KR20120136519A - A composition for promoting hair growth comprising alpha-hydroxy acid - Google Patents

Abstract

PURPOSE: An agent containing alpha-hydroxy acid(AHA) compounds with glycolic acid is provided to promote hair growth. CONSTITUTION: A composition for promoting hair growth contains 10 to 10^-12 M glycolic acid as an active ingredient. The composition for promoting hair growth contains 10 to 10^-12M lactic acid and 5 to 10^-12M trichloroacetic acid as active ingredients. A method for promoting hair growth comprises a step of treating a local part of human body with glycolic acid 4 days or more a week. A hair growing agent contains glycolic acid, lactic acid, or trichloroacetylic acid as an active ingredient.

Description

Hair growth promoting composition comprising alpha hydroxy acid as an active ingredient {A COMPOSITION FOR PROMOTING HAIR GROWTH COMPRISING ALPHA-HYDROXY ACID}

The present invention relates to a hair growth promoter comprising compounds known as alpha-hydroxy acid (aka AHA) containing glycolic acid as an active ingredient.

In general, when looking at the structure of the hair, the hair follicle looks like a stem growing from the bulb of the plant. This bulbous part is called hair follicles. At the bottom center of the hairball, there is a dermal papilla, where capillaries form a web. The area surrounding the breast nipple is called mosquito matrix (毛 基質). Mosquito matrix is composed of mosquito matrix cells and melanocytes and is very active in cell division, corresponding to the hair production plant. Differentiate from the mosquito matrix and migrate to the surface of the skin. The innermost part of this keratinized structure is hair (hair shafts).

This hair is composed of three parts from the center to the outer part of the hair, hair, and hair. In addition, this hair is surrounded by a sheath (hair root herb: inner hair root herb (+ 毛 根 墅) + outer hair root herb (外側 毛 根 墅)). There are melanocytes between the mosquito-cells in the hair follicles, and the melanin produced by the melanocytes is later devoured by the hair-forming cells to determine the color of the hair according to the amount of melanin.

In addition, 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, telogen. This cycle is repeated over three to six years, with the result that on average 50 to 100 hairs fall out normally. In general, alopecia refers to an increase in the number of abnormal hair loss due to shortening of hair growth rate in the growing period and increased number of hair in the retrogressive or resting period among these cycles. The causes of alopecia have been discussed, such as poor blood circulation, excessive male hormone action, excessive sebum secretion, peroxide, bacterial deterioration of the scalp function, genetic factors, aging, stress.

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 caused by social conditions. It is increasing.

Alopecia is classified into congenital alopecia and acquired alopecia. Congenital alopecia refers to the absence of hair from birth, and acquired alopecia refers to the loss of hair as it ages. In particular, alopecia areata can not be found in non-cancerous alopecia and skin lesions, but can be classified into alopecia in pathological skin and scar alopecia.

It can also be classified as androgenetic alopecia, alopecia areata and other alopecia. About 50 to 100 hairs fall a day. Male hair loss is a symptom of a naturally reduced number of hairs that do not regenerate after being lost. This is often referred to as adult or mild alopecia. Most people who complain of alopecia are included in this type. This symptom is usually characterized after 25 years of age, but has recently been noticeably increasing in men around the age of 20. There are many cases of male alopecia, such as a rounded off from the parietal side, an M-shaped prominent head on both sides of the forehead, and a U-shaped forehead.

The most common cause of male alopecia is genetic factors, as it is currently known. However, not all genes are expressed, and the factor involved in gene expression is also male hormones. In other words, due to the effects of male hormones, men have more baldness than women, and do not become bald before puberty, and there is no baldness to those who castrated before puberty. In addition, there are the following theories as several causes. The cause of androgenetic alopecia is the hormonal theory that it comes from an imbalance between male and female hormones. In other words, the increase in the male hormone inhibiting the growth of the hair in the crown at the forehead, indicating this result. There are different theories according to race, but the ratio of hair loss varies according to race. The reason for this is not yet clear, but statistically, Korea has a very low probability of hair loss compared to whites and blacks. But male alopecia is more common in developed countries than in less developed countries. In fact, there are reports that alopecia is not found in primitive peoples and in very few cases in developing countries.

Alopecia areata is a phenomenon in which hair falls out in a circle. This alopecia areata may be confused with alopecia areata or feminine alopecia, but the cause and the size of the hair fall out are also completely different.

Male alopecia is a physiological phenomenon, whereas alopecia areata is classified as pathological. The onset of hair loss usually starts at about 2 to 3 cm in diameter, and increases gradually in number and size as it progresses. Then the whole head may eventually be hair loss. In particular, alopecia areata is also called alopecia areata because it is difficult to treat hair loss phenomenon appearing on the back or side of the head. In alopecia areata, the prevalence rate is below 75% and is more than 75%, and it is a phenomenon that can appear in anyone without differences in race or ethnicity as well as between men and women. Alopecia areata has a different name depending on the extent of hair loss. The widening range is called malignant alopecia areata, and malignant hair loss progresses further and all of the hair falls out. Frontal alopecia and all hair falling out of the body are called general alopecia. There are many theories about the cause of alopecia areata, but there is no clear orthodoxy. At first, parasitic emergence was suggested, followed by fungal and then bacteria. Since the early 1900s, psychological and neurological causes of alopecia areata have been developed. Recently, it is known as an autoimmune disease.

In addition to the alopecia areata and alopecia areata, hair loss due to endocrine abnormalities, nutritional disorders, hair loss due to metabolic disorders, medications, and inflammation, infection tumors and other pollution, hair loss such as stride are very diverse.

On the other hand, hair growth consists of a complex interaction between epithelial cells and dermal cells of hair follicles, and according to their interactions, the cycle of active growth, anagen, catagen, and resting telogen Circulate The core of hair growth is the dermal papilla (DP) of hair follicles, which circulate into growth or degeneration by releasing hair growth or inhibitory factors into the hair matrix cells surrounding them.

To date, there are two hair growth specialties approved by the US Food and Drug Administration, Finasteride (Propecia from MSD) and Minoxidil (Pfizer's Rogaine). Finasteride is a drug developed to treat prostatic hypertrophy and has the effect of inhibiting the function of 5-alpha-reductase, which produces male hormone DHT, which has the effect of treating male hair loss and causes hair loss. Minoxidil, on the other hand, was originally a drug that regulates hypertension due to vasorelaxation, but it was developed as a hair regrowth agent by observing hair growth up to 24 in patients taking it. There are few side effects, but the maximum effect should be applied twice a day or more than six months, and stop using the effect. It has been shown to be effective in proliferating hair epithelial cells and stimulating growth phase induction at rest in animal models.

The mechanism of action is not fully elucidated, but is explained by growth factor-related and hemolytic effects. However, 20-30% of patients appear to be unresponsive to these two drugs, and the side effects are severe. Therefore, there is a need to develop new therapies that prevent hair loss and induce hair growth, that is, these mechanisms and other compensatory substances.

Targets of hair growth products are developed to promote hair growth, improve blood circulation, resolve nutritional deficiencies, alleviate scalp inflammation, and inhibit 5-alpha-reductase function.Anti-androgenic and non-androgen drugs Natural substances and substances that produce synergistic effects with already developed drugs are also being explored.

The present invention solves the above problems and the object of the present invention is to provide a new hair growth promoter.

In order to achieve the above object, the present invention provides a composition for promoting hair growth, comprising glycolic acid as an active ingredient.

In one embodiment of the present invention, the concentration of glycolic acid (glycolic acid) is preferably 10 ^-1 ~ 10 ^-6 M, but is not limited thereto.

The present invention also provides a composition for promoting hair growth using lactic acid as an active ingredient.

In one embodiment of the present invention, the concentration of lactic acid is preferably 10 ^-1 ~ 10 ^-6 M, but is not limited thereto.

In another aspect, the present invention provides a composition for promoting hair growth using trichloroacetic acid as an active ingredient.

In one embodiment of the present invention, the concentration of trichloroacetic acid is preferably 10 ^-1 to 10 ^-8 M, but is not limited thereto.

In another aspect, the present invention provides a method for promoting hair growth, comprising the step of treating glycolic acid (glycolic acid) to the local site of the human body for 4 days or more.

In another aspect, the present invention provides a method for promoting hair growth, comprising the step of treating lactic acid to a local part of the human body for 4 days or more.

In another aspect, the present invention provides a method for promoting hair growth comprising the step of treating trichloroacetic acid to a local site of the human body for 4 days or more.

On the other hand, the composition of the present invention may further contain auxiliary components in addition to the active compound of the present invention. Auxiliary ingredients include vitamins, minerals, blood circulation improvers, scalp penetrants, skin irritants and / or moisturizers.

First, vitamins such as vitamins B1, B2, B6, B12, C, calcium pantothenate, nicotinic acid amide, folic acid and biotin, and minerals such as zinc, iron, calcium, and magnesium may be added. The use of such vitamins and minerals is preferred because it can enhance the bioactive effect. In this case, the vitamins and minerals are preferably contained in an amount of 0.01 to 10% by weight based on the total weight of the final composition, and in particular, vitamins B1, B2 and C are 0.01 to 3% by weight and 0.01 to 3% by weight, respectively, based on the total weight of the final composition. And 0.01 to 4% by weight.

Blood circulation improving agent is added to enhance blood circulation and to enhance the biological activity effect, gamma or alpha linoleic acid, oleic acid, EPA, tocopherol and the like can be used. At this time, the blood circulation improving agent is preferably included in 0.1 to 10% by weight relative to the total weight of the final composition.

Scalp penetration agents use dimethyl sulfoxide (DMSO), Triton-X, various surfactants or povidones, and are used to enhance the penetration of pharmaceutical components into the dermal layer deep into the scalp. In particular, the addition of menthol, a skin stimulant, increases skin irritation, which further enhances the effect of the pharmaceutical ingredient on the dermal layer of the skin. At this time, the scalp penetration agents such as dimethyl sulfoxide, triton-X, and povidone are each contained in an amount of 1 to 20% by weight based on the total weight of the final composition, and skin irritants such as menthol are preferably included in an amount of 1 to 5% by weight of the total weight of the final composition. In particular, when dimethyl sulfoxide, Triton-X and povidone, which are scalp penetrants, are used separately, 1.0 to 20% by weight of dimethyl sulfoxide, 1.0 to 10.0% by weight of Triton-X and 1.0 to povidone, based on the total weight of the final composition. It is preferably included in the 5.0 wt%. In particular, the old scalp layer, such as baldness is difficult to penetrate the usual active ingredients, many kinds of hair growth, hair growth agent is also a major cause that does not exhibit its efficacy. Among them, dimethyl sulfoxide (DMSO) is preferable as a scalp penetrant, and DMSO is a low molecular compound, which has a property of passing through a biological membrane well and increasing cell membrane permeability of other substances. DMSO also has an antioxidant action that removes hydroxy radicals (OH '). DMSO has the advantage of dissolving water, alcohol and almost all organic and biochemicals, and is widely used as a solvent for biopolymers in nuclear magnetic resonance analyzers. The mechanism by which DMSO helps infiltrate the scalp has not been elucidated, but it is believed to be due to the ability to instantly dissolve polymers such as proteins with excellent dissolving power.

Moisturizers are added to increase the moisturizing effect of the final composition to enhance the sustainability of the drug, with glycerin being preferred and added at 0.5 to 5% by weight relative to the total weight of the final composition.

Meanwhile, the hair growth promoting composition of the present invention may be used directly with the compounds of the present invention, but is preferably processed and prepared with a pharmaceutically acceptable carrier according to a pharmaceutical preparation method known in the art. Examples of such carriers include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, Polyvinylpyrrolidone, water, methyl hydroxybenzoate, propyl hydroxybenzoate, talc, magnesium stearate and mineral oil. In addition, the hair growth promoting composition of the present invention may further comprise a filler, anti-coagulant, lubricant, wetting agent, fragrance, emulsifier or preservative.

Hair growth promoters according to the present invention may be formulated using methods well known in the art to provide rapid, sustained or delayed release of the active ingredient after administration. The formulations may be in the form of tablets, pills, granules, powders, sachets, elixirs, suspensions, emulsions, solutions, syrups, aerosols, soft or hard gelatin capsules, sterile injectable solutions, sterile powders and the like. When prepared in the form of granules, liquids, etc. to enhance the taste, natural flavors such as plum, lemon, pineapple or herb, or natural pigments such as fruit juice, chlorphyllin and sweeteners such as fructose, honey, Sugar alcohols, sugars and the like can be mixed with an acidulant such as citric acid and sodium citrate.

In addition, the hair growth promoting composition according to the present invention can be administered through a variety of routes including scalp application, oral, etc., it is most preferred to use a method for administering the scalp application.

The daily scalp application amount of the final composition used as the hair growth promoter according to the present invention is in the range of 1 g to 100 g. However, the actual application amount should be determined in consideration of various related factors such as the application method, the age, sex, weight of the patient and the severity of the patient, and the application amount is not intended to limit the scope of the present invention in any aspect.

Hereinafter, the present invention will be described.

The present invention intends to use AHAs, including glycolic acid, to stimulate hair follicle epithelial cells and dermal cells to promote their proliferation and, as a result, hair follicle reconstruction and regeneration. The proven hair growth control screening method was used to evaluate the potential of hair loss treatment agents. First, experiments using animals and culture experiments using human hair follicle tissues were conducted to investigate their hair growth effects. In animal experiments, the growth effect was observed, and human hair follicle culture screening method was found to require careful interpretation between experiments due to the large variation of the properties of the original hair.

Glycolic acid (glycolic acid) at a very small concentration of the hair growth effect of converting the rest of the hair to the growth phase has been proved to use it as an active ingredient of the hair regrowth agent.

After application, hair keratinocyte proliferation was greatly increased and the size of dermal papilla cells and dermal papilla was also increased. This effect was also observed in trichloroacetic acid, salicylic acid, and lactic acid.

Hereinafter, the present invention will be described in detail.

C57BL6  Screening of Hair Growth Effects Using Animals

After shaving the hair on the rat's back with an electric razor, 1M of various AHA substances were applied four times in the first week only, which clearly induced hair growth from the resting phase to the growth phase compared to the control group and the unapplied area (Fig. 2).

Among them, in the concentration-specific treatment of glycolic acid, a certain hair growth effect was observed even after application using a cotton swab of 200ul per day on the first day of the experiment at a concentration of 0.5M or more (FIG. 3).

Validation Using Human Hair Follicle Tissue Culture .

In the human hair follicles, different concentrations of GA (10 ^-2 to 10 ^-10 ) were added and measured at 4 and 7 days of length, showing toxicity at 10 ^-2 , and at 10 ^-4 to 10 ^-8 M than the control. It showed a slightly superior effect, ^10-10 M showed a certain hair follicle growth compared to the control (Fig. 4).

In the same manner, the experiment was carried out at a concentration of 10 ⁻⁸ to 10 ⁻¹² M, and showed the highest hair growth at 10 ⁻¹⁰ M (FIG. 5).

As can be seen through the present invention, the alpha hydroxy acids including glycolic acid of the present invention exhibit hair growth effects and thus can be used as hair growth promoters.

1 is a diagram showing the structure of glycolic acid.
Figure 2 is a picture showing the hair growth effect of GA, LA and TCA using C57BL / 6, 200ul four times a week to apply the drug of GA, LA and TCA 1M dissolved in Q-water in hairy shaved animals 4 The results of weekly observations are shown (GA is glycolic acid; LA is lactic acid; TCA is trichloroacetic acid).
Figure 3 is a photograph showing the hair growth effect according to the concentration of GA using C57BL / 6, and shows the results obtained by applying 200ul of the drug once dissolved in Q-water in hairs shaved animals, etc. once per 200 weeks.
Figure 4 is a graph showing the hair growth effect of GA using human hair follicle tissue culture, measuring the length of 4 and 7 days after the growth of put different GA (10 ^-2 ~ 10 ^-10 M) in human hair follicle tissue .
Figure 5 is a graph showing the hair growth effect of GA using human hair follicle tissue culture,
Human hair follicle tissue with different concentrations of GA (10 ^-8 ~ 10 ^-12 M) was added to measure the length of the 5, 7, 9, 12 days.

The present invention will now be described in more detail by way of non-limiting examples. The following examples are intended to illustrate the invention and the scope of the invention is not to be construed as being limited by the following examples.

Example  1: Hair growth search using animal experiment

For the experiment, C57BL / 6, female, 6 weeks old (Oriental Bio, Gyeonggi-do) were purchased and stabilized for 3-4 days. Anesthesia was performed with Forane and the hair was removed using an electric razor. After 1 ~ 2 days, 200ul of 1M GA, LA and TCA of the corresponding drugs were applied (topical application), observed for 4 weeks, and photographed for comparison.

Example  2: Human hair follicle  Hair Growth Search Using Tissue Culture

The hair follicle to be used for tissue culture was first cut out and tissues surrounding the hair follicles were cleaned to prevent contamination with fibroblasts, the dermal cells of the skin.

Organized hair follicles were cut out of epidermis and sebaceous gland for maximum growth, and 8-10 follicles were added for each experimental condition, and cultured in William E media (W 412H, Sigma, St. Louis, MO, USA). Filar micrometer eyepieces (American Opical, NY, USA) were used to measure hair follicle length every 2-3 days and cultures were replaced.

Claims (15)

Hair growth promoting composition comprising a glycolic acid (glycolic acid) as an active ingredient. According to claim 1, wherein the glycolic acid (glycolic acid) concentration of the hair growth promoting composition, characterized in that 10 ~ 10 ^-12 M. A composition for promoting hair growth comprising lactic acid as an active ingredient. 4. The composition for promoting hair growth according to claim 3, wherein the concentration of lactic acid is 10-10 ^-12 M. Hair growth promoting composition comprising trichloroacetic acid as an active ingredient. 6. The composition for promoting hair growth according to claim 5, wherein the concentration of trichloroacetic acid is 5-10 ^-12 M. A method for promoting hair growth comprising treating glycolic acid with a topical portion of the human body at least four days a week. The method of claim 7, wherein the concentration of glycolic acid (glycolic acid) to be applied is 10 ^-1 ~ 10 ^-12 M, characterized in that the hair growth promoting method. A method for promoting hair growth comprising treating lactic acid with a topical portion of the human body for at least 4 days a week. The method of claim 9, wherein the concentration of lactic acid to be applied is 10 ⁻¹ to 10 ⁻¹² M. 10. A method of promoting hair growth comprising treating trichloroacetic acid with a topical portion of the human body at least four days a week. 12. The method of claim 11, wherein the concentration of trichloroacetic acid to be applied is 10 ^-1 to 10 ^-12 M. Hair regrowth agent comprising at least one compound selected from the group consisting of glycolic acid, lactic acid, and trichloroacetyl acid as an active ingredient. Hair growth agent comprising at least one compound selected from the group consisting of glycolic acid, lactic acid, and trichloroacetyl acid as an active ingredient. A shampoo or cosmetic composition for promoting growth and growth comprising at least one compound selected from the group consisting of glycolic acid, lactic acid, and trichloroacetyl acid as an active ingredient.

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