Note: Descriptions are shown in the official language in which they were submitted.
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PREPARATION FOR EXTERNAL USE ON SKIN
BACKGROUND OF THE INVENTION
Field of the Invention
[0001]
The present invention relates to a preparation for
external use on skin which is excellent in percutaneous
absorption of ascorbic acid or an ascorbic acid derivative,
and has a high humectant effect.
Description of Related Art
[0002]
It is known that ascorbic acid or an ascorbic acid
derivative exhibits various effects such as anti-inflammatory
effects, effects of ameliorating acne, whitening effects,
anti-ageing effects, antioxidation effects, effects of
stimulating cells due to acceleration of syntheses for
biological components such as collagen, effects of controlling
DNA damage or cell disorders of epidermal kerationocytes due
to UV, and is widely employed in a preparation for external
use on skin in anticipation of these effects. In order to
sufficiently exhibit these effects, a method for increasing
the percutaneous absorption amount of ascorbic acid or an
ascorbic acid derivative and for allowing it to be effectively
absorbed was needed.
[0003]
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A low molecular weight betaine represented by
trimethylglycine is widely employed as a humectant in a
preparation for external use on skin. It is known that the
low molecular weight betaine enhances percutaneous absorption
of a whitening component such as an ascorbic acid derivative.
It is also known that, in a preparation for external use on
skin containing a whitening agent, a low molecular weight
betaine, and an oil component selected from silicone oils and
plant oils, percutaneous absorption of the whitening agent is
improved thereby enhancing an effect on improving skin
pigmentation and dullness by the whitening agent, enhancing
an effect on improving rough skin and humectant function and
providing a good sensation in use as well as enhancing a
whitening effect (Patent document 1: JP-A-2001-89321).
[0004]
Diglycerol is a component employed in a preparation for
external use on skin as a humectant component. It is known
that by employing trimethylglycine and diglycerol together,
a humectant effect is sustained (Patent document 2:
JP-A-8-20520).
SUMMARY OF THE INVENTION
[0005]
The present invention has as an object to provide a
preparation for external use on skin comprising ascorbic acid
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or an ascorbic acid derivative, in which the percutaneous
absorption amount of the ascorbic acid or the ascorbic acid
derivative is increased, an effect on improving skin
pigmentation and dullness is sufficiently exhibited, and an
excellent humectant effect is exhibited.
[0006]
As a result of diligent research in order to overcome
the problems described above, the present inventors discovered
that, by employing diglycerol and a low molecular weight
betaine together in a preparation for external use on skin
comprising one or more compounds selected from ascorbic acid
and ascorbic acid derivatives, a preparation for external use
on skin in which the percutaneous absorption of the ascorbic
acid or the ascorbic acid derivative is increased, an effect
on improving skin pigmentation and dullness is sufficiently
exhibited, and an excellent humectant effect is exhibited is
provided.
[0007]
That is, the present invention relates to preparations
for external use on skin described in ( 1 ) to ( 3 ) shown in the
following.
(1) A preparation for external use on skin, comprising (A) one
or more compounds selected from ascorbic acid and ascorbic acid
derivatives; (B) diglycerol; and (C) a low molecular weight
betaine.
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( 2 ) The preparation for external use on skin described in ( 1 ) ,
wherein the low molecular weight betaine is trimethylglycine.
( 3 ) The preparation for external use on skin described in ( 1 )
or (2) , further comprising at least one component selected from
the group consisting of a whitening component, an
anti-inflammatory component, an antibacterial component, a
cell stimulating component, an astringent component, an
antioxidant component, an anti-ageing component, and a
humectant component.
DETAILED DESCRIPTION OF THE INVENTION
In the specification of the present application, "
means "% by weight" unless otherwise indicated.
[0008]
In the present invention, by employing one or more
compounds selected from ascorbic acid and ascorbic acid
derivatives together with diglycerol and a low molecular weight
betaine, the percutaneous absorption amount of the ascorbic
acid or the ascorbic acid derivative can be dramatically
increased. For this reason, a preparation for external use
on skin in which an effect of the ascorbic acid or the ascorbic
acid derivative is sufficiently exhibited, and an excellent
effect on improving skin pigmentation and dullness is exhibited
can be provided. In addition, by using the preparation for
external use on skin of the present invention, the skin can
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be protected from dryness, which is a unique property derived
from ascorbic acid or an ascorbic acid derivative, and the
moisture retention ability of the skin can be maintained and
enhanced. Accordingly, the moisture retention ability of the
skin is improved, skin pigmentation or dullness is improved,
and skin firmness and elasticity is dramatically improved.
[0009}
As the ascorbic acid or its derivative employed in the
present invention, products which are commercially available
as components of a preparation for external use on skin in the
field of medicines, quasi drugs, or cosmetics, can be employed.
In addition, the ascorbic acid or its derivative employed in
the present invention is not particularly limited as long as
it is employed as a component of a preparation for external
use on skin in the field of medicines, quasi drugs, or cosmetics,
and the compounds described above can be freely employed alone
or in combination of two or more kinds thereof.
Among the ascorbic acid and the ascorbic acid derivatives
of the present invention described above, ascorbic acid,
ascorbyl phosphoric ester derivatives, ascorbyl sulfuric
ester derivatives, ascorbyl palmitic ester derivatives,
ascorbyl ether derivatives are preferable. More specific
examples include ascorbyl monophosphoric esters, ascorbyl
diphosphoric esters, ascorbyl triphosphoric esters,
ascorbyl-2-monosulfuric ester, ascorbyl-2-disulfuric ester,
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ascorbyl-2-trisulfuric ester, ascorbyl monopalmitic esters,
ascorbyl dipalmitic esters, ascorbyl tripalmitic esters,
ascorbyl-2-glucoside, and salts thereof. In view of high
safety with respect to the skin or mucosa and high effects,
ascorbic acid, ascorbyl monophosphoric esters and salts
thereof, ascorbyl palmitate and ascorbyl-2-glucoside, are
particularly preferable.
In the present invention, any of D-, L- and DL-ascorbic
acids can be employed. In the present invention, since
percutaneous absorption of ascorbic acid or its derivative is
dramatically improved, a water-soluble ascorbic acid or a
water-soluble ascorbic acid derivative (for example, ester
derivatives or ether derivatives of ascorbic acid and the like) ,
which is generally considered difficult to be absorbed into
the skin can be also preferably employed. Specific examples
of the water-soluble ascorbic acid derivative include, as ester
derivatives, L-ascorbyl phosphoric ester derivatives such as
L-ascorbyl monophosphoric esters, L-ascorbyl diphosphoric
esters and L-ascorbyl triphosphoric esters; L-ascorbyl
sulfuric esters such as L-ascorbyl-2-sulfuric ester; and the
like, and as ether derivatives, L-ascorbyl-2-glucoside and the
like. Among these, L-ascorbic acid, L-ascorbyl phosphoric
ester derivatives, L-ascorbyl-2-sulfuric ester, and
L-ascorbyl-2-glucoside are preferable. In view of high safety
with respect to the skin or mucosa and high effects, L-ascorbic
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acid, L-ascorbyl monophosphoric esters, and
L-ascorbyl-2-glucoside, are particularly preferable.
[0010]
In addition, the ascorbic acid or its derivative may be
employed as a pharmaceutically acceptable salt. As examples
thereof, mention may be made of, for example, salts with an
organic base (for example, salts with a tertiary amine such
as a trimethylamine salt, a triethylamine salt, a
monoethanolamine salt, a triethanolamine salt and pyridine
salt, basic ammonium salts such as arginine, and the like),
salts with an inorganic base (for example, ammonium salts,
alkali metal salts such as a sodium salt and a potassium salt,
alkaline earth metal salts such as a calcium salt and a
magnesium salt, an aluminum salt, and the like) . In particular,
preferable salts are a sodium salt, and a potassium salt. As
specific examples thereof, mention may be made of sodium
ascorbate, sodium ascorbyl monophosphate, sodium ascorbyl
diphosphate, sodium ascorbyl triphosphate, sodium
ascorbyl-2-sulfate and the like.
(0011]
In the preparation for external use on skin of the present
invention, the blending amount of the ascorbic acid or its
derivative can preferably range from 0.1 to 30~ by weight with
respect to the total weight of the preparation for external
use on skin. Within the range described above, the amount can
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be appropriately selected, depending on the various desired
effects of the ascorbic acid or its derivative and depending
on use of the preparation for external use on skin. In view
of the effects of the present invention, the amount is more
preferably in the range of from 3 to 25% by weight, and is
particularly preferably in the range of from 5 to 20% by weight.
[0012]
The diglycerol employed in the preparation for external
use on skin of the present invention is a known compound, and
the blending amount of the diglycerol employed in the
preparation for external use on skin is not particularly
limited as long as the effects of the present invention can
be exhibited, and can be appropriately selected as long as the
effects of the present invention can be exhibited. The amount
may commonly range from 1 to 95~ by weight with respect to the
total weight of the preparation for external use on skin, may
preferably range from 1 to 50~ by weight, may more preferably
range from 1 to 20% by weight, and may particularly preferably
range from 1 to 10% by weight.
[0013]
The low molecular weight betaine employed in the
preparation for external use on skin of the present invention
means one having a molecular weight of 200 or less, and forming
an amphoteric ion in the molecule. Specific examples thereof
include a quaternary ammonium base, a quaternary phosphonium
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base, a tertiary sulfonium base, and the like. They exhibit
little surfactant activity. Among these, an
N,N,N-trialkylamino acid represented by formula (1) shown
below is preferable.
[0014]
R~
--N+ c ~ coo-
z
~ n
Formula 1
( )
wherein R1, R2, and R3 independently represent an alkyl
group having 1 to 6 carbon atoms; and n represents 1 to 6.
[0015]
As R1 to R3, a straight or branched chain alkyl group
having 1 to 6 carbon atoms can be widely employed. That is,
as examples thereof, mention may be made of, a methyl group,
an ethyl group, a propyl group, an isopropyl group, a butyl
group, an isobutyl group a sec-butyl group, tert-butyl group,
a pentyl group, an isopentyl group, a neopentyl group, a
test-pentyl group, a hexyl group, an isohexyl group, a
3-methylpentyl group, 2,2-dimethylbutyl group, a
2, 3-dimethylbutyl group, and the like. R1 to R3 may be the same
or different.
In particular, in the case of n = 1, examples thereof
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include trimethylglycine, triethylglycine, tripropylglycine,
and triisopropylglycine; in the case of n = 2, examples thereof
include trimethyl-beta-alanine; and in the case of n - 3,
examples thereof include trimethyl-gamma-aminobutyric acid,
and the like. Trimethylglycine is preferable.
In addition, the low molecular weight betaines described
above may have substituents. In particular, in the case of
n - l, as examples thereof, mention may be made of
N,N,N-trimethylalanine, N,N,N-triethylalanine,
N,N,N-triisopropylalanine, N,N,N-trimethylmethylalanine,
carnitine, acetyl carnitine, and the like. Carnitine is
preferable.
[0016]
In the preparation for external use on skin of the present
invention, the blending amount of the low molecular weight
betaine preferably ranges from 0. 5 to 10% by weight with respect
to the total weight of the preparation for external use on skin.
Within the range described above, the amount can be
appropriately selected depending on various desired effects
of ascorbic acid or depending on use of the preparations for
external use on skin. In view of the effects of the present
invention, the amount is preferably in the range of from 0.5
to 9% by weight, and is particularly preferably in the range
of from 1 to 8% by weight. If the amount is below 0. l~ by weight,
the effects cannot be exhibited in some cases. On the other
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hand, if the amount exceeds 10~ by weight, a poor sensation
in use may be provided in some cases.
[0017]
In the preparation for external use on skin of the present
invention, in addition to the ascorbic acid or its derivative
described above, various components such as a whitening
component, an anti-inflammatory component, an antibacterial
component, a cell stimulating component, an astringent
component, an antioxidant component, a component for
ameliorating acne, an anti-ageing component, a component for
accelerating syntheses for biological ingredients such as
collagen, a blood circulation accelerator component and a
humectant component can be blended alone or in combination of
two or more kinds thereof in order to further add other useful
effects to the preparation for external use on skin.
Preferably, components are one or more kinds of the whitening
component, the anti-inflammatory component, the antibacterial
component, the cell stimulating component, the astringent
component, the antioxidant component, the anti-ageing
component, and the humectant component. The components
described above are not particularly limited as long as they
are conventionally employed or will be employed in the future
as the components of preparations for external use on skin in
the field of medicines, quasi drugs, or cosmetics. As the
components described above, any components can be
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appropriately selected and be employed.
[0018)
For example, as examples of whitening components,
mention may be made of arbutin; ellagic acid; phytic acid;
rucinol; chamomile ET; vitamins such as vitamin A or
derivatives thereof, vitamin E or derivatives thereof,
pantothenic acid or derivatives thereof, and the like; and the
like. Among these, as preferable examples thereof, mention
may be made of pantothenic acid or derivatives thereof, ellagic
acid, phytic acid, vitamin A or derivatives thereof, and
vitamin E or derivatives thereof. The whitening components
described above can be employed alone or in combination of two
or more kinds thereof.
[0019)
Plant components exhibiting whitening effects may be
employed as whitening components. As examples of the plant
components described above, mention may be made of components
derived from plants such as iris, almond, aloe, gingko, oolong
tea, rose hips, Scutellaria baicalensis, Coptis japonica,
Hypericum erectum, dead nettle, seaweed, Pueraria Iobata, cape
jasmine, Sophora flavescens, chlorella, Schlechtendaria
chinensis, wheat, rice, rice germ, oryzanol, rice bran, Asarum
sieboldii, Zanthoxyli fructus, perilla, Paeoniae radix,
Cnidium officinale, Morus australis, soybean, fermented
soybean, tea, Angelica sinensis, Calendula officinalis,
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garlic, Hamamelis virginiana, safflower, Paeonia suffruticosa,
Coix lacryma-jobi, Angelica sinensis [sic] , Salvia leucantha,
Uncaria gambir, asebiwarabi [phonetic spelling] , Podocarpus
macrophyllus, Flammulina velutipes, Diospyros kaki, Catalpa
ovata, black bean, Gentiana amarella, Scrophularia
buergeriana, Smilax medoca, snap bean, shokuma [phonetic
spellingp , Paris polyphylla, sage, Peuceadanum praeruptorum,
Japanese radish, Ericaceae, Lespedeza homoloba, toshin
(phonetic spelling], Picrasma quassioides, parsley, holly,
hop, Lespedeza cyrtobotrya, clove, Glycyrrhiza glabra, and the
like. Preferable are plant components derived from iris, aloe,
gingko, oolong tea, rose hips, Scutellaria baicalensis, Coptis
japonica, Hypericum erectum, dead nettle, seaweed, Pueraria
lobata, cape jasmine, Sophora flavescens, Schlechtendaria
chinensis, wheat, rice, rice bran, Asarum sieboldii,
Zanthoxyli fructus, perilla, Paeoniae radix, Cnidium
officinale, Morus australis, tea, Angelica sinensis,
Calendula officinalis, Hamamelis virginiana, safflower,
Paeonia suffruticosa, Coix lacryma-jobi, Salvia leucantha,
Uncaria gambir, Flammulina velutipes, Diospyros kaki, Catalpa
ovata, black bean, Gentiana amarella, Smilaxmedoca, snap bean,
Paris polyphylla, sage, Peuceadanum praeruptorum, Japanese
radish, Ericaceae, Lespedeza homoloba, toshin [phonetic
spelling], Picrasma quassioides, parsley, holly, hop, clove,
Glycyrrhiza glabra, and Angelica sinensis [sic]. More
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preferable are plant components derived from iris, aloe, gingko,
rose hips, Scutellaria baicalensis, Coptis japonica,
Hypericum erectum, cape jasmine, Sophora flavescens, rice,
rice bran, Asarum sieboldii, Paeoniae radix, Cnidium
officinale, Morus australis, tea, Angelica sinensis,
Calendula officinalis, Hamamelis virginiana, safflower,
Paeonia suffruticosa, Salvia leucantha, Uncaria gambir,
Flammulina velutipes, Diospyros kaki, sage, Japanese radish,
Ericaceae, parsley, hop, Glycyrrhiza glabra, and Coix
lacryma-jobi. In the case of employing the plant components
described above in the preparation for external use on skin
of the present invention, the form of the plant components is
not particularly limited. In general, the form such as a plant
extract, an essential oil, or the like, can be employed.
[0020]
Asexamplesof anti-inflammatory components, mention may
be made of allantoin, calamine, glycyrrhizic acid or
derivatives thereof, glycyrrhetic acid or derivatives thereof,
zinc oxide, guaiazulene, tocopherol acetate, pyridoxine
hydrochloride, menthol, camphor, turpentine oil, indomethacin,
salicylic acid or derivatives thereof, and the like.
Preferable are allantoin, glycyrrhizic acid or derivatives
thereof, glycyrrhetic acid or derivatives thereof,
guaiazulene, and menthol.
[0021]
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As examples of antibacterial components, mention may be
made of chlorhexidine, salicylic acid, benzalkonium chloride,
acrinol, ethanol, benzethonium chloride, cresol, gluconic
acid and derivatives thereof, povidone iodine, potassium
iodide, iodine, isopropyl methylphenol, triclocarban,
triclosan, sensitizing dye No. 101, sensitizing dye 201,
paraben, phenoxyethanol, 1,2-pentane diol,
alkyldiaminoglycine hydrochloride, and the like. As
preferable examples thereof, mention may be made of
benzalkonium chloride, benzethonium chloride, gluconic acid
and derivatives thereof, isopropyl methylphenol, triclocarban,
triclosan, sensitizing dye No. 101, sensitizing dye No. 201,
paraben, phenoxyethanol, 1,2-pentane diol,
alkyldiaminoglycine hydrochloride, and the like. More
preferable are benzalkonium chloride, gluconic acid and
derivatives thereof, benzethonium chloride, and isopropyl
methylphenol.
[0022]
As examples of cell stimulating components, mention may
be made of amino acids such as y-aminobutyric acid,
e-aminopuronic acid, and the like: vitamins such as retinol,
thiamine, riboflavin, pyridoxine hydrochloride, pantothenic
acid, and the like; alpha-hydroxylic acids such as glycolic
acid, lactic acid, and the like; tannin, flavonoid, saponin,
allatoin, sensitizing dye No. 301, and the like. Preferable
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are amino acids such as Y-aminobutyric acid, e-aminopuronic
acid, and the like; and vitamins such as retinol, thiamine,
riboflavin, pyridoxine hydrochloride, pantothenic acid, and
the like.
[0023]
As examples of astringent components, mention may be made
of metal salts such as alum, chlorohydroxyaluminum, aluminum
chloride, allantoin aluminum salt, zinc sulfate, aluminum
potassium sulfate, and the like; and organic acids such as
tannic acid, citric acid, lactic acid, succinic acid, and the
like. Preferable are alum, chlorohydroxyaluminum, aluminum
chloride, allantoin aluminum salt, aluminum potassium sulfate,
and tannic acid.
[0024]
As examples of antioxidant components, mention may be
made of tocopherol and derivatives thereof,
butylhydroxyanisole, dibutylhydroxytoluene, sodium hydrogen
sulfite, erythorbic acid and salts thereof, flavonoid,
glutathione, glutathione peroxidase,
glutathione-S-transferase, catalase, superoxide dismutase,
thioredoxin, taurine, thiotaurine, hypotaurine, and the like.
Preferable are tocopherol and derivatives thereof,
thiotaurine, hypotaurine, thioredoxin, and flavonoid.
[0025]
As examples of anti-ageing components, mention may be
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made of retinoid (retinol, retinoic acid, retinal, and the
like), pangamic acid, kinetin, ursolic acid, an extract of
Curcuma longa, sphirigosine derivatives, silicon, silicic acid,
N-methyl-L-serine, mevalonolactone, andthe like. Preferable
are retinoid (retinol, retinoic acid, retinal, and the like) ,
and kinetin.
[0026]
As examples of humectant components, mention may be made
of amino acids and derivatives thereof such as alanine, serine,
leucine, isoleucine, threonine, glycine, proline,
hydroxyproline, glucosamine, theanine, and the like; peptides
such as collagen, collagen peptide, gelatin, and the like;
polyhydric alcohols such as glycerol, 1,3-butylene glycol,
propylene glycol, polyethylene glycol, and the like; sugar
alcohols such as sorbitol and the like; phospholipids such as
lecithin, hydrogenated lecithin, and the like;
mucopolysaccharides such as hyaluronic acid, heparin,
chondroitin, and the like; components based on NMF such as
lactic acid, sodium pyrrolidone carbonate, urea, and the like;
polyglutamic acid, and the like. Preferable are alanine,
serine, glycine, proline, hydroxyproline, glucosamine,
theanine, collagen, collagen peptide, glycerol, 1,3-butylene
glycol, hydrogenated lecithin, hyaluronic acid, heparin,
chondroitin, lactic acid, sodium pyrrolidone carbonate, and
polyglutamic acid.
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[0027]
In the case of employing humectant components, the ratio
thereof blended in the preparation for external use on skin
of the present invention commonly ranges from 0.1 to 10% by
weight, preferably ranges from 0.5 to 5% by weight, and more
preferably ranges from 0.5 to 5% by weight [sic].
[0028]
In the preparation for external use on skin of the present
invention, in addition to the components described above,
surfactants, solubilizing components, fats and oils, sugars,
or percutaneous absorption accelerator components can be
further blended. In particular, by blending surfactants,
solubilizing components, or fats and oils, stability of the
water-soluble ascorbic acid in an aqueous medium, efficacy
thereof, and sensation in use can be improved.
[0029]
As examples of surfactants employed herein, mention may
be made of various nonionic surfactants, examples of which
include polyoxyethylene (hereinafter, referred to as POE)
branched alkyl ethers such as POE octyldodecyl alcohol, POE
2-decyltetradecyl alcohol, and the like; POE alkyl ethers such
as POE oleyl alcohol ether, POE cetyl alcohol ether, and the
like; sorbitan esters such as sorbitan monooleate, sorbitan
monoisostearate, sorbitan monolaurate, and the like; POE
sorbitan esters such as POE sorbitan monooleate, POE sorbitan
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monoisostearate, POE sorbitan monolaurate, and the like;
glycerol fatty acid esters such as glycerol monooleate,
glycerol monostearate, glycerol monomyristate, and the like;
POE glycerol fatty acid esters such as POE glycerol monooleate,
POE glycerol monostearate, POE glycerol monomyristate, and the
like; POE hardened castor oil fatty acid esters such as POE
dihydrocholesterol ester, POE hardened castor oil, POE
hardened castor oil isostearate, and the like; POE alkyl aryl
ethers such as POE octyl phenyl ether, and the like; glycerol
alkyl ethers such as monoisostearyl glyceryl ether,
monomyristyl glyceryl ether, and the likes POE glycerol alkyl
ethers such as POE monostearyl glyceryl ether, POE monomyristyl
glyceryl ether, and the like; polyglycerol fatty acid esters
such as diglyceryl monostearate, decaglyceryl decastearate,
decaglyceryl decaisostearate, diglyceryl diisostearate, and
the like; or natural surfactants such as lecithin, hydrogenated
lecithin, saponin, surfactin sodium salt, cholesterol, bile
acid, and the like; and the like. The surfactants described
above can be employed alone or in combination of two or more
kinds thereof.
(0030]
As fats and oils, they are not particularly limited as
long as they are those employed as components of preparations
for external use in the field of medicines, quasi drugs, or
cosmetics. As examples thereof, mention may be made of
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synthetic oils such as middle-chain fatty acid triglyceride,
and the like; vegetable oils such as soybean oil, rice oil,
rapeseed oil, cotton seed oil, sesame oil, safflower oil,
castor oil, olive oil, cacao butter, camellia oil, sunflower
oil, palm oil, linseed oil, perilla oil, shea oil, saru
[phonetic spelling] oil, coconut oil, Japan wax, jojoba oil,
grape seed oil, avocado oil, and the like; animal oils such
as mink oil, yolk oil, beef tallow, milk fat, lard, and the
liked waxes such as beeswax, spermaceti wax, lanolin, carnauba
wax, candelilla wax, and the like; hydrocarbons such as liquid
paraffin, squalene, squalane, microcrystalline wax, ceresin
wax, paraffin wax, vaseline, and the like; natural or synthetic
fatty acids such as lauric acid, myristic acid, stearic acid,
oleic acid, isostearic acid, behenic acid, and the like;
natural or synthetic higher alcohols such as cetanol, stearyl
alcohol, hexyldecanol, octyldecanol, lauryl alcohol, and the
like; esters or ethers such as isopropyl myristate, isopropyl
palmitate, octyldodecyl myristate, octyldodecyl oleate,
cholesterol oleate, and the like; silicone oils; and the like.
The fats and oils described above can be employed alone or in
combination of two or more kinds thereof.
[0031]
As sugars, they are not particularly limited as long as
they are those employed as components of preparations for
external use in the field of medicines, quasi drugs, or
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cosmetics. As examples thereof, mention may be made of
monosaccharides (such as glucose, galactose, mannose, ribose,
arabinose, xylose, deoxyribose, fructose, ribulose, lyxose,
and the like), disaccharides (such as sucrose, trehalose,
lactose, maltose, cellobiose, and the like), oligosaccharides
(such as lactulose, raffinose, pullulan, and the like),
cellulose and derivatives thereof (such as methylcellulose,
ethylcellulose, hydroxyethylcellulose,
hydroxypropylcellulose, carboxymethylcellulose,
carboxyethylcellulose, nitrocellulose, and the like), polymer
sugars (such as chondroitin sulfate, hyaluronic acid, dermatan,
heparan, heparin, keratan, and salts thereof
(pharmaceutically or physiologically acceptable salts such as
sodium chondroitin sulfate, sodium hyaluronate, dermatan
sulfate, haparan sulfate, keratan sulfate, and the like) , and
the like), and sugar alcohols (such as mannitol, xylitol,
erythritol, pentaerythritol, maltitol, sorbitol,
polydextrose, and the like) , and in addition, xylose, inositol,
dextrin and derivatives thereof, honey, a muscovado extract,
and the like. The sugars described above may be employed alone
or in combination of two or more kinds thereof.
[0032]
In the preparation for external use on skin of the present
invention, various components which are generally employed as
components of preparations for external use in the field of
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medicines, quasi drugs, or cosmetics, such as amino acids,
reducers for irritation, thickening agents, preservatives, UV
controlling agents, coloring agents, pH adjustors, perfumes,
and the like, can be blended within a quantitative and
qualitative range which does not impair the quality such as
apparent stability, viscosity, and the like, and does not
impair the effects of the present invention. The components
described above can be freely employed alone or in combination
of two or more kinds thereof.
[0033]
The preparation for external use on skin of the present
invention can be prepared in a preferable form of a paste, a
mousse, a gel, a liquid, a milky lotion, a cream, a sheet (base
material carrier) , an aerosol, a spray, or the like, by blending
and mixing each of optional components described above if
necessary, and in addition, blending another solvent or a base
agent of a preparation for external use generally employed or
the like if necessary. They can be produced in a conventional
method known in the art.
[0034]
The preparation for external use on skin of the present
invention may commonly have liquid properties at pH 1 to pH
8. In view of stability of the water-soluble ascorbic acid,
low irritation with respect to the skin and mucosa, and a good
sensation in use on the skin, it is in the range of preferably
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from pH 2 to pH 7, and more preferably from pH 2 to pH 6.
[0035]
The preparation for external use on skin of the present
invention can be formed into various compositions for external
use in the field of cosmetics, medicines for external use, or
quasi drugs for external use, including makeup cosmetics such
as foundations, lipsticks, mascaras, eye shadows, eyeliners,
eyebrow colors and nail varnishes; base cosmetics such as milky
lotions, creams, lotions, oils and facial packs; cleansing
compositions such as face cleansing compositions, cleansers
and body washes; underarm deodorants, athlete's foot remedies,
anti-itching preparations, wound healing preparations, dry
bathing preparations, cleaning preparations,
anti-inflammatory analgesic preparations, acne remedies,
hemorrhoidal preparations, sterilizing preparations,
whitening preparations, UV controlling preparations, and the
like. In view of enhancing effects on the skin, the preparation
of the present invention is preferably employed as a product
for applying on the outer skin, such as a percutaneous
preparation.
EXAMPLES
[0036]
In the following, the present invention is described in
detail based on Examples and Test Examples. It should be
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understood that the present invention is not limited to the
Examples and the like. In each of the composition examples
described below, "°s" means % by weight (W/W) , unless otherwise
indicated.
[0037]
Test Example 1
The dorsal skin of a hairless mouse was pinched and fixed
between percutaneous absorption cells, and the cell at the
receptor side was filled with saline and the cell at the donor
side was filled with each of the preparations shown in Table
1. The solutions in both cells were incubated at 37°C while
being agitated with a stirrer bar. After 24 hours, the
concentration of ascorbic acid in the solution at the receptor
side was measured by high performance liquid chromatography.
The measurement results are shown in Table 1. The results are
represented by the relative ratio based on the permeation
amount of ascorbic acid in Comparative Example 1 (solution
containing only ascorbic acid), which was defined as 1.
[0038]
Table 1
ComparativeComparativeComparativeExample Example
Exam le Exam Exam le 1 2
1 le 2 3
L-ascorbic acid 10% 10% 10% 10% 10%
Diglycerol - 5% - 5% 10%
Trimethylglycine - - 5% 5% 2%
Water 90% 85% 85% 80% 78%
Relative ratio of percutaneous1.0 1.2 1.5 2.0 1.8
permeation amount
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[0039]
From the results of the test, it could be confirmed that,
in the case of combining diglycerol and trimethylglycine, the
permeation amount of ascorbic acid, namely, percutaneous
absorption amount thereof was increased. The preparation for
external use on skin comprising ascorbic acid together with
diglycerol and trimethylglycine can deliver ascorbic acid into
the skin more; thus, an effect that ascorbic acid possesses
can be sufficiently exhibited.
[0040]
Test Example 2
Ten panelists were asked to actually use the preparations
of Comparative Example 1 and Example 2, and to perform sensory
evaluation in terms of improvement of the skin pigmentation,
improvement of the skin dullness, an elasticity sensation of
the skin, and a moisturizing sensation of the skin. They were
asked to apply the preparations to the entire face twice a day
after washing the face and treating the skin with the lotion
usually employed. The evaluation was performed by first,
employing the preparation of Comparative Example 1
continuously for 2 weeks, then, employing the preparation of
Example 2 continuously for 2 weeks. As the evaluation criteria,
the panelists were asked to evaluate whether the preparation
of Example 2 is better than, almost equal to, or inferior to
that of Comparative Example 1, and the cases where the ratio
CA 02508093 2005-05-20
of the panelists who answered that the preparation of Example
2 is better than that of Comparative Example l,is 80~ or higher
was defined as 00, from 60 to 80% was defined as O, from 50
to 60~ was defined as d, and lower than 50~ was defined as x.
In addition, the same sensory evaluation was performed by
asking panelists to actually use the preparations of
Comparative Example 1 and Comparative Example 3. The results
are shown in Table 2.
[0041]
Table 2
Comparative Example 2
Example 3
Improvement of the skin pigmentationD O
Improvement of the skin dullnessO 00
Elasticity sensation of the O 00
skin
Moisturizing sensation of D 00
the skin
[0042]
From the results of the test, it was confirmed that, in
the case of the preparation of Example 2 in which diglycerol
and trimethylglycine were contained together with ascorbic
acid, the percutaneous absorption of ascorbic acid was
increased, an effect that ascorbic acid possesses was
sufficiently exhibited, whereby the skin dullness and
pigmentation was improved, elasticity of the skin was increased,
a moisturizing sensation of the skin was improved, and an
excellent effect on restoring the skin's moisture and the firm
26
appearance of the skin was exhibited.
27
