JPS6229407B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a hair nourishing cosmetic containing a water-soluble salt of dehydroepiandrosterone sulfate as an active ingredient. Many drugs have been applied to treat male pattern baldness. Its mechanism of action includes combinations of drugs that promote blood circulation in the scalp, activate hair matrix cells, and suppress the secretion of lipids in the scalp, as well as combinations of amino acids and vitamins that are nutrients for hair. There are many examples. Japanese Patent Publication No. 32-7550 discloses a skin treatment agent containing a steroid compound containing dehydroepiandrosterone, but there is no description regarding the hair growth effect. Moreover, this substance hardly dissolves in an aqueous solution, and even if it is used in a hair-growth cosmetic base, it cannot exhibit its hair-growth effect. The present inventors have conducted extensive research into the application of water-soluble salts of dehydroepiandrosterone sulfate to cosmetics, and have found that when applied to human or animal skin, it exhibits a significant hair growth promoting effect. This finding led to the completion of the present invention. That is, the present invention is a hair-growth cosmetic characterized by containing a water-soluble salt of dehydroepiandrosterone sulfate. Examples of water-soluble salts of dehydroepiandrosterone sulfate used in the present invention include alkali metal salts such as sodium salts, potassium salts, and lithium salts, and basic amino acid salts such as ammonium salts, lysine salts, histidine salts, and arginine salts. Examples include salt. The amount of the water-soluble salt of dehydroepiandrosterone sulfate of the present invention is usually 0.0001 to 3.0% by weight based on the total weight of the hair-growth cosmetic product.
Preferably it is 0.001 to 1.0% by weight. The water-soluble salt of dehydroepiandrosterone sulfate of the present invention is safe for the human body and does not cause skin irritation, and the compound can be added to olive oil in an amount of 0.2 or 1% by weight.
A skin irritation test was conducted using the dispersed liquid as a sample liquid according to the Draize method described below. As a result, both the animal skin irritation score and the human skin irritation score were 0. It has been confirmed that it is non-irritating. [Draize, J.H., Association of Food and
Drug offcials of the United States Appraisal
of the Safety of Chemicals in Foods Drugs
and Cosmetics, 46 (1959), Texas State
Department of Health, Austin) The hair nourishing cosmetics of the present invention can be applied to hair tonics, hair lotions, hair creams, hair creams, etc. according to conventional methods.
It can be made into formulations such as shampoo and rinse. Examples of the base in the hair-growth cosmetic of the present invention include water, alcohols such as ethanol, polyhydric alcohols such as glycerin, liquid paraffin, higher fatty acids (stearic acid, etc.), fatty acid glycerides (glycerin monostearate, etc.) , higher alcohols, animal and vegetable oils, oily substances such as waxes, surfactants (emulsifiers, solubilizers), disinfectants,
A keratolytic agent or the like may be added as appropriate. The hair growth cosmetic of the present invention exhibits a markedly good hair growth promoting effect (hair growth effect) when applied to human or animal skin, and is stable even after long-term storage, and has extremely high commercial value. . Examples will be described below. In the examples, parts mean parts by weight, and % means weight %. Example 1 0.05 g each of sodium salt, potassium salt, lithium salt, ammonium salt, lysine salt, histidine salt, and arginine salt of dehydroepiandrosterone sulfate was added to a 50% aqueous solution of ethyl alcohol (50%
The lotion (hair-growth cosmetic) of the present invention was prepared by dissolving 499.95 g of ethanol). As a comparison, a lotion containing the same amount of water instead of the water-soluble salt of dehydroepiandrosterone sulfate was used. Next, the hair growth effect of this lotion on white mice was investigated. DDY white mouse (male, 6 weeks old, average weight 35
g) After cutting the dorsal skin from the tail with electric clippers, remove the hair completely with hair removal cream, and from the next day apply the lotion of the present invention to the skin of the subject area 2 mornings and evenings every day.
0.1 ml per animal was applied twice. A group of 10 animals
The animals in the control group were treated with a 50% alcohol aqueous solution. The hair growth effect was determined by comparing the visual evaluation score, hair length, and hair weight with the control group. Table 1 shows the criteria for determining the hair growth effect.

[Table] On the 15th day after the start of the experiment, the animals were sacrificed and evaluated visually according to the criteria shown in Table 1. The evaluation scores were totaled to determine the average evaluation score per animal. Furthermore, the skin of the subject was excised, a certain area of the skin was punched out using a punch with a diameter of 12 mm, the weight of the hair was measured after drying, and the length of 20 of the hairs was also measured.
The mean value and standard deviation were calculated. The results of this experiment are shown in Table 2. As is clear from the results in Table 2, the hair growth promoting effect of the lotion containing the water-soluble salt of dehydroepiandrosterone sulfate of the present invention on mice was remarkable, and the hair length and hair weight of all test application groups were Both values were higher than those of the control group, and the sample-applied group also showed a higher evaluation score by visual evaluation, indicating that the sample of the present invention had a hair-nourishing effect.

[Table] Salt

[Table] Sulfate Note 2 DHA: Dehydroepiandrosterone Example 2 A cream containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention was prepared according to the following formulation, and its hair growth effect was investigated. The cream contains 10 parts of liquid paraffin, 5 parts of stearic acid, 6 parts of glyceryl monostearate, 1.5 parts of triethalylamine, 77.49 parts of purified water, sodium salt, potassium salt, lithium salt, ammonium salt of dehydroepiandrosterone sulfate,
0.01 each of lysine salt, histidine salt, and arginine salt
It was prepared by a conventional method. A comparative cream was prepared by adding the same amount of water instead of the water-soluble salt of dehydroepiandrosterone sulfate in the above formulation. The results of this experiment are shown in Table 3. As is clear from the results in Table 3, the hair growth promoting effect of the cream containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention is remarkable, and both the hair length and hair weight of the sample application group are lower than that of the control group. The hair growth effect was recognized as higher than the value of , and the evaluation score was also high.

【table】

[Table] Sulfate Note 2 DHA: Dehydroepiandrosterone Example 3 The hair-growth effect of a lotion containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention was examined by applying it to the scalp of a healthy male.
The lotion consists of 70 parts of 95% ethanol, glycerin, 1 part of fragrance, 27.99 parts of purified water, and 0.01 parts of various water-soluble salts of dehydroepiandrosterone sulfate.
It was prepared by a conventional method. Comparative lotions were prepared by adding the same amount of water in place of the various water-soluble salts of dehydroepiandrosterone sulfate in the above formulation. In an evaluation experiment, the hair of the panelists at a position 5 cm above the ears was shaved in two places on the left and right with a diameter of 1 cm, and the lotions containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention were applied twice a day morning and evening.
Approximately 3 ml of the drug was applied twice to the left side and compared to the untreated right side. In addition, 10 panelists were used for each sample. The effectiveness was determined by cutting off 20 hairs from the test area on the 28th day after the start of the actual trial and measuring their lengths. The results of the experiment are shown in Table 4. The hair growth promoting effect of the lotion containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention is remarkable, and the hair length in the sample application area is more effective than the control area. There was found.

[Table] Example 4 The hair-growth effect of lotions containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention was investigated by applying them to the scalps of patients with androgenetic alopecia. The lotion was prepared in the same manner as in Example 3. In the evaluation experiment, two symmetrical hair removal areas of the panelists were shaved to a diameter of 1 cm, and the lotion containing various water-soluble salts of dehydroepiandrosterone sulfate of the present invention was applied twice daily in the morning and evening for about 30 minutes.
ml was applied only to the left side and compared with the untreated right side. In addition, 10 panelists were used for each sample. The effectiveness was determined by cutting off 20 hairs from the test area on the 28th day after the start of the actual trial and measuring their lengths. The results of the experiment are shown in Table 5. As is clear from the results in Table 5, the hair growth promoting effect of the lotion of the present invention is remarkable, and the length of the hair in the sample application area has a hair-nourishing effect compared to the control area. found.

[Table] Example 5 Sodium salt of dehydroepiandrosterone sulfate and steroid analog compounds described in JP-A-53-119862, JP-A-55-120506, and JP-A-57-99516 (see below) Regarding the compounds shown in Table 6), mouse hair growth promoting effect test,
The hair growth and hair growth effects were investigated through a human hair growth promoting effect test and a practical test. Table 6 Sample Name Example 5 Sodium salt of dehydroepiandrosterone sulfate. Comparative Example 1 A-Noru Andro Star 3(5), 16-
Dien-2-on. Comparative example 2 A-nor-androstar 3(5), 6,
16-triene-2-on. Comparative example 3 4,19-bisnol-androstar 3
(5), 16-dien-2-one. Comparative Example 4 1ξ-Methyl-A-nor-androster 3(5),16-dien-2-one. Comparative Example 5 11α-hydroxyprogesterone. Comparative Example 6 11α-acetoxyprogesterone. Comparative Example 7 4-Androstene-3-one-17-
β carboxylic acid. Experimental method and results (1) Mouse hair growth promoting effect test 0.1 g of each sample shown in Table 6 above was dissolved in 100 g of 50% alcohol to prepare a test lotion. ddY white mouse (male, 6 weeks old, average weight 35
g) After cutting the dorsal skin from the tail with electric clippers, the hair was completely removed with hair removal cream, and from the next day, each sample of Example 5 and Comparative Examples 1 to 7 was applied to the test skin twice a day in the morning and evening. 0.1 ml was applied per animal. 1
Ten animals per group were used for the samples. The hair growth effect was determined by comparing the visual evaluation score, hair length, and hair weight according to the criteria shown in Table 7 with the control group. On the 15th day after the start of the experiment, the animals were sacrificed and evaluated visually according to criteria, and the evaluation scores were totaled to determine the average evaluation score per animal.
Furthermore, after punching out the skin of the test area and drying it, the weight of the hair was measured, and the lengths of 20 of the hairs were also measured, and the average value of each hair was measured.

【table】

【table】

[Table] As shown in Table 8, the lotion of Example 5, which is a hair nourishing cosmetic of the present invention, has a remarkable hair growth promoting effect on mice compared to Comparative Examples 1 to 7, and has a significant effect on hair length, hair weight, It was found that both evaluation scores were excellent. (2) Human hair growth promotion effect test The heads of 10 test subjects who were male pattern baldness patients were shaved into a circular shape with a diameter of 1 cm at two locations on the left and right, 5 cm above the ears. Approximately 3 ml of Milsi lotion containing the samples of Example 5 or Comparative Examples 1 to 7 and having the formulation shown in Table 9 was applied to the left side twice a day in the morning and evening on the test site, and compared with the untreated right side. The effectiveness was determined by shaving 20 hairs each on the left and right test sites on the 28th day after the start of the test, and calculating the average length of the 20 hairs on the left side (where Example or Comparative Example was applied) (B ) divided by the average length (A) of 20 hairs on the right side (untreated) for evaluation. The judgment results were shown as the average value of (B)/(A) of 10 test subjects.

【table】

【table】

[Table] As is clear from the results in Table 10, the hair growth promoting effect of the milky lotion of the present invention (Example 5) is remarkable, and the value of B/A is compared to any of Comparative Examples 1 to 7. It turned out to be quite large.

Claims (1)

[Scope of Claims] 1. A hair nourishing cosmetic comprising a water-soluble salt of dehydroepiandrosterone sulfate. 2. The hair nourishing cosmetic according to claim 1, wherein the water-soluble salt of dehydroepiandrosterone sulfate is a sodium salt, potassium salt, lithium salt, ammonium salt, or basic amino acid salt. 3 The amount of water-soluble salt of dehydroepiandrosterone sulfate is 0.0001 based on the total weight of the composition.
The hair nourishing cosmetic according to claim 1, which is blended in an amount of ~3.0% by weight.