apart from
the mixture of
antibacterial agents.
[0035] In certain embodiments, the oral care composition includes from about
0.04 weight % to
about 2.8 weight % mixture of antibacterial agents, based on the total weight
of the oral care
composition. For example, the oral care composition includes from about 0.05
weight % to about
2.0 weight % mixture of antibacterial agents, from about 0.1 weight % to about
1 weight % mixture
of antibacterial agents, or from about 0.1 weight % to about 0.5 weight %
mixture of antibacterial
agents, based on the total weight of the oral care composition. In one
implementation, the oral
care composition includes about 0.15 weight % mixture of antibacterial agents.
[0036] As described above, the mixture of antibacterial agents includes
oleanic acid and eugenol.
Eugenol may also be provided as eugenol, methyl eugenol, iso-eugenol, or
combinations thereof.
The mixture of antibacterial agents includes oleanic acid and eugenol at a 2:1
ratio by weight. In
some embodiments, the mixture of antibacterial agents may include additional
antibacterial agents.
In other embodiments, the mixture of antibacterial agents only includes
oleanic acid and eugenol.
[0037] For example, the oral care composition may include from about 0.02
weight % to about
2.0 weight %, from about 0.05 weight % to about 0.5 weight %, from about 0.1
weight % to about
0.25 weight %, or from about 0.1 weight % to about 0.2 weight % oleanic acid,
based on the total
weight of the oral care composition. In one preferred embodiment, the oral
care composition may
include 0.10 weight % oleanic acid. Correspondingly, the oral care composition
may include from
0.01 weight % to 1.0 weight % eugenol, based on the total weight of the oral
care composition.
For example, the oral care composition includes from about 0.025 weight % to
about 0.25 weight
%, from about 0.02 weight % to about 0.6 weight %, from about 0.04 weight % to
about 0.2
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weight %, or from about 0.05 weight % to about 0.10 weight % eugenol, based on
the total weight
of the oral care composition. In a preferred embodiment, the oral care
composition may include
0.05 weight % eugenol. In some embodiments, the oral care composition may
include methyl
eugenol and/or iso eugenol instead of or in addition to eugenol.
[0038] Generally, viscosity is an important parameter for oral care
compositions, such as
toothpastes or whitening gels. For example, when the viscosity of an oral care
composition is too
low, it may become too runny and physical phase separation may take place. In
some cases, this
will not only affect the aesthetics of the oral care composition but also the
homogeneity of the
ingredients in the oral care composition. On the other hand, if the viscosity
of the oral care
compositions is too high, the oral care composition will be difficult to
manufacture and package.
In addition, oral care compositions with high viscosity are very difficult for
users to evacuate from
commonly used packages, such as tubes or syringes. Accordingly, it's important
to select
ingredients for oral care compositions that achieve a desirable range of
viscosity to ensure product
manufacturability, stability, and quality, as well as consumer acceptance.
[0039] In some embodiments, the viscosity of the oral care composition is from
about 10,000
centipoise (cPs) to about 500,000 cPs at 25 C. For example, the viscosity of
the oral care
composition is from about 50,000 cPs to about 400,000 cPs at 25 C. In one
embodiment, the
viscosity of the oral care composition is from about 125,000 cPs to about
300,000 cPs at 25 C.
[0040] In some embodiments, the oral care composition may include additional
ingredients
common to oral care compositions, such as carriers, dispersants, whitening
agents, flavoring
agents, tartar control agents, surfactants, sweeteners, humectants, colorants,
antibacterial agents,
preservatives, dyes, and pigments.
[0041] All ingredients used in the compositions described herein should be
orally acceptable.
"Orally acceptable" means an ingredient which is present in the composition as
described in an
amount and form which does not render the composition unsafe, unpalatable, or
otherwise
unsuitable for use in the oral cavity. In addition, the additional ingredients
should not substantially
inhibit the efficacy of the mixture of antibacterial agents described above.
[0042] In various embodiments of the present disclosure, the oral care
composition includes an
orally acceptable carrier. As used herein, an "orally acceptable carrier"
refers to a material or
combination of materials that are safe for use in the oral care compositions
of the present disclosure
while retaining significant efficacy for the mixture of antibacterial agents.
In certain embodiments,
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the carrier is specifically selected to ensure that there is no substantially
reduction in efficacy for
the mixture of antibacterial agents. For example, the oral care composition
may use water as the
carrier. In certain embodiments, the oral care composition includes 90 weight
% or less, 70 weight
% or less, or 50 weight % or less carrier, based on the total weight of the
oral care composition.
[0043] In certain embodiments, the oral care composition may include one or
more humectants.
In some embodiments, the humectant is a mixture of humectants, such as
glycerin and sorbitol,
and a polyhydric alcohol, such as propylene glycol, butylene glycol, hexylene
glycol, polyethylene
glycol. In certain embodiments, the oral care composition includes from 5
weight % to 40 weight
% or from 10 weight % to 30 weight % humectant, based on a total weight of the
oral care
composition.
[0044] The oral care composition may include one or more whitening agent. As
used herein, a
"whitening agent" is a material that affects whitening of a tooth surface to
which it is applied. For
example, in some embodiments, the whitening agent is an oxidizing agent. In
its broadest sense,
"oxidizing agent" is intended to include those compounds which can accept an
electron from
another molecule in the environment of the oral cavity without having a
deleterious or
unacceptably harmful effect on the oral cavity in normal and accepted use.
[0045] In some embodiments, the whitening agent may include peroxides and
hydroperoxides,
such as hydrogen peroxide, peroxides of alkali and alkaline earth metals,
organic peroxy
compounds, peroxy acids, salts thereof, and mixtures thereof. Peroxides of
alkali and alkaline
earth metals include lithium peroxide, potassium peroxide, sodium peroxide,
magnesium peroxide,
calcium peroxide, barium peroxide, and mixtures thereof. Organic peroxy
compounds include
urea peroxide, carbamide peroxide (also known as urea hydrogen peroxide),
glyceryl hydrogen
peroxide, alkyl hydrogen peroxides, dialkyl peroxides, alkyl peroxy acids,
peroxy esters, diacyl
peroxides, benzoyl peroxide, and monoperoxyphthalate, and mixtures thereof.
Peroxy acids and
their salts include organic peroxy acids such as alkyl peroxy acids, and
monoperoxyphthalate and
mixtures thereof, as well as inorganic peroxy acid salts such as percarbonate,
perphosphate,
perborate and persilicate salts of alkali and alkaline earth metals such as
lithium, potassium,
sodium, magnesium, calcium and barium, and mixtures thereof. In some
embodiments a non-
peroxide whitening agent may be provided. Whitening agents among those useful
herein include
non-peroxy compounds, such as chlorine dioxide, chlorites and hypochlorites.
Chlorites and
hypochlorites include those of alkali and alkaline earth metals such as
lithium, potassium, sodium,
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magnesium, calcium and barium. Non-peroxide whitening agents also include
colorants, such as
titanium dioxide and hydroxyapatite.
[0046] In some embodiments, the oral care composition includes from about
0.01% to about 50%
whitening agent based on a total weight of the oral care composition. For
example, the oral care
composition includes from about 0.05 weight % to about 40 weight % whitening
agent. In one
embodiment, the oral care composition includes about 0.1 weight % whitening
agent based on a
total weight of the oral care composition.
[0047] In one embodiment, the oral care composition includes one or more
surfactants. In some
embodiments, the surfactants enhance stability of the composition, help clean
the oral cavity
surfaces through detergency, and provide foam upon agitation, e.g., during
brushing with an oral
care composition of the disclosure. Surfactants or surface active agents
generally achieve
increased whitening action by thoroughly dispersing the whitening agent
throughout the oral
cavity. In various embodiments, suitable surface active agents may function as
a surface active
agent, emulsifier, and/or foam modulator.
[0048] Any orally acceptable surfactant, most of which are anionic, nonionic,
cationic, or
amphoteric, may be used. A combination of surfactants may also be used.
Suitable anionic
surfactants include without limitation water-soluble salts of C8_20 alkyl
sulfates, sulfonated
monoglycerides of C8_20 fatty acids, sarcosinates, taurates and the like.
Illustrative examples of
these and other classes include sodium lauryl sulfate, sodium cocoyl
monoglyceride sulfonate,
sodium lauryl sarcosinate, sodium lauryl isoethionate, sodium laureth
carboxylate, and sodium
dodecyl benzenesulfonate. Suitable nonionic surfactants include without
limitation poloxamers,
polyoxyethylene sorbitan esters, fatty alcohol ethoxylates, alkylphenol
ethoxylates, tertiary amine
oxides, tertiary phosphine oxides, dialkyl sulfoxides and the like. Suitable
amphoteric surfactants
include, without limitation, derivatives of C8_20 aliphatic secondary and
tertiary amines having an
anionic group such as carboxylate, sulfate, sulfonate, phosphate or
phosphonate. A suitable
example is cocoamidopropyl betaine.
[0049] In some embodiments, the oral care composition includes from about
0.01% to about
20.0% surfactant based on a total weight of the oral care composition. For
example, the oral care
composition includes from about 1.0 weight % to about 10.0 weight %
surfactant. In one
embodiment, the oral care composition includes about 2 weight % surfactant
based on a total
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weight of the oral care composition. For example, the oral care composition
may include about 2
weight % sodium lauryl sulfate.
[0050] In certain embodiments, the oral care composition may include
thickening agents or
thickeners. Any orally acceptable thickening agent may be used, including
without limitation
carbomers, also known as carboxyvinyl polymers, carrageenans, also known as
Irish moss and
more particularly carrageenan (iota-carrageenan), high molecular weight
polyethylene glycols
(such as CARBOWAXTM, available from The Dow Chemical Company), cellulosic
polymers such
as hydroxyethylcellulose, carboxymethylcellulose ("CMC") and salts thereof,
e.g., CMC sodium,
natural gums such as karaya, xanthan, gum arabic and tragacanth, colloidal
magnesium aluminum
silicate, and colloidal or fumed silica and mixtures of the same. The
thickening agent may be a
combination of one or more orally acceptable thickening agents.
[0051] In some embodiments, the oral care composition includes from about
0.01% to about 30%
thickening agent based on a total weight of the oral care composition. For
example, the oral care
composition includes from about 0.1 weight % to about 20 weight % thickening
agent. In yet
another example, the oral care composition includes from about 0.5 weight % to
about 10 weight
% thickening agent based on a total weight of the oral care composition. For
example, the oral
care composition may include about 3 weight % fumed silica.
[0052] In some embodiments, the oral care composition includes an antioxidant.
Acceptable
antioxidants include BHA, BHT, vitamin A, carotenoids, vitamin E, flavonoids,
polyphenols,
ascorbic acid, herbal antioxidants, chlorophyll, melatonin and mixtures
thereof. In some
embodiments, the oral care composition includes from about 0.001% to about 1%
antioxidants
based on a total weight of the oral care composition. In one embodiment, the
oral care composition
includes about 0.03 weight % antioxidant by weight.
[0053] In certain embodiments, the oral care composition includes one or more
flavoring agents.
Useful flavoring agents include any material or mixture of materials operable
to enhance the taste
of the oral care composition. Any orally acceptable natural or synthetic
flavoring agent may be
used, such as flavoring oils, flavoring aldehydes, esters, alcohols, similar
materials, and
combinations thereof. Flavoring agents include vanillin, sage, marjoram,
parsley oil, spearmint
oil, cinnamon oil, oil of wintergreen (methylsalicylate), peppermint oil,
clove oil, bay oil, anise
oil, eucalyptus oil, citrus oils, fruit oils and essences including those
derived from lemon, orange,
lime, grapefruit, apricot, banana, grape, apple, strawberry, cherry,
pineapple, etc., bean- and nut-
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derived flavors such as coffee, cocoa, cola, peanut, almond, etc., adsorbed
and encapsulated
flavorants, and mixtures thereof. Also encompassed within flavoring agents
herein are ingredients
that provide fragrance and/or other sensory effect in the mouth, including
cooling or warming
effects. Such ingredients include menthol, menthyl acetate, menthyl lactate,
camphor, eucalyptus
oil, eucalyptol, anethole, eugenol, cassia, oxanone, x-irisone, propenyl
guaiethol, thymol, linalool,
benzaldehyde, cinnamaldehyde,
N-ethyl-p-menthan-3 -c arboxamine, N,2,3-trimethy1-2-
isopropylbutanamide, 3-1-menthoxypropane-1,2-diol, cinnamaldehyde glycerol
acetal (CGA),
methone glycerol acetal (MGA) and mixtures thereof.
[0054] In some embodiments, the oral care composition includes from about
0.01% to about 5%
flavoring agents based on a total weight of the oral care composition. For
example, the oral care
composition includes from about 0.05 weight % to about 3 weight % flavoring
agents. In yet
another embodiment, the oral care composition includes from about 0.1 weight %
to about 3 weight
%, from about 0.2 weight % to about 2.5 weight %, or about 1.5 weight %
flavoring agents based
on a total weight of the oral care composition. For example, the oral care
composition may include
about 1.5 weight % of dental cream flavor.
[0055] In some embodiments, the oral care composition may also include one or
more sweeteners.
Sweeteners among those useful herein include orally acceptable natural or
artificial, nutritive or
non-nutritive sweeteners. Such sweeteners include dextrose, polydextrose,
sucrose, maltose,
dextrin, dried invert sugar, mannose, xylose, ribose, fructose, levulose,
galactose, corn syrup
(including high fructose corn syrup and corn syrup solids), partially
hydrolyzed starch,
hydrogenated starch hydrolysate, sorbitol, mannitol, xylitol, maltitol,
isomalt, aspartame, neotame,
saccharin and salts thereof, sucralose, dipeptide-based intense sweeteners,
cyclamates,
dihydrochalcones and mixtures thereof. Some embodiments may include one or
more sweeteners.
In some embodiments, the oral care composition includes from about 0.005% to
about 5%
sweeteners based on a total weight of the oral care composition. In other
embodiments, the oral
care composition includes from about 0.01% to about 1% sweeteners based on a
total weight of
the oral care composition. For example, the oral care composition may include
about 0.5 weight
% sodium saccharin and about 0.04 weight % sucralose.
[0056] In some embodiments, the oral care composition may include colorants.
Colorants, such
as dyes or pigments, may be food color additives presently certified under the
Food Drug &
Cosmetic Act for use in food and ingested drugs, including dyes such as FD&C
Red No. 3 (sodium
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salt of tetraiodofluorescein), Food Red 17, disodium salt of 6-hydroxy-5-{ (2-
methoxy-5-methy1-
4-sulphophenyl)azo}-2-naphthalenesulfonic acid, Food Yellow 13, sodium salt of
a mixture of the
mono and disulphonic acids of quinophtalone or 2-(2-quinoly1) indanedione,
FD&C Yellow No.
(sodium salt of 4-p-sulfophenylazo- 1-p- sulfopheny1-5-hydroxypyrazole-3
carboxylic acid),
FD&C Yellow No. 6 (sodium salt of p-sulfophenylazo-B-naphto1-6-monosulfonate),
FD&C Green
No. 3 (disodium salt of 4-1 [4-(N-ethyl-p- sulfobenzylamino)-phenyl] -(4-
hydroxy-2-
sulfoniumpheny1)-methylene } -[1-(N-ethyl-N-p-sulfobenzy1)-DELTA-3,5-cycl-
ohexadienimine] ,
FD&C Blue No. 1 (disodium salt of dibenzyldiethyl-diamino- triphenylcarbinol
trisulfonic acid
anhydrite), FD&C Blue No. 2 (sodium salt of disulfonic acid of indigotin) and
mixtures thereof in
various proportions. Typically, colorants, if included, are present in very
small quantities.
[0057] In some embodiments, the oral care composition may also include one or
more pH
modifying agents. The pH modifying agents among those useful herein include
acidifying agents
to lower pH, basifying agents to raise pH and buffering agents to control pH
within a desired range.
For example, one or more compounds selected from acidifying, basifying and
buffering agents can
be included to provide a pH of 2 to 10, or in various embodiments from about 2
to about 8, from
about 3 to about 9, from about 4 to about 8, from about 5 to about 7, from
about 6 to about 10, and
from about 7 to about 9. Any orally acceptable pH modifying agent may be used,
including
without limitation carboxylic, phosphoric and sulfonic acids, acid salts
(e.g., monosodium citrate,
disodium citrate, monosodium malate, etc.), alkali metal hydroxides such as
sodium hydroxide,
carbonates such as sodium carbonate, bicarbonates, sesquicarbonates, borates,
silicates,
phosphates (e.g., monosodium phosphate, trisodium phosphate, pyrophosphate
salts, etc.),
imidazole and mixtures thereof. One or more pH modifying agents are optionally
present in a total
amount effective to maintain the composition in an orally acceptable pH range.
In some
embodiments, the oral care composition includes from about 0.01% to about 10%
pH modifier
agents based on a total weight of the oral care composition. For example, the
oral care composition
may include about 0.9 weight % sodium acid pyrophosphate (SAPP) and about 2
weight %
tetrasodium pyrophosphate (TSPP) as a pH modifier.
[0058] The oral care composition may include one or more preservatives. In
some embodiments,
the preservatives improve an antimicrobial characteristic of the oral care
composition to improve
storage life or prevent decay.
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[0059] In certain embodiments, the one or more preservatives include at least
one of sodium
benzoate, methyl paraben, ethyl paraben, zinc citrate, zinc oxide, triclosan,
stannum salts, and
combinations thereof.
[0060] The oral care composition may include an effective amount of
preservatives. For example,
the oral care composition may include an amount of preservatives effective to
reduce a spoilage
of the oral care composition during storage or use.
[0061] However, in some implementations, other than the mixture of
antibacterial agents, the oral
care composition lacks additional antibacterial agents or preservatives.
[0062] The oral care composition of the present disclosure may also include
one or more additional
active ingredients, which are operable for the prevention or treatment of a
condition or disorder of
hard or soft tissue of the oral cavity, the prevention or treatment of a
physiological disorder or
condition, or to provide a cosmetic benefit.
[0063] Some embodiments of the present disclosure include a dental abrasive or
combination of
dental abrasive agents. As used herein, the term "abrasive" or "abrasive
agent" also includes
materials commonly referred to as "polishing agents." Any orally acceptable
abrasive may be
used, but typically, type, fineness (particle size) and amount of abrasive
should be selected so that
tooth enamel is not excessively abraded in normal use of the composition.
Suitable abrasives
include without limitation silica (in the form of silica gel, hydrated silica
or precipitated silica),
alumina, insoluble phosphates, calcium carbonate, resinous abrasives such as
urea-formaldehyde
condensation products and the like.
[0064] Among insoluble phosphates useful as abrasives are orthophosphates,
polymetaphosphates
and pyrophosphates. Illustrative examples are dicalcium orthophosphate
dihydrate, calcium
pyrophosphate, n-calcium pyrophosphate, tricalcium phosphate, calcium
polymetaphosphate and
insoluble sodium polymetaphosphate.
[0065] Average particle size of an abrasive, if present, is generally from
about 0.1 to 100 about
p.m. For example, the particle size may be from about 1 to about 80 p.m or
from about 5 to about
60 p.m. In some embodiments, one or more abrasives are present in an amount of
from about 0.01
% to about 70% by weight, based on the total weight of the oral care
composition. In other
embodiments, the oral care composition includes from about 0.1 weight % to
about 60 weight %
abrasives. In some embodiments, the abrasive is calcium pyrophosphate. In some
embodiments,
the oral care composition includes from 0.01 weight % to about 70 weight %
calcium
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pyrophosphate based on a total weight of the oral care composition. In another
embodiment, the
oral care composition includes about 20 weight % calcium pyrophosphate.
[0066] In various embodiments of the present disclosure, the oral care
composition includes an
anticalculus agent. Suitable anticalculus agents include without limitation
phosphates and
polyphosphates (for example pyrophosphates), polyaminopropanesulfonic acid
(AMPS),
hexametaphosphate salts, zinc citrate trihydrate, polypeptides, polyolefin
sulfonates, polyolefin
phosphates, diphosphonates. In some embodiments, the anticalculus agent is
present in an amount
of from about 0.01% to about 30% weight based on the total weight of the oral
care composition.
In some embodiments, the oral care composition includes a mixture of
anticalculus agents. In
some embodiments, tetrasodium pyrophosphate (TSPP) and sodium tripolyphosphate
(STPP) are
used as the anticalculus agents. In some embodiments, the anticalculus agent
includes from 0.1%
to 10 weight % TSPP, or about 2 weight % TSPP.
[0067] The oral care compositions of the present disclosure may also include a
synthetic anionic
polymeric polycarboxylate. The synthetic anionic polymeric polycarboxylate may
act as a
stabilizer for the polyphosphate anti-tartar agent and may help to block
access of painful or pain-
causing materials, such as sugars, to the tooth nerves.
[0068] In some embodiments, the oral care composition optionally includes a
source of fluoride
ions. In some embodiments, the source of fluoride ions is selected from:
fluoride,
monofluorophosphate (MFP), and fluorosilicate salts. In some embodiments, one
or more fluoride
ion-releasing compounds are optionally present in an amount providing a total
of 100 to 20,000
ppm, 200 to 5,000 ppm, or 500 to 2,500 ppm, fluoride ions. If present, in some
embodiments, the
amount of fluoride source in the oral care composition ranges from about 0.01%
to about 10% by
weight, based on the total weight of the oral care composition, typically
about 0.5% to about 1.5
weight %. For example, the oral care composition may include about 0.76 weight
% MFP.
[0069] The compositions also may include a stannous ion or a stannous ion
source to mitigate
calcium loss. Suitable stannous ion sources include without limitation
stannous fluoride, other
stannous halides such as stannous chloride dihydrate, stannous pyrophosphate,
organic stannous
carboxylate salts such as stannous formate, acetate, gluconate, lactate,
tartrate, oxalate, malonate
and citrate, stannous ethylene glyoxide and the like. In some embodiments, one
or more stannous
ion sources are included in the oral care composition. For example, the oral
care composition may
include from about 0.01% to about 10% stannous ion source by weight, based on
the total weight
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of the oral care composition. In one embodiment, the oral care composition
includes from about
0.1 weight % to about 7 weight % stannous ion source or from about 0.2 weight
% to about 5
weight % stannous ion source.
EXAMPLES
[0070] Aspects of the present disclosure may be further understood by
referring to the following
examples. The examples are illustrative, and are not intended to be limiting
embodiments thereof.
Table 1 illustrates an oral care composition according to embodiments of the
present disclosure
and three comparative examples. The compositions of Table 1 had the same
amount for all
ingredients except that Oral Care Composition Example 1 included both oleanic
acid and eugenol
at a 2:1 weight ratio, while Comparative Example A and Comparative Example B
included only
oleanic acid or eugenol, respectively. Comparative Example C included both
oleanic acid and
eugenol at a 3:1 weight ratio.
TABLE 1
Oral Care
Comparative Comparative Comparative
Ingredient Composition
Example A Example B Example C
Example 1
Oleanolic Acid 0.1 % 0.1 % 0.15 %
Eugenol 0.05 % 0.05 % 0.05 %
Humectant 31 %
Thickener 1.0 %
Abrasives 45 %
Surfactants 2.55 %
Sodium
1.1%
monofluorophosphate
Tetra sodium
1.1%
pyrophosphate
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Water, flavor,
q.s q.s q.s q.s
sweetener and minors
[0071] Table 2 illustrates an antibacterial efficacy of the oral care
compositions. The antibacterial
composition was measured under the University of Manchester (UoM) biofilm
model as follows:
dental plaque was collected from 4 healthy volunteers and pooled together as
inoculum. The
optical density (OD) of the inoculum was matched to 0.3 absorbance at 610nm.
Sterile HAP disks
were incubated under anaerobic conditions at 37 C for 24 hours with 1 ml of
sterile artificial
saliva (with 0.01% sucrose) and 1 ml of pooled saliva in a 24 well microplate.
Freshly prepared
treatment solutions were prepared for each of the composition of Table 1
comprising 1 part
composition and 2 parts sterile distilled water. The treatment solutions were
then added to the well
and allowed to contact with the HAP disks for 10 mins. The treatment solutions
were then replaced
with 2 ml of sterile PBS and allowed to contact for 1 min. The liquid phase
was then removed and
replaced by 2 ml of sterile artificial saliva. The disks were treated in
triplicates for each
composition of Table 1 for 8 days. At intervals of 2, 4, and 8 days the disks
were collected
aseptically and transferred into half strength pre-reduced thioglycollate
medium. 100 Ill of the
collected samples were plated in duplicates for each disk on Neomycin-
Vancomycin (NV) Agar,
for Total Gram negative Anaerobes. Plates were surface spread using a sterile
spreader and
incubated anaerobically @37 C for 72 hours before counting the colonies. The
pH was monitored
for the entire period of the study using the liquid phase. The UoM number
represents the log
CFU/mL of bacterial in the sample. The lower the UoM number, the lower the
bacterial
concentration and the more effective the antibacterial efficacy of the oral
care composition.
TABLE 2
Sample Oleanic Acid Eugenol UoM
Oral Care
0.1 % 0.05 % 3.75
Composition #1
Comparative
0.1 % -- 3.92
Example A
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Comparative
-- 0.05 % 3.88
Example B
Comparative
0.15 % 0.05 % 3.77
Example C
[0072] As illustrated in Table 2, the oral care composition including the
mixture of antibacterial
agents having a 2:1 ratio of oleanic acid to eugenol displayed enhanced
antibacterial efficacy when
compared to comparative compositions including oleanic acid or eugenol
separately or including
other ratios of oleanic acid to eugenol, such as 3:1 as in Comparative
Composition C.
[0073] Accordingly, as illustrated in Table 2, Oral care compositions
according to embodiments
of the present disclosure provide enhanced antibacterial effects due to the
synergistic effects of
oleanic acid and eugenol when present at a 2:1 weight ratio. In other
implementations, oleanic
acid and eugenol are present at a weight ratio between 2:1 and 3:1.
[0074] The present disclosure has been described with reference to exemplary
embodiments.
Although a few embodiments have been shown and described, it will be
appreciated by those
skilled in the art that changes may be made in these embodiments without
departing from the
principles and spirit of preceding detailed description. It is intended that
the present disclosure be
construed as including all such modifications and alterations insofar as they
come within the scope
of the appended claims or the equivalents thereof.
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