JPH1017457A - Percutaneous absorption-stimulating preparation for external use for skin - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a percutaneous absorption-stimulating preparation for external use for skin, excellent in a roughened skin-improving effect by compounding a carboxylic acid derivative, water and one of polysaccharides. SOLUTION: This percutaneous absorption-stimulating preparation for external use for skin contains a carboxylic acid derivative as a water-soluble physiologically active ingredient, water and one or more kinds of polysaccharides. The carboxylic acid derivative and the polysaccharide are compounded in amounts of 0.01-5wt.% and 0.01-2wt.%, respectively. The carboxylic acid derivative is e.g. γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, and the polysaccharide is e.g. xanthane gum, carrageenan. The preparation can be applied to cosmetics and medicines. The ingredients in the percutaneous absorption- stimulating preparation for external use for skin act on the skin to stimulate the percutaneous absorption of the carboxylic acid derivative and accelerate the functions of the skin. Therefore, the preparation can allow to express an excellent roughened skin-improving effect in a short time and sustain the effect.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a transdermal preparation for percutaneous absorption promotion. More specifically, it promotes the absorption of carboxylic acid derivatives that are water-soluble physiologically active ingredients in the skin,
The present invention relates to a percutaneous absorption promoting skin external preparation having an excellent effect of improving rough skin.

[0002]

BACKGROUND OF THE INVENTION It is known that water-soluble physiologically active ingredients generally have a lower skin absorption rate than oil-soluble physiologically active ingredients. The present applicant has previously described γ-aminobutyric acid, γ-amino-β-hydroxybutyric acid, and derivatives thereof (Japanese Patent Publication No. 58-26726).
And diisopropylamine dichloroacetate (Japanese Patent Application Laid-Open No. 53-136528) have been found to have an antiaging effect and a beautiful skin effect by improving the skin function of a carboxylic acid derivative which is a water-soluble physiologically active ingredient. .

On the other hand, up to the present, as a transdermal absorption enhancer, an aprotic solvent such as dimethyl sulfoxide or 1-
Dodecylazacycloheptan-2-one (commonly referred to as A
ZONE), terpenes, menthols and the like have been reported, and the present applicant has previously found that hair growth effects of a hair restorer containing sesquiterpenes and having a percutaneous absorption-promoting effect have a hair growth effect. (Japanese Unexamined Patent Publication No. 6-135821)
No.). However, preparations containing these compounds are not preferable as external preparations for the skin, such as damaging the epidermis and causing irritation. An object of the present invention is to provide a percutaneous absorption-promoting skin external preparation having an excellent effect of improving rough skin.

[0004]

SUMMARY OF THE INVENTION In view of such circumstances, the present inventor has set forth the above object as one or two or more selected from specific carboxylic acid derivatives, water and polysaccharides. It has been found that this can be achieved by a transdermal preparation for percutaneous absorption accelerating skin which comprises at least two or more species. That is, the present invention is a percutaneous absorption promoting skin external preparation comprising a carboxylic acid derivative, water, and one or more selected from polysaccharides.

[0005]

Embodiments of the present invention will be described below in detail. Examples of the carboxylic acid derivatives used in the transdermal absorption promoting skin external preparation of the present invention include, for example, γ-aminobutyric acid and γ-aminobutyric acid.
Organic compounds having a carboxyl group in a part of the structure, such as amino-β-hydroxybutyric acid, derivatives thereof, and diisopropylamine dichloroacetate, and salts thereof are exemplified. The compounding amount of the carboxylic acid derivative is desirably 0.01 to 5% by weight. If the amount is less than 0.01% by weight, a sufficient effect may not be exhibited. If the amount exceeds 5% by weight, an effect suitable for the amount may not be exhibited.

[0006] Polysaccharides used in the transdermal preparation for promoting percutaneous absorption of the present invention include, for example, xanthan gum, guar gum, bacterial cellulose, carrageenan and the like. The compounding amount of the polysaccharide is desirably 0.01 to 2% by weight. If the amount is less than 0.01% by weight, a sufficient effect may not be exhibited. If the amount exceeds 2% by weight, an effect suitable for the amount may not be exhibited.

[0007] As described above, the percutaneous absorption promoting skin external preparation of the present invention comprises a mixture of one or more selected from carboxylic acid derivatives, water and polysaccharides. It acts on the skin to promote percutaneous absorption of the carboxylic acid derivative, enhances the skin function, and expresses a remarkable effect such as exhibiting and maintaining an excellent effect of improving rough skin in a short time.

[0008] The percutaneous absorption promoting skin external preparation of the present invention can be applied, for example, as a cosmetic or pharmaceutical, and as a dosage form, it can be applied to lotions, emulsions, creams, packs and the like. it can. In addition, in addition to the above, the percutaneous absorption promoting skin external preparation of the present invention, waxes, pigments, fragrances,
Preservatives, surfactants, pigments, vitamins, chelating agents,
Cooling agents, wetting agents, emulsifying aids, hormones, antioxidants and the like can be appropriately compounded within a range that achieves the object of the present invention.

[0009]

The present invention will be described below in detail based on examples and comparative examples. In addition, the unit of the compounding amount of the components described in Examples and Comparative Examples is% by weight. The percutaneous absorption test method is as follows. The acceptor part of the Franz vertical diffusion cell is filled with a phosphate buffer solution (containing 150 mM sodium chloride, pH 7.2), and the abdominal skin of a hairless rat that has been peeled off is mounted.
The samples shown in the following Examples and Comparative Examples were provided on the skin, and the amount of the carboxylic acid derivative that permeated the skin and accumulated in the phosphate buffer solution in the acceptor portion was quantified by high performance liquid chromatography. The experiment was performed in three groups, and the average value was calculated. The evaluation was based on the results. The sensory test method for improving rough skin is as follows. A sample was applied twice a day (morning and evening) to 20 female subjects (35 to 55 years old) who complain of rough skin, fine wrinkles, and dry skin for three consecutive months, and the effect after two months was evaluated. As a result of the test, the skin softness, smoothness, and elasticity were evaluated, and as a result, overall, "the skin was moistened", "the skin became smooth", and "the skin became taut" And the number of respondents.

Examples 1 to 4 and Comparative Example 1 Carboxylic acid derivatives were blended as shown in Table 1, each external preparation for skin was prepared with the following composition, and the above experiment was carried out. The permeation amount of the carboxylic acid derivative was determined.
Note that diisopropylamine dichloroacetate is DAD
Abbreviated as A.

[0011]

[Table 1]

(1) Preparation method Each of (A) and (B) is uniformly dissolved at room temperature, (B) is added to (A) with stirring, and emulsified and dispersed to prepare.

(2) Characteristics Table 1 shows the results of tests conducted on each transdermal absorption promoting skin external preparation. As shown in Table 1, Examples 1 to 5 of the present invention
DADA of the skin external preparation of Comparative Example 4 was higher than DADA of the skin external preparation of Comparative Example 1.
A remarkable absorption-promoting effect was observed in the absorption of. Also,
The skin external preparations of Examples 1 to 4 of the present invention were also superior to the skin external preparation of Comparative Example 1 in the rough skin improving effect.

Examples 5 to 8 and Comparative Example 2 Carboxylic acid derivatives were blended as shown in Table 2, each skin external preparation was prepared with the following composition, and the above experiment was carried out. The permeation amount of the carboxylic acid derivative was determined. Here, γ-aminobutyric acid and γ-amino-β-hydroxybutyric acid are abbreviated as GABA and GABOB, respectively.

[0015]

[Table 2]

(1) Preparation method Each of (A) and (B) is uniformly dissolved at room temperature, (B) is added to (A) with stirring, and emulsified and dispersed to prepare.

(2) Characteristics Table 2 shows the results of tests of each transdermal absorption promoting skin external preparation. As shown in Table 2, Examples 5 to 5 of the present invention
8 is more GABA than the skin external preparation of Comparative Example 2.
A remarkable transdermal absorption-promoting effect was observed in the absorption of. Also, the skin external preparations of Examples 5 to 8 of the present invention were superior to the skin external preparation of Comparative Example 2 in the effect of improving rough skin.

[0018]

As described above, it is apparent that the present invention provides an external preparation for skin which promotes the absorption of the carboxylic acid derivative of the present invention in the skin and is excellent in the effect of improving rough skin.

Claims (1)

[Claims] 1. A percutaneous absorption promoting external skin preparation comprising a carboxylic acid derivative, water and one or more selected from polysaccharides.