JP2003183148A - Skin care composition for external use - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a shin care composition for external use showing an excellent skin-moisturizing effect and skin dryness-improving effect which moisturizes a dry skin and inhibits itch and eczema. <P>SOLUTION: This skin care composition for external use contains (A) ceramides, (B) at least one polyol selected from polyols each having a valency of ≥2 and (C) at least one kind selected from the group consisting of antiphlogistic compounds and aitinflammatory compounds, wherein the weight ratio of the component (A)/component (B) is from 1/100 to 100/1. The skin care composition further contains at least one plant extract. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an external preparation for skin, and more particularly, to an elderly person who is excellent in the moisturizing effect and skin improving effect on the skin and moisturizes dry skin to suppress itching and eczema. It relates to an optimal external preparation composition for skin.

[0002]

2. Description of the Related Art Conventionally, moisture in the stratum corneum is important for moisturizing the skin and making the skin soft. To maintain this moisture, water-soluble components contained in the stratum corneum, namely free It is known that amino acids, urea, organic acids, inorganic ions, etc. are involved. Therefore, for the purpose of improving or preventing rough skin, such a water-soluble component is mixed with an external skin preparation or a cosmetic and used. Further, for the same purpose, various moisturizing substances having high affinity with water have been developed and used. In particular, many elderly people have dry skin, and many symptoms such as senile xerosis, senile pruritus, and sebum-deficient eczema are observed. Therefore, skin care for the elderly is important, and external skin preparations and cosmetics are used after bathing in hospitals and welfare facilities.

However, when these moisturizing substances are applied to the skin, the action is to supply water to the stratum corneum on the skin horny layer, and its effect is temporary, so that it is fundamental. To improve the water retention capacity of keratin,
It was not essentially to prevent or cure the rough skin.

On the other hand, ceramides are present in the stratum corneum of the skin,
It is known to contribute to its barrier ability and water retention ability, and it is also known to improve the dry condition of the skin by external application.

As such ceramides, generally, natural ceramides (cattle brain extract and plant extract), synthetic ceramides (by combination with fermentation method and organic synthesis),
A synthetic pseudo ceramide (a synthetic product having a function and structure similar to ceramide) is appropriately used.

In Japanese Patent Laid-Open No. 4-112810, the solid fat content in fats and oils is 70% by weight or more, and the amount of intercorneocyte lipids in solid fats, that is, the content of ceramides is 50% by weight or more. Emulsified water-soluble cosmetics are described. However, the effect of suppressing itching and eczema is insufficient,
I was not satisfied.

Further, in JP-A-8-119847, by using a ceramide in combination with a dicarboxylic acid, a dicarboxylic acid salt, and a polyhydric alcohol, it is possible to obtain an excellent moisturizing ability and to induce a feeling of irritation. No skin cosmetics have been proposed. However, it is insufficient for the elderly with dry skin, and it has been difficult to control itching symptoms and eczema.

[0008]

SUMMARY OF THE INVENTION Therefore, the object of the present invention is to provide a skin external preparation composition which is excellent in moisturizing effect and skin improving effect on skin and moisturizes dry skin to suppress itching and eczema, especially for elderly people. It is to provide a person with an optimal external composition for skin.

[0009]

The present inventors have blended ceramides, divalent or higher valent polyols and anti-inflammatory or anti-inflammatory action compounds, and ceramides and divalent or higher valent polyols in a specific ratio. It was found that the above-mentioned external preparation for skin has an excellent moisturizing effect on skin and an effect of improving bulkiness, moisturizes dry skin, and suppresses itch and eczema, and completed the present invention.

That is, according to the present invention, the components (A) and (B) are
And (C) (A) ceramides (B) containing one or more kinds selected from divalent or higher-valent polyols (C) one or more kinds selected from the group of anti-inflammatory compounds and anti-inflammatory compounds, and the component (A) / Weight ratio of component (B) is 1/10
The external preparation composition for skin is 0 to 100/1.

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION Component (A) used in the present invention
Is an amphipathic lipid having one or more hydroxyl groups and amide groups in the molecule, which is a natural ceramide, a synthetic ceramide, or an analog thereof (also referred to as a synthetic pseudoceramide) obtained at the room temperature ( The solid state at 25 ° C.) is referred to simply as ceramides. Examples of such ceramides include Ceramide H03 (Sederma, trihydroxypalmitoamide hydroxypropylmyristyl ether), Ceramide II (Quest, ceramide 2), Questamide
H (Quest, bishydroxyethyl biscetyl malonamide), Ceramide TIC-001 (Takasago fragrance, (2S, 3R) -2-
Octadecanoylaminooctadecane-1,3-diol), Sofcare ceramide SL-E (Kao, N- (hexadecyloxyhydroxypropyl) -N-hydroxyethylhexadecanamide) and the like can be mentioned.

The ceramides may be any one or more selected from the group consisting of natural ceramides, synthetic ceramides and synthetic pseudoceramides, from the viewpoints of the moisturizing effect on the skin of the elderly and the effect of improving bulkiness and the effect of suppressing itching and eczema. Can be used for.

The synthetic ceramide has the general formula (1)

[0014]

[Chemical 3]

(In the formula, R ¹ and R ² represent a linear or branched, saturated or unsaturated hydrocarbon group having 8 to 26 carbon atoms, which may be substituted by one or more hydroxyl groups.) The synthetic ceramides represented are preferred. As the synthetic pseudo ceramide, a compound represented by the general formula (2)

[0016]

[Chemical 4]

(In the formula, R ³ represents a straight chain or branched chain saturated or unsaturated hydrocarbon group having 10 to 26 carbon atoms, and R ⁴ represents a straight chain or branched chain saturated or unsaturated group having 9 to 25 carbon atoms. A synthetic pseudo-ceramide represented by (showing an unsaturated hydrocarbon group) is preferable.

The synthetic ceramide represented by the general formula (1):
Examples of the hydrocarbon group represented by R ¹ and R ² include octyl group, nonyl group, decyl group, undecyl group, dodecyl group, tridecyl group, tetradecyl group, pentadecyl group,
Hexadecyl group, heptadecyl group, octadecyl group, nonadecyl group, eicosyl group, heneicosyl group, docosyl group, tricosyl group, tetracosyl group, pentacosyl group, hexacosyl group, nonenyl group, decenyl group, undecenyl group, dodecenyl group, tridecenyl group, tetradecenyl group , Pentadecenyl group, hexadecenyl group, heptadecenyl group, octadecenyl group, nonadecenyl group, eicosenyl group, heneicosenyl group, docosenyl group, tricosenyl group, tetracocenyl group, pentacosenyl group, hexacocenyl group, nonadienyl group, decadienyl group, undecadienyl group, undecadienyl group, undecadecenyl group Group, tetradecadienyl group, pentadecadienyl group,
Hexadecadienyl group, heptadecadienyl group, octadecadienyl group, nonadecadienyl group, eicosadienyl group, heneicosadienyl group, docosadienyl group, tricosadienyl group, tetracosadienyl group, pentacosadienyl group, hexaco Examples thereof include a sadienyl group, a 2-hexyldecyl group, a 2-octylundecyl group, a 2-decyltetradecyl group, and groups in which 1 to 3 hydroxyl groups are substituted in these groups. In the present invention, as R ¹ and R ² , an alkyl group having 8 to 26 carbon atoms, particularly an alkyl group having 10 to 18 carbon atoms is preferable. Incidentally, R ¹ and R ² may be the same or different.

The hydrocarbon group represented by R ³ of the synthetic pseudo-ceramide represented by the general formula (2) is a group in which a hydroxyl group is substituted in R ¹ and R ² and a hydrocarbon group having 8 to 9 carbon atoms. Examples of the group represented by R ⁴ include a group in which a hydroxyl group is substituted in R ¹ and R ² and a group excluding a hydrocarbon group having 8 and 26 carbon atoms. In the present invention, R ³ is preferably an alkyl group having 10 to 18 carbon atoms, and R ⁴ is preferably an alkyl group having 9 to 17 carbon atoms. Incidentally, R ³ and R ⁴ may be the same or different.

The synthetic pseudo-ceramide represented by the general formula (2) can be prepared by a known method [for example, Polish Journal of Chemistry (Pol. J. Chem.) 52 . 1059 (1978),
Same 52 . 1283 (1978), JP-A-62-228048, JP-A-63-
It can be manufactured according to Japanese Patent Laid-Open No. 192703 and Japanese Patent Laid-Open No. 63-216852.

The content of the component (A) used in the present invention is 0.00 in the skin external preparation composition from the viewpoints of the moisturizing effect on the skin, the effect of improving bulkiness, and the effect of suppressing itch and eczema.
5 to 20% by weight (hereinafter simply referred to as%) is preferable,
0.01 to 10% is more preferable, 0.03 to 10% is further preferable, and 0.1 to 5% is particularly preferable. Two or more kinds of the component (A) may be contained, in which case the total amount is the content.

As the component (B) used in the present invention,
Ethylene glycol, propylene glycol, 1,3-
Glycols such as butylene glycol, 1,4-butylene glycol and dipropylene glycol; glycerin;
Polyglycerins such as diglycerin, triglycerin and tetraglycerin; monosaccharides such as glucose and fructose; polysaccharides such as sucrose, maltose and maltitol; starch-degrading sugar reducing alcohols such as xylitol, sorbitol, maltotriose, threitol and erythritol. Etc. can be mentioned.

Ethylene glycol, propylene glycol, 1,3-butylene glycol and glycerin are preferable from the viewpoints of moisturizing effect on skin, improving bulkiness and preventing stickiness.

The content of the component (B) used in the present invention is from the viewpoint of the skin moisturizing effect and the bulkiness improving effect.
0.01 to 30% is preferable in the skin external preparation composition,
0.1 to 25% is more preferable, 0.5 to 20% is still more preferable, and 1 to 15% is particularly preferable. Ingredient (B) is 2
One or more species may be contained, in which case the total weight is the content.

The content weight ratio (A) / (B) of the component (A) and the component (B) used in the present invention is from the viewpoint of the skin moisturizing effect and the effect of improving bulkiness, and the effect of suppressing itching and eczema. , 1/100 to 100/1 are preferable, and 1/80
To 80/1 are more preferable, 1/50 to 50/1 are still more preferable, 1/30 to 30/1 are particularly preferable, and 1/2
0-20 / 1 is the most preferable.

As the component (C) used in the present invention,
Guaiazulene, Allantoin, Glycyrrhizic acid, Glycyrrhizic acid salt, Tranexamic acid, ε-Amino-n-
Examples thereof include caproic acid ester, epidihydrocholesterol, epidihydrocholesterol phosphoric acid ester and the like. From the viewpoint of the effect of suppressing itching and eczema on the skin of the elderly,
Guaiazulene, allantoin, glycyrrhizinic acid and glycyrrhizinate are preferred.

The amount of the component (C) used in the present invention is preferably 0.0001 to 10% in the composition, and 0.001 to 5%, from the viewpoint of the effect of suppressing itching and eczema of the skin.
Is more preferable, 0.01 to 5% is still more preferable, and 0.
1-2% is particularly preferable. Two or more kinds of component (C) may be contained, in which case the total weight is the content.

From the viewpoint of skin moisturizing and bulkiness improving effects, the present invention preferably further contains a plant extract (also referred to as component (D)) containing no component (A). The plant extract used in the present invention, asunaro, green tea,
Persimmon leaf, horse chestnut, hamamelis, chamomile, tuberose, eucalyptus, hop, ginger, gambir,
Neubara, horse chestnut, lily, pearl barley, cattail,
Examples of the extract include loquat, gardenia, rapeseed ginseng, saponum, birch, armature, clove, safflower, oleander, iris and clara.

The solvent used for extraction is usually one used for extraction of plant components, such as water, petroleum ether, n.
-Hexane, toluene, dichloroethane, chloroform, ether, ethyl acetate, acetone, methanol, ethanol, propanol, butanol, ethylene glycol, propylene glycol, butylene glycol and the like can be mentioned, and water, ethanol, propylene glycol and butylene glycol are particularly preferable. These can be used alone or in combination of two or more. In addition, the extraction conditions can be applied to normal conditions, and for example, the above plants can be used for 3-10
Immersion or heating under reflux may be performed at 0 ° C. for several hours to several weeks. When used as an essential oil, a usual method can be adopted, and for example, it can be obtained from the above plant by steam distillation, extraction method, compression method, or the like. The extract, steam distillate or compressed product of these plants can be used in the present invention as it is, but a fraction having a high activity is fractionated by a suitable separation means such as gel filtration, chromatography or precision distillation. You can also

Eucalyptus extract, hamamelis extract, and asunaro extract are preferable from the viewpoints of moisturizing and improving the bulkiness of the skin.

The content of the plant extract used in the present invention is from the viewpoint of the moisturizing effect on skin and the effect of improving bulkiness.
0.01 to 30% is preferable in the composition, and 0.05 to 2
0% is more preferable, 0.05 to 15% is further preferable, and 0.1 to 10% is particularly preferable. Two or more kinds of plant extracts may be contained, in which case the total weight is the content.

An antiseptic agent or a bactericidal agent can be added to the composition for external preparation for skin of the present invention. For example, benzoic acid,
Methylparaben, ethylparaben, propylparaben,
Butylparaben, ethanol, isopropanol, isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, chlorohexidine gluconate and the like can be mentioned. When these preservatives or bactericides are blended, the composition for external preparation for skin contains 0.0001 to 5%, preferably 0.001 to 5%, more preferably 0.005 to 2%.
%, Particularly preferably 0.005 to 1%.

The skin external preparation composition of the present invention is further added with components such as oil, water and a surfactant which are usually used in the skin external preparation composition, and an emulsion type, a dispersion type, a two-layer type and a solubilizing type are added. ,
It can be made into a desired dosage form such as gel, and can be made into lotion, emulsion, cream, pack, foundation and the like.

Examples of the oil component include hydrocarbons such as solid or liquid paraffin, crystal oil, ceresin, ozokerite, montan wax, squalane, and squalene; olive oil; carnauba wax; lanolin; jojoba oil; glycerin monostearate ester, glycerin distearin. Ester oils such as acid esters, glycerin monooleate, isopropyl stearate, neopentyl glycol dicaprate, cholesterol isostearate; higher fatty acids such as stearic acid and palmitic acid; higher alcohols such as cetanol and stearyl alcohol; cholesterol, etc. The sterols can be used. When these oils are added, it is preferable to add 0.01 to 50%, and particularly preferably 0.05 to 30% to the skin external preparation composition.

When the external skin preparation composition of the present invention is emulsified or solubilized, it is preferable to add a surfactant. Examples of the surfactant include polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester,
Polyoxyethylene sorbitol fatty acid ester, glycerin fatty acid ester, polyoxyethylene hydrogenated castor oil alkyl sulfate ester, polyoxyethylene alkyl sulfate ester, alkyl phosphate ester, polyoxyethylene alkyl phosphate ester, fatty acid alkali metal salt, sorbitan fatty acid ester, Examples thereof include alkyl glyceryl ether. When these surfactants are blended, 0.01 to 5 is added to the skin external preparation composition.
It is preferably 0%, and particularly preferably 0.05 to 30%.

The external preparation for skin of the present invention may further contain silicones as an oil or a surfactant. The silicones are not particularly limited as long as they are usually blended in a skin external preparation, and for example, octamethylpolysiloxane, tetradecamethylpolysiloxane, methylpolysiloxane, highly polymerized methylpolysiloxane, methylphenyl. In addition to polysiloxane,
Methyl polycyclosiloxanes such as octamethylcyclotetrasiloxane and decamethylcyclopentasiloxane,
Trimethylsiloxysilicic acid, further polyether modified silicone, polyether alkyl modified silicone,
Examples thereof include alkyl glyceryl ether modified silicone. When blending these silicones,
When used as an oil component, such as dimethylpolysiloxane, when used as a surfactant, such as dimethylpolysiloxane, when used as a surfactant, the total amount of non-silicone oil component or surfactant The amount may be adjusted to be the above amount.

The external preparation composition for skin of the present invention may be further blended with a powder to provide a makeup cosmetic such as a foundation. Examples of this powder include mica,
Extenders such as talc, sericite, kaolin, nylon powder, polymethylsilsesquioxane, inorganic pigments such as pearl, red 202, red 226, yellow 4, organic pigments such as aluminum lake, zinc oxide, titanium oxide, oxidation Examples thereof include inorganic powders such as zirconium and iron oxide for protection against ultraviolet rays. These powders are treated with silicone such as methylhydrodienemethylpolysiloxane, trimethylsiloxysilicic acid, methylpolysiloxane, etc., fluorine treatment with perfluoroalkyl phosphate ester, perfluoroalcohol etc., amino acid treatment with N-acyl glutamic acid etc., Those treated with lecithin, metal soap, fatty acid, alkyl phosphate, etc. can also be used. When these powders are blended, the blending amount in the external skin preparation composition can be appropriately set according to the dosage form, but it is usually preferably 0.1 to 50%, and particularly preferably 1 to 30. % Is preferable.

Further, the skin external preparation composition of the present invention may contain various components which are usually added to cosmetics, quasi-drugs, pharmaceuticals, etc. within a range not impairing the object of the present invention. Examples of such components include inorganic salts such as magnesium sulfate, potassium sulfate, sodium sulfate, magnesium chloride, sodium chloride; polyvinyl alcohol, carboxyvinyl polymer, carboxymethyl cellulose, gelatin, tragacanth gum, xanthan gum, agarose, etc. viscosity modifiers; ultraviolet rays Absorbents, pigments, fragrances and the like can be mentioned.

The external preparation for skin of the present invention has an excellent moisturizing effect on skin and an effect of improving bulkiness, moisturizes dry skin, especially the skin of elderly people, and can suppress itching and eczema. The reason for this is presumed to be that the ceramides, the anti-inflammatory compound and / or the anti-inflammatory compound can easily penetrate into the dried skin stratum corneum due to the synergistic effect with the divalent or higher valent polyol.

[0040]

EXAMPLES Production Examples Synthetic pseudoceramides (1) to (2) and synthetic ceramides (1) to (2) shown in Table 1 produced according to the method described in Example 2 of JP-A-62-228048. 2) was used in the examples.

[0041]

[Table 1]

Examples 1 to 10 and Comparative Examples 1 to 8 According to the formulation shown in Table 2 below, skin external preparation compositions were prepared by a conventional method.

[0043]

[Table 2]

Test Example 1 In order to examine the effect of the external preparation composition for skin of the present invention, the compounded compositions shown in Examples 1 to 10 and Comparative Examples 1 to 8 in Table 2 were used for skin roughness, itching, eczema, etc. Once a day for 7 20 panelists over 65 who have skin symptoms
A use test was carried out in which the composition was applied to a site with skin symptoms for consecutive days. The results are shown in Table 3.

[0045]

[Table 3]

From the results shown in Table 3, it is clear that the external preparation for skin of the present invention has a moist feeling on the skin, a high effect of improving bulkiness, a high effect of suppressing itching and eczema, and no sticky feeling on the skin. became.

Test Example 2 Using the skin external preparation compositions of Example 2 and Comparative Example 2, 19 panelists aged 65 years or older who have skin symptoms such as skin roughness, itching, and eczema once a day. A use test of applying to the right lower limb was performed once and continuously for 8 weeks. After the use test, for skin "dryness", "desquamation", "scarring", "erythema", "wetting / thickening", "papule / small blisters" and "erosion" skin rash before the test start and for 8 weeks Each of the subsequent cases was diagnosed, and the degree of improvement was evaluated on the basis of five grades of marked improvement, improvement, slight improvement, unchanged and deterioration. The results are shown in Table 4.

[0048]

[Table 4]

From the results shown in Table 4, it is clear that the external preparation for skin of the present invention has a high skin improving effect.

[0050]

EFFECTS OF THE INVENTION The external preparation for skin of the present invention is excellent in the moisturizing effect on the skin and the effect of improving the bulkiness, and it is effective in moisturizing the dry skin of the elderly and suppressing the itching and eczema.

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Claims (4)

[Claims] 1. Components (A), (B) and (C) (A) Ceramides (B) One or more selected from dihydric or higher polyols (C) From the group of anti-inflammatory compounds and anti-inflammatory compounds Contains at least one selected, and the weight ratio of component (A) / component (B) is 1/10
A skin external preparation composition which is 0 to 100/1. 2. The external skin preparation composition according to claim 1, wherein the component (B) is at least one selected from ethylene glycol, propylene glycol, 1,3-butylene glycol and glycerin. 3. The external skin preparation composition according to claim 1, further comprising one or more kinds of plant extracts containing no component (A). 4. The component (A) is represented by the general formula (1): (In the formula, R ¹ and R ² represent a linear or branched saturated or unsaturated hydrocarbon group having 8 to 26 carbon atoms, which may be substituted by one or more hydroxyl groups.). Synthetic ceramide or general formula (2) (In the formula, R ³ represents a linear or branched saturated or unsaturated hydrocarbon group having 10 to 26 carbon atoms, and R ⁴ represents 9 to 2 carbon atoms.
5 represents a straight chain or branched chain saturated or unsaturated hydrocarbon group. 1) selected from the group of synthetic pseudo-ceramides represented by
The external preparation composition for skin according to any one of claims 1 to 3, which is one or more kinds.