JPS627162B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to cosmetics for preventing skin aging (skin cosmetics used for preventing skin aging). More specifically, the present invention relates to skin cosmetics with excellent skin aging prevention effects (improving rough skin, improving keratin, increasing turnover rate, etc.). Aging skin is dry, rough skin that lacks smoothness and exhibits a phenomenon of exfoliation of keratin cells.
It is said that aging skin has a slow turnover rate, and that when an anti-aging effect is imparted to the skin, the turnover rate becomes faster. The applicant previously discovered and proposed that vitamin E orotate ester and γ-aminobutyric acid compounds enhance skin function and have an anti-aging effect by dilating peripheral blood vessels in the skin (Tokuko Showa).
52-2979 and Special Publication No. 58-26726). However, all of these effects are slow-acting, with creams showing their effects after 6 months and lotions showing their effects after 3 months.
This was not completely satisfactory and left room for improvement. The present inventors have conducted intensive research to improve this difficulty, and as a result, the following γ-
When aminobutyric acid compounds and vitamin E orotate ester are used together, the synergistic effect of the two results in excellent skin aging prevention effects (excellent effects on improving rough skin and keratin, and speeding up turnover rate). ) has been discovered in a very short period of time, one month after the start of use, and that a long-acting cosmetic for preventing skin aging can be obtained, and the present invention has been completed. That is, the present invention has the following general formula, (In the formula, R ₁ and R ₂ are a hydrogen atom or a methyl group, and R is a hydrogen atom or an alkyl group or an alkenyl group.) and vitamin E orotate ester. This is a cosmetic for preventing skin aging, which is made by blending the following into a skin cosmetic base. γ- used in the present invention, represented by the above general formula
Aminobutyric acid, N-methyl-γ-aminobutyric acid, N-
Dimethyl-γ-aminobutyric acid and their methyl esters, ethyl esters, propyl esters,
Butyl esters etc. are easily soluble in water, alcohol, etc.
Suitable for formulation into aqueous bases. In addition, γ-aminobutyric acid, N-methyl-γ-aminobutyric acid, 2-ethylhexyl ester, octyl ester, oleic ester, lauryl ester, hexadecyl ester, stearin ester, etc. of N-dimethyl-γ-aminobutyric acid are glycols,
It has a high affinity with surfactants, oils and fats, and is suitable for blending into oily bases. In the present invention, the usage amount (compounding amount) of at least one of the γ-aminobutyric acid compounds represented by the above general formula is 0.01 based on the weight of the composition (cosmetic).
~25% by weight, preferably 0.025-2.5%, most preferably 0.05-1.0%. The cosmetic of the present invention can be prepared by directly adding the γ-aminobutyric acid compound or vitamin E orotate ester of the above general formula to the base of cream, emulsion, or lotion, or by adding these compounds to the oil phase component or water phase component. , dissolved in a solvent such as alcohol and blended,
It is prepared by performing treatments such as emulsification, mixing, dispersion, dissolution, and solubilization. The above-mentioned γ-aminobutyric acid compound and vitamin E orotate compounded in cosmetics are stable and absorbed into the skin, and enhance skin function by dilating peripheral blood vessels.
It prevents skin wrinkles, makes the skin smooth and moisturized, and has excellent skin aging prevention effects (excellent for improving rough skin and keratin).
The effect of accelerating the turnover rate) can be synergistically expressed and sustained in a short period of time, resulting in remarkable effects. Examples will be described below. Note that parts shown in Examples mean parts by weight. The methods for measuring the turnover rate of the stratum corneum, the test method for measuring the effect of improving rough skin, and the test method for measuring the effect of improving the stratum corneum described in the Examples are as follows. (1) Method for measuring the turnover rate of the stratum corneum An ointment containing 5% by weight of the fluorescent dye dansyl chloride in white petrolatum is made, and the ointment is applied to the skin of the subject's forearm for 24 hours, and dansyl chloride is applied to the stratum corneum. Osmotic binding of chloride. After that, the test sample was applied to the same area twice a day (morning and evening), and the fluorescence of dansyl chloride was examined every day.
The number of days until the fluorescence disappeared was defined as the turnover rate of the skin stratum corneum. Note that the normal turnover rate of the stratum corneum of the skin is 14 to 16 days, but in aged skin, the turnover rate increases to around 18 days. On the other hand, if the anti-aging effect appears, the time will be shortened to around 12 days. (2) Test method for measuring the effect of improving rough skin The effect of continuous application for 4 weeks was investigated on 20 middle-aged and elderly subjects who had rough skin on their lower legs. Approximately 1 g of cream was applied to the test site on the left lower leg of the subject twice a day, and the condition of the skin before and after the test was evaluated according to the criteria in Table 1. No sample was applied to the right lower leg, which served as a control. Table 1 Judgment criteria for skin dryness -: Normal ±: Slight dryness, no scaling +: Slight dryness, mild scaling ++: Moderate dryness, scaling +++: Dryness, significant scaling Judgment results for test and control areas before and after the test If the skin dryness has improved by two or more levels (e.g. +→-, ++→±), it is considered "effective", if it has improved by one step, it is "slightly effective", and if there is no change, it is "ineffective". And so. It should be noted that there were no cases of skin dryness progressing during the test period. (3) Test method for measuring the effect of improving keratin (increasing the anti-peeling properties of keratinocytes) Scotch tape (Nichiban Mending Tape) was adhered to the skin of the test subject before and after the above-mentioned rough skin improvement measurement test, and it was peeled off. The condition of the keratinocytes attached to the tape was examined in detail using a scanning electron microscope, and the anti-peeling properties of skin keratinocytes were determined according to the criteria shown in Table 2, and the keratin improving effect was determined. Table 2 Judgment criteria for keratin improvement effect (increased anti-desquamation property of keratinocytes) Evaluation score 1: No scale observed 〃 2: Small scale scattered 〃 3: Small to medium scale noticeable 〃 4: Large scale noticeable When the difference between the evaluation score of the test site and that of the control site after 4 weeks of continuous application was 2 points or more, it was considered "effective," when it was 1 point, "somewhat effective," and when it was 0 points, "ineffective." There were no cases in which the evaluation score of the test site was higher than that of the control site. Example 1 (skin milk)

【table】

[Table] Components 1 to 4 of the above (Table 3) formulation were mixed uniformly with stirring, and then heated and stirred at 75° C. for 5 minutes to uniformly melt the mixture. Next, ingredients 5 to 8 and ingredient 10 are added to this molten mixture and homogeneously emulsified, and then ingredient 9 is added and cooled to room temperature to form a homogeneous oil-in-water emulsion. was prepared. For each of the obtained skin milks, the effect on improving rough skin, the effect on improving keratin, and the turnover rate of the stratum corneum were examined using the test methods described above. The results are shown in Table 4.

[Table] As is clear from the results in Table 4, skin milk No. 1 (invention) containing gamma-aminobutyric acid and vitamin E orotate ester has an effect on improving rough skin, an effect on improving keratin, and The effect of increasing the over speed is synergistically improved and manifested. On the other hand, skin milk No. 2 (comparative example) containing only γ-aminobutyric acid and skin milk No. 3 (comparative example) containing only vitamin E orotate ester showed no effect. considerably lower than the skin milk of the present invention (No. 1),
Moreover, it was only slightly better than skin milk-based skin milk No. 4 (control example). Furthermore, these skin milks (Table 3) were used by 50 subjects (women aged 25 to 45) who suffer from fine wrinkles.
The product was applied and used twice a day (morning and evening) on children for 3 consecutive months, and the results after 1 month and 3 months are shown in Table 5 below.

[Table] As is clear from the results in Table 5 above, γ-
Skin milk No. 1 (invention), which is a combination of aminobutyric acid and vitamin E orotate ester, has the effect of smoothing out wrinkles, improving texture, and reducing the feeling of moisture. It appears after one month, has remarkable rapid effect and long-lasting effect, and has excellent effects. On the other hand, skin milk No. 2 (comparative example) containing only γ-aminobutyric acid has a very low effect on smoothing wrinkles and improving texture after one month, and only slightly appears after three months. . The moisturizing feeling appears a little after one month, but it is considerably lower than the skin milk No. 1 of the present invention. Also, skin milk No. 3 containing only vitamin E orotate ester (comparative example)
After one month, there is no wrinkle smoothing effect or effect on texture, and although it appears slightly after three months, it is relatively low and has a remarkable slow effect. Furthermore, a skin milk base (base) that does not contain both γ-aminobutyric acid and vitamin E orotate ester.
In Skin Milk No. 4 (control example), almost no effect on wrinkle smoothing, texture, or moisturizing feeling was observed even after 3 months. Example 2 (Cream) After stirring the required mixture of oil phase components shown in Table 6 below and the corresponding water phase component mixture at 80°C, the water phase components were uniformly added and mixed into the oil phase component. After that, each cream (sample No. 1 to No.
8) was prepared.

[Table] Next, each of the obtained creams (No. 1 to No. 6 in Table 6)
Regarding 8), the effect on improving rough skin, the effect on improving keratin, and the turnover rate of the stratum corneum were investigated using the test method described above. The results are shown in Table 7.

【table】

[Table] As is clear from the results in Table 7, the creams of the present invention (No. 1, No.
3, No. 4, No. 5, and No. 6) are excellent in improving effects on rough skin and improving keratin, the turnover rate of the stratum corneum is extremely fast, and these effects are synergistically improved. Furthermore, 1 dose of each cream shown in Table 6 was given to 50 subjects (females aged 25 to 45) who were concerned about fine lines.
Table 8 shows the results of a practical test (panel test) when the product was applied and used twice a day (morning and evening) for three consecutive months.

[Table] As is clear from the results in Table 8, the creams of the present invention (No. 1, No.
3, No. 4, No. 5, and No. 6) are extremely superior in their wrinkle smoothing effect, texture effect, and moisturizing effect, and these effects are synergistically improved. .

Claims (1)

[Claims] 1. The following general formula (In the formula, R ₁ and R ₂ are a hydrogen atom or a methyl group, and R is a hydrogen atom or an alkyl group or an alkenyl group.) and vitamin E orotate ester. A cosmetic for preventing skin aging, which is made by blending the following into a skin cosmetic base. 2. The cosmetic according to claim 1, wherein at least one of the γ-aminobutyric acid compounds is blended in an amount of 0.01 to 25% by weight based on the weight of the composition. 3. The cosmetic according to claim 1, wherein the vitamin E orotate ester is blended in an amount of 0.01 to 25% by weight based on the weight of the composition.