KR19990018331A - Hair growth promoting composition - Google Patents

Abstract

The present invention relates to a hair growth promoting composition containing high ginseng extract that inhibits 5 alpha-reductase as an active ingredient for promoting hair growth. The composition according to the present invention strongly inhibits the activity of 5 alpha-reductase associated with alopecia, and also has excellent bactericidal power against dandruff (Pytilosporum obale), and also in the results of animal tests and clinical trials that determine direct effects. It has a very good hair growth promoting effect.

Description

Hair growth promoting composition

The present invention relates to a hair growth promoting composition. More specifically, the present invention relates to the activity of 5-alpha-reductase related to alopecia by containing high ginseng extract that inhibits 5 alpha-reductase as a hair growth promoting active ingredient or by containing ginseng extract and a conventional hair growth promoter component. The present invention relates to a hair growth promoting composition which is excellent in animal test and clinical test results that inhibits and has excellent bactericidal power against dandruff (Pytilosporum obale) and determines the direct effect.

The human hair is about 100,000 to 150,000 pieces, each hair has a different cycle and grow and drop out through the anagen, catagen, and telogen. This cycle is repeated over three to six years, with the result that on average 50-100 hairs fall out normally. In general, alopecia refers to a shortage of hair growth in the growth phase and more hair in the degenerative or maintenance phase of these cycles, resulting in an abnormal number of hairs falling out.

The causes of hair loss have been discussed, such as hyperthermia of male hormone action, excess sebum secretion, poor circulation of blood circulation, hypoxia caused by peroxide, bacteria, genetic factors, aging, stress, and the like. However, to date, no clear cause of hair loss is known, and in recent years, a growing number of people are suffering from hair loss due to changes in diet and stress due to social conditions. It is increasing.

Conventionally, in the treatment or prevention of such alopecia, preparations mainly containing female hormones for promoting blood circulation, strengthening of hair root function, scalp moisturizing, and suppressing male hormones, preparations containing minoxidil, trichosaccharide, etc. Although it is being sold, there is a problem of side effects and there is no clear effect in terms of effects yet.

On the other hand, androgenetic alopecia is directly dependent on the amount of androgen, which is dependent on androgen hormones. Accordingly, many studies have recently been reported for the prevention and treatment of hair loss through inhibition of androgen activity. Briefly explain the mechanism of hair loss on male hormones are as follows. Testosterone, one of the male hormones, is converted to the active male hormone dihydrotestosterone by an enzyme called 5 alpha-reductase. By binding to the protein that causes hair loss, hair loss progresses. In addition, such mechanisms may produce excessive sebum, causing acne or seborrheic dermatitis, and as a result, scalp may cause inflammation and hair loss. As a result, androgenetic alopecia is due to the excessive production of dihydrotestosterone by the action of 5 alpha-reductase, and if the activity of 5 alpha-reductase is inhibited, then masculine alopecia can be prevented and treated effectively.

The inventors of the present invention selected the natural and natural materials that have the effect of preventing hair loss and hair loss against hair loss, and found that high ginseng extract strongly inhibits the activity of 5 alpha-reductase even at low concentrations and at the same time to dandruff. It has been found to have a strong antimicrobial effect, and also contains other ingredients that are mainly composed of high ginseng extract and conventionally formulated to hair growth promoters in Korea or Japan, for example, pepper tink, tocopherol acetate, benzyl nicotinate, hair roots for promoting blood circulation. In case of using with medicinal extract, ginseng extract, red ginseng extract, oyster extract, cloves extract, hinokithiol, nicotinic acid amide, el-menthol, pyrotonolamine for sterilization or keratin dissolution, silicic acid and other moisturizers It turns out that the effect is even higher.

The present invention relates to a hair growth promoting composition characterized by inhibiting 5 alpha-reductase as an active ingredient and containing 0.001 to 10% by weight of high ginseng extract.

Although the wool or hair growth agent using the high ginseng extract is introduced in several patent literatures, (1) exemplifies the high ginseng extract as one ingredient that can be used together with urea as the main ingredient (Japanese Patent Laid-Open No. 7-267830). (2) discloses the effect of wool by simple combination of various plant extracts such as ginseng extract (Japanese Patent Laid-Open No. 7-277930), but there is no mention of their mechanism of action, and (3) Although ginseng extract is used as one of the ingredients (Japanese Patent Laid-Open No. 5-58851), there is no technical proof regarding the mechanism of action of the ginseng extract.

The hair growth promoting composition of the present invention has a clear mechanism of action of the high ginseng extract inhibiting the activity of 5 alpha-reductase and exhibits the effect of preventing wool and hair loss, and at the same time, it has an excellent therapeutic effect against dandruff itching, which is one of the scalp diseases. This invention is a step further than the prior art in that it was found.

General properties, applications and confirmation test method for the ginseng used in the present invention is as follows. The scientific name is Sophora flavescens or Sophora angustifolia, and the herbal name is Sophora radix, which uses the root as a herbal medicine. The ginseng has the shape of columnar or conical root, 5 ~ 20㎝ long, 2 ~ 3㎝ diameter, the outer surface is dark brown to yellow brown, and the vertical wrinkles are clear, and the skin is peeled off and yellowish white and fibrous. It also has a unique nausea, smells bitter and has a residual. Alkaloids are the most representative of the main components, such as matrine (matrine), oxymatrine (oxymatrine), sophoranol (sophoranol), and the flavonoids (flavonoids) such as curaridin (kuraridin), iso-hydrokaritin ( isoanhydroicaritin). The leaves also contain luteolin-7-glucose and the seeds contain cytisine.

The use of ginseng is used as a high-density stomach agent, peripheral vasoconstrictor, antipyretic analgesic, and parasitic parasite. Toxicity is 0.4g / kg, so avoid large doses (Ref. 194-196, 1994). As a confirmation test, 0.5 g of red ginseng extract is added with 10 ml of water, boiled, filtered, and 2 ml of mayer reagent is dropped into 2 ml of the filtrate, yellow precipitates are formed (refer to alkaloids such as martrin). Test, Korean Pharmacopoeia VI).

<Preparation of Ginseng Extract>

Referring to the extraction method of ginseng used in the present invention is as follows. First, the ginseng root was purified and powdered and cooled for 5 days in about 10 times the amount of the extraction solvent, and then the extract powder was dried, and the dried powder of the ginseng extract was obtained by filtration, concentration, and freeze drying.

The extraction solvent used at this time is one or two of purified water, methanol, ethanol, propanol, butanol, glycerol, propylene glycol, 1,3-butylene glycol, methyl acetate, ethyl acetate, benzene, hexane, diethyl ether, dichloromethane It is preferable to mix and use the above solvent for extraction.

<Evaluation of 5 Alpha-reductase Activity Inhibitory Activity of Ginseng Extract>

5-alpha-reductase activity was used in the 5-alpha-reductase activity inhibition experiments in rat liver (adult, Sprague-Dawley, male rat (8-10weeks old), liver), and the amount of protein was determined by protein quantification. A protein suspension was prepared. In addition, an enzyme reaction solution was prepared in a general manner. Radiolabeled testosterone ( ³ Htestosterone) was used as a substrate of 5 alpha-reductase, and the enzyme reaction solution: protein suspension: high ginseng extract = 70: 20: 10 in a thermostat at a ratio of 2 minutes. After reacting in an incubator, the reaction solvent was blown out, the remaining material was dissolved in a developing solvent, developed on a thin layer chromatogram (TLC), and the conversion rate of the developed testosterone was measured, and the result was measured as a control (high ginseng extract). 5 alpha-reductase inhibition rate was evaluated as compared to the conversion rate without addition). The inhibition rate calculation method is as follows.

% Inhibition = [(A-B) / A] x 100

A = conversion of testosterone to dihydrotestosterone (without extract)

B = conversion of testosterone to dihydrotestosterone (extract added)

Experimental results by the above inhibition rate calculation method are as follows.

<Evaluation of Antimicrobial Activity against Dandruff Bacteria (Pytirosporum ovale) of Ginseng Extracts>

The antimicrobial activity of the extract obtained by the above method was determined by adding a ginseng extract of a certain concentration to the pytirosporum obale cultured in a liquid medium, followed by culturing in an anaerobic culture tank, and then inhibiting the growth of the pytirosporum obale. MIC) was obtained, and as a result, the minimum inhibitory concentration (MIC) range for Pytylosporum obare of ginseng extract by each extraction solvent was estimated to be 10 to 100 ppm.

The content of ginseng extract in the hair growth promoting composition of the present invention is 0.001 to 10% by weight is suitable. If the amount is less than 0.001% by weight, the effect cannot be sufficiently exhibited. At 10% by weight or more, the effect is not proportional to dose and it is difficult to maintain the formulation. In addition, ingredients blended with conventional hair growth promoters, such as hinokithiol, red pepper tincture, ginseng extract, red ginseng extract, oyster extract, sugar extract, cloves extract, tocopherol acetate, nicotinic acid amide, nicotinic acid benzyl, pyroxtonolamine, salicylic acid, L-menthol and the like do not limit the concentration of the active ingredient in the range that can maintain the formulation without disturbing the effect, but in consideration of human safety or formulation stability, preferably hinokthiol, pyroxtone amine 0.001 ~ 1.0 Weight%, red pepper tincture, ginseng extract, red ginseng extract, oyster extract, sugar extract, cloves extract, 0.001-10% by weight of tocopherol acetate, 0.01-10% by weight of nicotinic acid amide, 0.001-0.1% by weight of nicotinic acid, salicylic acid And el-menthol is appropriately 0.01 to 1.0% by weight. The composition according to the present invention includes all formulations that can be applied to the scalp, such as shampoos, hair conditioners, hair lotions, liquid wool types, and also aerosol types of these formulations.

The composition prepared by the above method was prepared as a liquid wool agent, and showed a good effect in the 5 alpha-reductase inhibition test and the bactericidal power test against dandruff, and the test using the C57BL / 6 mouse, the hair growth evaluation test animal. And in a clinical trial against alopecia, it was evaluated that the hair growth promoting effect was excellent without any side effects such as skin redness.

Hereinafter, although an Example and a comparative example demonstrate this invention, the technical scope of this invention is not limited to these Examples.

Preparation and Effect Evaluation Test of Wool Ginseng Extract Containing High Ginseng Extract

Using a high ginseng extract and other auxiliary components according to the present invention to prepare a liquid wool agent in the composition ratio shown in Table 1-1.

Table 1-1

5-alpha-reductase activity inhibitory evaluation test

In order to evaluate the inhibitory activity against 5-alpha-reductase of the wool composition prepared in Examples and Comparative Examples, 5-alpha-reductase activity inhibitory power was evaluated by the method described above. The calculation method of inhibition rate evaluation is as follows.

% Inhibition = [(A-B) / A] x 100

A = conversion of testosterone to dihydrotestosterone (40 wt% aqueous ethanol solution)

B = conversion of testosterone to dihydrotestosterone (each example and comparative example)

5 alpha-reductase activity inhibitory effect is judged to be effective only when 80% or more result.

The activity inhibitory test results of the 5-alpha-reductase are shown in Table 1-2 below.

TABLE 1-2

As described above, the compositions of Examples 1 to 5 containing high ginseng extract showed a significantly higher inhibitory activity of 5 alpha-reductase activity compared to Comparative Examples 1 to 2.

Test of bactericidal power against Dandruff (Pytilosporum obale)

Minimal microbial inhibitor concentration (MIC, Minimal Ingibitory) was added to the liquid medium of Examples and Comparative Examples in 5.0%, 1.0%, 0.1%, 0.01%, respectively, and incubated for 3-4 days by inoculation with pytirosporum obale. Concentration) was measured.

Table 1-3

As described above, the bactericidal power of 10 times or more was shown against dandruff bacteria than Comparative Examples 1 and 2 including other bactericides such as pyrotonolamine and salicylic acid.

Hair growth promoting effect test using animal

Hair growth promoting effect test was used to remove the hair of the back area using 42 ~ 56 days old mice (C57BL / 6, male) and once a day, 100 times in each dorsal area for each of the above Examples and Comparative Examples Microcroliters were applied for 28 days.

The results were compared by calculating the ratio of the area where the newborn hair was grown with respect to the area from which hair was removed using an image analyzer, and it was determined that the hair growth promoting effect was greater than 70%.

Table 1-4

As described above, the compositions of Examples 1 to 5 containing high ginseng extract showed two times higher hair growth promoting effect than the compositions of Comparative Examples 1 and 2 and did not include other auxiliary components. It showed a higher effect than the case.

Hair growth promoting effect clinical trial

In order to confirm the excellent activity inhibitory effect of 5 alpha-reductase of Ginseng and the hair growth promoting effect shown in the animal test, the subjects with alopecia were selected and tested for clinical effects.

In order to measure the clinical effect of hair growth promotion using Example 4 containing the ginseng extract and Comparative Example 1 containing no ginseng extract, a person with alopecia of adult male hair loss from 30 to 50 years old or more than 100 Ten people were tested.

The method of use was to apply water droplets (about 2ml) 2 ~ 3 times a day to the hair loss site and used for at least 1 month up to 3 months depending on the degree of effect checking.

To determine the effect, the average daily hair loss, triage findings, and improvement of subjective symptom improvement were evaluated in five stages according to the following evaluation scale, and overall improvement was taken as the average of the evaluation scale. The final judgment was that the overall improvement was more than 3.0 points, and the results are shown in Table 1-5 below.

Table 1-5

As described above, Example 4 containing the high ginseng extract showed a marked improvement compared to Comparative Example 1, and it was found that no side effects were found in all subjects during the use period, and thus, the composition was safe for human body.

The hair growth promoting effect of the wool agent was shown to inhibit the activity of 5 alpha-reductase strongly than that of the comparative example containing the ginseng extract, and also showed excellent bactericidal power against dandruff bacteria In addition, animal studies and clinical trials that determine direct effects have been shown to have very good hair growth promoting effects.

Preparation and Effect Evaluation Test of Shampoo Compositions Containing High Ginseng Extract

The ginseng extract according to the present invention and other auxiliary ingredients and ingredients for preparing the function and formulation of the shampoo, etc. were prepared by the conventional shampoo manufacturing method with the composition ratio shown in the following Table 2-1.

TABLE 2-1

5-alpha-reductase activity inhibition test

In order to evaluate the activity inhibitory activity of 5-alpha-reductase of the sampu compositions prepared in Examples and Comparative Examples, the inhibition of 5-alpha-reductase activity was evaluated by the method described above. The inhibition rate calculation method is as follows.

% Inhibition = [A-B) / A] x 100

A = conversion of testosterone to dihydrotestosterone

(4% aqueous solution of POE lauryl sulfate solution (30%))

B = conversion of testosterone to dihydrotestosterone

(10% aqueous solution of each Example and Comparative Example)

5 alpha-reductase activity inhibitory effect is judged to be effective only when 80% or more result.

The activity inhibitory test results of the 5 alpha-reductase are shown in Table 2-2.

Table 2-2

As described above, the compositions of Examples 6 to 10 containing high ginseng extract showed a significantly higher inhibitory activity of 5 alpha-reductase activity compared to the compositions of Comparative Examples 3 to 4.

Test of bactericidal power against Dandruff (Pytilosporum obale)

The shampoos of Examples and Comparative Examples were added to the liquid medium at 5.0%, 1.0%, and 0.01%, respectively, and inoculated with phytirosporum obale, followed by incubation for 3 to 4 days, followed by minimal microbial inhibitory concentration (MIC). Measured.

TABLE 2-3

As described above, the bactericidal power of 10 times or more was exhibited against the dandruff bacteria than Comparative Examples 3 and 4 including other fungicides such as pyrotonolamine and salicylic acid.

Animal hair growth promoting effect test

Hair growth promoting effect test using 42 to 56 days old mice (C57BL / 6, male) to remove the hair on the back area and 10 times each day for each of the dorsal area for each of the above Examples and Comparative Examples, 100 microliters was applied and a rinse with purified water using a brush was performed for 28 days.

As a result, the ratio of the area where the newborn hair was grown was compared to the area from which hair was removed using an image analyzer, and it was judged that the hair growth promoting effect was more than 70%.

Table 2-4

As described above, the compositions of Examples 6 to 10 containing high ginseng extract showed a significantly higher hair growth promoting effect compared to Comparative Examples 3 to 4, and the other components contained higher than that of the other components. The effect was shown.

Hair growth promoting effect clinical trial

In order to confirm the superior activity inhibitory effect of ginseng 5 alpha-reductase confirmed in the above experiment and the hair growth promoting effect shown in the animal test, the subjects with alopecia were selected and tested.

In order to measure the clinical effect on hair growth promotion using Example 9 containing high ginseng extract and Comparative Example 3 containing no ginseng extract, the adult male and female hair loss from 30 to 50 years old or the average daily hair loss is 100 or more. Ten people were tested.

The method of use was used as a shampoo of Example 9 and Comparative Example 3 once every three to three times, depending on the degree of effect checking used for at least 1 month to a maximum of 3 months, the use of more than that was not effective .

The determination of the effect was evaluated in five stages according to the following evaluation scales, and the average daily hair loss, visual judgment findings, and degree of improvement of subjective symptoms were triturated according to the following evaluation scale. The final judgment was that the overall improvement was valid above 3.0 and the results are shown in Table 2-5 below.

Table 2-5

From the above results, Example 9 containing the high ginseng extract showed a marked improvement compared to Comparative Example 3, it was found that no adverse effects were found in all subjects during the period of use, which is a safe composition for the human body.

In the shampoo, the content of high ginseng extract is shown to promote hair growth at a higher concentration than that of the wool agent, which is believed to be due to the dilution of the active ingredient because it is a rinsing product. It was shown that the Example containing the ginseng extract strongly inhibited the activity of 5 alpha-reductase than that of the Comparative Example which did not contain it, and the bactericidal power against dandruff was also shown to be turbid and the animal test to determine the direct effect And clinical trials also showed a very good hair growth promoting effect.

Preparation and Effect Evaluation Test of Hair Conditioner Composition Containing Ginseng Extract

Using the high ginseng extract according to the present invention and other auxiliary ingredients and ingredients for preparing the function and formulation of the hair conditioner, the composition ratio was prepared by the conventional hair conditioner manufacturing method as shown in Table 3-1.

Table 3-1

5-alpha-reductase activity inhibitory evaluation test

In order to evaluate the inhibitory activity against 5-alpha-reductase of the hair conditioner compositions prepared in Examples and Comparative Examples, the inhibitory activity of 5-alpha-reductase activity was evaluated by the method described above. The inhibition rate calculation method is as follows.

% Inhibition = [(A-B) / A] x 100

A = conversion of dihydrotestosterone to testosterone

(0.8% aqueous solution of stearyl methylbenzyl ammonium chloride (25%))

B = conversion rate of testosterone to dihydrotestosterone

(10% aqueous solution of each Example and Comparative Example)

5 alpha-reductase activity inhibitory effect is judged to be effective only when 80% or more result.

The activity inhibitory test results of the 5-alpha-reductase are shown in Table 3-2.

Table 3-2

As described above, the compositions of Examples 11 to 15 containing high ginseng extract showed a significantly higher inhibitory activity of 5 alpha-reductase activity compared to Comparative Examples 5 to 6.

Test of bactericidal power against Dandruff (Pytilosporum obale)

The hair conditioner of Example and Comparative Example was added to the liquid medium at 5.0%, 1.0%, 0.1%, and 0.01%, respectively, and inoculated with phytirosporum obale, followed by incubation for 3 to 4 days, followed by minimum microbial inhibitory concentration (MIC, Minimal). Ingibitory Concentration) was measured.

Table 3-3

As described above, the bactericidal power of 10 times or more was exhibited against the dandruff bacteria than Comparative Examples 3 and 4 including other fungicides such as pyrotonolamine and salicylic acid.

Animal hair growth promoting effect test

Hair growth promoting effect test using 42 to 56 days old mice (C57BL / 6, male) to remove the hair on the back area and 10 times each day for each of the dorsal area for each of the above Examples and Comparative Examples, 100 microliters was applied and a rinse with purified water using a brush was performed for 28 days.

The results were compared by calculating the ratio of the area in which the newborn hair was grown with respect to the area from which hair was removed using an image analyzer, and it was judged that the hair growth promoting effect was more than 70%.

Table 3-4

As described above, the compositions of Examples 11 to 15 containing high ginseng extract showed a significantly higher hair growth promoting effect compared to Comparative Examples 5 to 6, and the other components contained higher than that of the other components. The effect was shown.

Hair growth promoting effect clinical trial

In order to confirm the superior activity inhibitory effect of ginseng 5 alpha-reductase confirmed in the above experiment and the hair growth promoting effect shown in the animal test, the subjects with alopecia were selected and tested.

In order to measure the clinical effect on hair growth promotion using Example 14 containing high ginseng extract and Comparative Example 5 containing no ginseng extract, a person with alopecia of adult male hair loss from 30 to 50 years old or more than 100 Ten people were tested.

The method of use is to wash the hair with a normal shampoo once every 1 to 3 days, and then use the hair conditioner of Example 14 and Comparative Example 5 in the usual way, depending on the degree of effect confirmation, from at least 1 month up to 3 months. The use was further ineffective.

The determination of the effect was evaluated in five stages according to the following evaluation scales, and the average daily hair loss, visual judgment findings, and degree of improvement in subjective symptoms were evaluated. The final judgment was that the overall improvement was valid above 3.0. The results are shown in Table 3-5 below.

Table 3-5

As described above, Example 14 oil containing high ginseng extract showed a remarkable improvement compared to Comparative Example 5, and it was found that no side effects were found in all subjects during the use period, and thus, the composition was safe for human body.

The hair conditioner shows a hair growth promoting effect at a higher concentration of the ginseng extract than that of the wool agent, which is judged to be the same reason as in the case of the shampoo, even though the hair growth promoting effect is not contained in the embodiment containing the ginseng extract. It showed stronger inhibition of 5-alpha-reductase activity than that of the comparative example. The bactericidal power against dandruff was also shown to be turbid. Appeared to be.

Claims (3)

Hair growth promoter composition characterized by containing 0.001 to 10% by weight of high ginseng extract that inhibits 5 alpha-reductase A hair growth accelerator composition comprising high ginseng extract as an active ingredient together with a conventional hair growth promoter auxiliary component. According to claim 2, the conventional hair growth promoter auxiliary ingredients are hinokithiol, pepper tink, ginseng extract, red ginseng extract, oyster extract, sugar extract, clove extract, tocopherol acetate, nicotinic acid amide, nicotinic acid benzyl, pyroxtonolamine, salicylic acid and Hair growth promoter composition, characterized in that one or two or more selected from L-menthol.