KR20060008662A - Hair growth promoter composition - Google Patents

Abstract

The present invention relates to a hair loss prevention and hair growth promoter composition containing a stone extract (石斛, Dendrobium nobile ) extract, as an active ingredient hair shortening the transition period from the resting phase to the growth phase of the hair growth cycle of new hair The composition of the present invention, which contains a grain extract having excellent hair follicle cell activity, together with a growth phase induction promoting action, shows an excellent effect of promoting hair growth and preventing hair loss, and simultaneously contains a component having a 5α-reductase activity inhibiting effect. Even if it is very safe and has excellent hair loss prevention and hair growth promoting effect.

Stone Extract, 5 alpha-reductase, promotes hair growth, hair follicle activity, prevents hair loss.

Description

Hair growth promoter composition {HAIR GROWTH AGENT COMPOSITION}

The present invention relates to a hair loss prevention and hair growth accelerator composition containing Dendrobium nobile extract, more specifically, the present invention as an active ingredient to shorten the cycle of transition from the resting phase to the growth phase of the hair growth cycle as a new active ingredient The present invention relates to a hair growth promoter containing a grain extract having excellent hair follicle cell activation with an effect of promoting hair growth phase inducing hair to grow quickly.

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, resulting in an average of 50 to 100 hairs falling out per day. Generally, the term alopecia refers to the increase in the number of hairs that fall abnormally due to shortening of the hair growth rate in the growth phase and more hair in the degenerative or resting phase.

The causes of alopecia have been discussed, such as excessive male hormone action, excessive sebum secretion, poor blood circulation, hypoglycemia caused by peroxide or bacteria, genetic factors, aging, stress. However, to date, no clear cause for hair loss is unknown, and it is known that a very complicated action is intertwined.

As for the various causes of hair loss, hair loss prevention products known to date are effective ingredients for promoting blood circulation, strengthening hair root function, moisturizing scalp, preventing dandruff, antioxidant effect, hair growth period, and suppressing male hormone activity. It contains ingredients, etc., but there is still no clear effect in terms of effects and side effects may be raised.

Experimental methods used to prevent hair loss and promote hair growth are mainly used in vivo evaluation using experimental animals and in vitro evaluation using hair follicle cells and tissue culture. In the 1980s, research on the differentiation mechanism of hair follicles became active with the development of culture methods of dermal papilla cells and outer root sheath cells, which are the core cells of hair follicles. With the development of tissue culture methods, it has been shown to be a useful evaluation model for research on hair growth, wool and hair loss prevention. In recent years, biochemical and molecular biological experiments have been actively conducted to identify various growth factors and genes related to hair growth, research on mechanism of action, and drug search.

The effects of a commercially available product on the hair as a hair growth or hair loss preventing agent on the hair include growth phase induction effect, hair growth phase extension effect, 5α-reductase inhibitory effect, blood circulation promoting effect, bactericidal effect, anti dandruff effect, moisturizing effect, antioxidant effect, etc. However, in the existing formulations, hair loss prevention and hair growth promoting effects are not sufficient.

Androgenetic alopecia is directly dependent on the amount of androgen, which is dependent on androgen hormones. Accordingly, many studies have recently been reported to prevent and treat hair loss by inhibiting androgen activity. Briefly explain the mechanism of hair loss on male hormones are as follows. In other words, testosterone, one of the male hormones, is converted to dihydrotestosterone, an active male hormone, by an enzyme called 5α-reductase. Induces hair loss. In addition, such mechanisms may cause excessive production of sebum, causing acne, seborrheic dermatitis, and the like, and as a result, scalp may occur with inflammation. As a result, androgenetic alopecia is due to the excessive production of dihydrotestosterone by the action of 5α-reductase, it will be able to prevent and treat masculine alopecia by inhibiting the activity of 5α-reductase. In view of this, male hair loss treatment using finasteride, which has been used as a prostate treatment for men, has been developed, but side effects such as sexual dysfunction have been reported, and their 5α-reductase activity against hair loss It is also difficult to fully anticipate the effect by inhibitory effect alone.

In view of the above problems, the present inventors screened dozens of plant extracts through animal experiments to confirm the growth-induction promoting action of hair among the effects on various mechanisms, hair growth period induction promoting effect in the stone extract It was found to be excellent, and also in the experiment evaluating the hair follicle cell activity of the Seokgok extract, very good results were obtained, which led to the completion of the present invention.                         

Specifically, the present inventors selected dozens of plant extracts having the effect of preventing hair loss and promoting hair growth for alopecia and securing safety to the human body, and then conducted a study on hair growth induction promoting effect, and the stone extract was In the hair growth cycle where new hair grows, grows and falls out, it is found that it promotes the transition from the resting phase to the growth phase. Moreover, Seokgok extract also showed very good results in vitro evaluation of the activity of hair follicle cells.

An example of using such a grain extract in hair products is Japanese Patent Application Laid-Open No. 2000-154113, where a grain extract ( Dendrobium officinale ) is used as a moisturizing plant extract. The raw material of the cosmetic composition used for the purpose of this is disclosed. However, there are no patents or documents that use grains in connection with promoting hair growth or preventing hair loss.

It is an object of the present invention to provide a hair growth promoter composition which has little side effects and has excellent hair growth promoting and anti-hair loss effects.

In order to achieve the above object, the present invention provides a hair loss prevention and hair growth promoter composition comprising an extract of Seokgok (石斛, Dendrobium nobile ) as an active ingredient.

Here, the content of the grains extract is preferably 0.01 to 10% by weight of the total weight of the composition as a solid content, the extraction solvent of the grains extract may be one or two or more mixed solvents of lower alcohols and hydrocarbon-based solvents.

In addition, the composition of the present invention may further comprise at least one 5α-reductase activity inhibiting component, wherein the content of the 5α-reductase activity inhibiting component is preferably 0.001 to 10% by weight.

In addition, the composition of the present invention may be included in a transdermal topical formulation that can be applied to the scalp, such as a liquid, cream, paste, aerosol.

According to the present invention, the composition comprising the Seokgok extract has a clear mechanism of action that promotes hair growth phase induction, as well as an active action on hair follicle cells, thereby exhibiting hair growth promoting effect. In addition, when the addition of 5α-reductase activity inhibitory ingredient as an active ingredient with the Seokok extract can be more excellent hair loss prevention and hair growth promoting effect.

Hereinafter, the composition of this invention is demonstrated more concretely.

First, in view of the background of the present invention, in order to prevent hair loss and promote hair growth for alopecia, various hair loss mechanisms or mechanisms of action should be approached through a variety of mechanisms. The study was examined. First of all, we have screened hundreds of combinations of male hormone-regulating components, blood circulation promoting components, cell activating components, and anti-inflammatory components, and hair loss prevention and hair growth promoting effects. As a result, it was found that Seokgok extract has excellent hair growth induction promoting action and hair follicle cell activity. In addition, it was also found that the composition including the 5α-reductase activity inhibitory ingredient for controlling male hormone action together with the grains extract has not only excellent hair loss prevention and hair growth promoting effect, but also no side effects. Therefore, in the present invention, in terms of hair growth stage induction promoting action, hair follicle cell activation action, 5α-reductase activity inhibiting action, and the like, which are evaluated as important factors for hair growth and hair loss prevention, a combination of various causes of hair loss is provided. It is to provide a composition having a hair loss prevention and hair growth promoting action.

In the composition of the present invention, Seokgok uses ground parts such as Dendrobium nobile (Orchidaceae) or other genus plants Dendrobium linawianum , Dendrobium officinale , Dendrobium moniliforme , etc. The herbal name is Dendrobii Herba . The shape of the granite is oblong, 20-40 cm in length, 4-6 mm in diameter, and the length of the node is 25-30 mm. The outer surface is golden yellow to yellow green with deep vertical grooves. This herb has almost no smell and tastes a bit bitter. Typical active ingredients include dendrobine, dendramine, nobilonine, dendroxine, dendrin, and 6-hydroxydendroxine. It contains, and contains the ingredients of other similar herbal medicines.

Looking at the manufacturing method of the grain extract contained in the composition of the present invention, first, the ground portion of the grain is refined and finely cooled for 5 days in about 10 times the amount of the extraction solvent, and then the extraction extract is filtered, concentrated and lyophilized Through the dry powder of the grains extract is obtained. At this time, the extraction solvent is not particularly limited in the selection, purified water; Lower alcohols such as methanol, ethanol, isopropyl alcohol and n-butanol; Polyhydric alcohols such as glycerol, propylene glycol and 1,3-butylene glycol; And hydrocarbon solvents such as methyl acetate, ethyl acetate, benzene, n-hexane, diethyl ether, dichloromethane, and the like. Among these solvents, one kind or a mixture of two or more kinds of lower alcohols and hydrocarbon solvents is preferable.

The soybean extract prepared as described above is preferably included as a solid content in 0.01 to 10% by weight of the total weight of the composition of the present invention. If it is less than 0.01% by weight, the hair growth phase induction promoting effect is not satisfactory, and at a concentration higher than 10% by weight, the effect thereof is not sufficient compared to the dose, which is not preferable.

The 5α-reductase activity inhibitory ingredient which may be included with the grain extract in the composition of the present invention is a compounding ingredient of an external preparation that exhibits a hair loss prevention effect by inhibiting the action of 5α-reductase in human hair follicles, and has no problem in terms of safety. It is not specifically limited, It can mix | blend individually or in combination of 2 or more components. Such 5α-reductase activity inhibitory ingredients include, for example, ginseng extract, uiyiin extract, clove extract, Bupyeongcho extract, birch extract, gallja extract, active extract, honbon extract, rhubarb extract, ginko extract, baekjajam extract, Plant-derived herbal ingredients such as white extract, betel extract, leaflet extract, turmeric extract, peony extract, red peony extract, engraver extract, thyme extract, fennel extract, native extract, mold extract, cow extract, tea extract, bovine extract Can be used. These herbal medicines are generally available in the process of the Korean Pharmacopoeia or herbal medicine standard, and are generally available on the market. The extracts of these herbal medicines are obtained by a conventional solvent extraction method and are not particularly limited in selecting a solvent.

In the composition of the present invention, the content of the 5α-reductase activity inhibiting component is preferably 0.001 to 10.0% by weight, particularly preferably 0.01 to 5.0% by weight, based on the total composition.

In addition, the composition of the present invention, to enhance the action of the grain extract or 5α-reductase activity inhibiting component and to impart additional functions suitable for use by alopecia patients, supplements such as anti-dandruff, keratin softeners, softening agents, moisturizing agents, etc. The components can be added, in which case a better effect is obtained.

Examples of auxiliary components, such as anti-dandruff agents, keratin softeners, coolants, and moisturizers, which are incorporated into these conventional hair loss prevention agents and hair growth promoters, include hinokithiol, capsicum tink, nicotinic acid benzyl, pyroxtonolamine, salicylic acid, and el-menthol. have. These auxiliary ingredients do not limit the concentration used in the range in which the dosage form can be maintained without disturbing the effect of the main ingredient, but in consideration of human safety or formulation stability, 0.001 to 0.1% by weight of hinochithiol and 0.001 to 0.1% of red pepper tink. 10% by weight, benzyl nicotinate is added in an amount of 0.001 to 0.1% by weight, pyrotonolamine in an amount of 0.001 to 1.0% by weight, salicylic acid and el-menthol in 0.01 to 1.0% by weight, respectively.

Hair growth promoter composition of the present invention can be prepared in any formulation that can be applied to the scalp, such as liquid, cream, paste, or solid phase, shampoo, hair conditioner, hair lotion for promoting hair growth by adding conventional additives It may be prepared in a composition such as a liquid wool type, and this also includes an aerosol type of these formulations.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, these Examples are only illustrative of the present invention, and the scope of the present invention is not limited to these.

In the effect test examples below, the C57BL / 6 mouse model was used as an animal test model for evaluating hair growth induction promoting effect. The C57BL / 6 mouse has black hair and has spontaneous alopecia. In addition, melanocytes (melanocytes) are present only in the hair follicles, and melanin synthesis matches well with the hair growth cycle, which has the advantage of determining the hair growth cycle in terms of skin color. It is widely used for research.

Preparation Example: Preparation Method of Seokgok Extract

Seokgok extract used in the embodiment of the present invention was prepared as follows:

First, the ground portion of Seokgok was chopped and passed through a sieve No. 10, and about 10 times the amount of ethanol of Korean pharmaceuticals was added thereto, followed by cooling at room temperature for 5 days. The extracted stock solution was filtered using Whatman # 2 filter paper, and the filtered extract was evaporated completely at 45 ° C. using a vacuum condenser to obtain a dried extract. Yield was about 1.9-2.5%.

Effect Test Example 1 Evaluation of Hair Growth Induction Promoting Effect of Stone Extracts

Hair growth phase induction promoting effect experiment was used 42-49 days old mice (C57BL / 6, male) widely used for the evaluation of hair growth phase induction action.                     

First, the hair on the back of the mouse was removed using an electric razor, and each mouse was weighed and divided into 12 pieces so that the weight was evenly distributed. After one day of adaptation, the control drug and the grain extract were applied to the hair removal site from the next day. At this time, 40% ethanol was used as a reference drug, and the concentrated solid of the Seokok extract prepared in Preparation Example was diluted to 40% ethanol at various concentrations. 100 µl each was applied to the back of the mouse once a day for 28 days to observe the growth-induction promoting effect. The results were obtained by using an image analyzer to determine the ratio of the area where the newborn hair was grown to the area from which hair was removed. Evaluated. Table 1 below shows the results of the hair growth phase induction promoting action of the Seokok extract, shows the effect according to the concentration.

Stone Extract Concentration 0.001% 0.01% 0.1% One% 10% Control Area ratio (%) 19.8 38.8 60.4 77.6 82.0 12.2

As shown in Table 1, the Seokgok extract showed a very good hair growth induction promoting action in a concentration-dependent manner. At concentrations lower than 0.01%, hair growth phase induction was better than the control, but not satisfactory. At concentrations higher than 10%, the action was not sufficient.

Effect Test Example 2 Evaluation of Increased Hair Follicle Activity of Seokgok Extracts

Human scalp tissue after scalp surgery was obtained from plastic surgery and hair follicle tissue was separated therefrom. First, the scalp tissue was sterilized by soaking in 70% ethanol for 1 minute and washed three times with M199, a cell culture medium. Under the stereo microscope, the epidermis and the dermis were cut with a surgical scalpel to separate the epidermis, and hair follicles embedded in the dermis were pulled out one by one using tweezers. The isolated hair follicles were transferred to M199 culture solution containing 10% fetal bovine serum (FBS), and the lower part of the hair follicles containing the dermal papilla was cut with a scalpel. The teat was separated using fine tweezers and transferred to M199 culture medium containing 20% FBS and incubated for 2 weeks. When cells grew from the dermal papilla tissue and filled with the culture vessel, the cells were separated from the culture vessel with 0.25% trypsin and 0.02% EDTA, followed by subculture.

2 ~ 3 passages of dermal papilla cells were diluted to a concentration of 2 × 10 ⁴ / ㎖ with M199 culture medium containing 10% FBS, 5 ml each of the 60 mm culture vessel was incubated for 24 hours in a 37 ℃ incubator. The next day, the culture medium containing FBS was removed, the culture medium containing FBS and the culture medium containing the Seokgok extract were incubated for 24 hours, and then radiation-labeled thymidine was added 10 μCi per plate. And further incubated for 24 hours. The cultured cells were washed three times with phosphate buffer and washed once with 5% trichloroacetic acid. Cells were dissolved in 0.1% sodium dodecyl sulfate and 0.5 N sodium hydroxide solution, mixed in a scintillation cocktail, and the amount of radioisotope was measured using a beta-counter. Cell activity was evaluated by comparing how much uptake of radiolabeled thymidine into the cells.

As a result of measuring the hair follicle activity of the Seokgok extract by the thymidine uptake measurement method, the hair follicle cell activity was excellent at relatively low concentration (10 ^-4 ~ 10 ^-6 %). . Table 2 shows the results of the hair follicle activity evaluation of the grain extract, the effect of the concentration.

Stone Extract Concentration Control 0.000001% 0.00001% 0.0001% Activity (%) 100 108.4 126.2 132.2

As can be seen from the above results, the stone extract is directly acted on the hair follicle epithelium, it is judged to have a hair growth promoting effect.

Examples 1-4 and Comparative Examples 1 and 2

According to the formulation of Table 3, in addition to the compositions of Examples 1 and 2, including the Seokgok extract, and in addition to the Seokgok extract, Examples 3 and 4 further comprising a ginseng extract or clove extract known as a 5α-reductase activity inhibiting component The composition of Comparative Example 1 and 2, and did not include the grain extract was prepared.

Compounding ingredient / weight (%) Comparative Example 1 Comparative Example 2 Example 1 Example 2 Example 3 Example 4 ethanol 40 40 40 40 40 40 Seokgok Extract - - 0.5 1.0 0.5 0.5 Ginseng extract 0.5 - - - 0.5 - Clove Extract - 0.5 - - - 0.5 Polysorbate 60 (Tween 60) 0.5 0.5 0.5 0.5 0.5 0.5 Purified water Add until 100% by weight

Effect Test Example 3: Evaluation of hair growth promoting effect by animal experiment

With each of the compositions prepared in the composition ratio as shown in Table 3 above, the hair growth promoting effect experiment was carried out in the same manner as in the evaluation of the hair growth phase induced action of the Seokok extract. Extract used in the composition used a concentrated solid according to the preparation. Table 4 below shows the results of the hair growth phase induction promoting action evaluation.                     

division Comparative Example 1 Comparative Example 2 Example 1 Example 2 Example 3 Example 4 Area ratio (%) 48.2 42.8 66.2 76.4 90.6 84.4

As shown in Table 4 above, hair growth promoting action was also observed in Comparative Example 1 and Comparative Example 2 containing only the 5α-reductase activity inhibiting component, but was not satisfactory. Example 1 and Example 2 containing only the grains extract exhibited excellent hair growth promoting action, and furthermore, in Examples 3 and 4 simultaneously containing the ginseng extract or clove extract together with the grains extract, It showed more excellent hair growth promoting action than when used alone.

These results indicate that the synergistic effect on the hair growth promoting action when the effect of inhibiting 5α-reductase activity together with the hair growth phase induction promoting action of the Seokok extract.

As can be seen from the above experimental results, in Examples containing both ginseng extract and cloves extract together with the Seokgok extract, hair growth phase induction promoting action and 5α-reductase activity inhibition, respectively, which are related to hair loss prevention or hair growth promoting action, respectively. Through different mechanisms, such as action, showed very good hair growth promoting effect, neither component showed the effect without affecting the action of the other active ingredient. Therefore, when appropriately used in combination with the Seokok extract and components having the inhibitory action of 5α-reductase activity, it provides various effects on the hair loss phenomenon entangled by various complex mechanisms, rather than showing the sole action by any one component We anticipate a much better hair loss prevention or hair growth promotion effect.

Subsequently, according to the present invention, a composition comprising an auxiliary ingredient together with a grain extract and an active ingredient having a 5α-reductase activity inhibitory activity was prepared as a liquid wool agent, and clinical trials were conducted in persons with alopecia.

Example 5

A composition containing a ginseng extract and other auxiliary ingredients together with the Seokok extract according to the present invention was prepared by the following prescription.

0.5% by weight stone extract;

0.5% by weight of ginseng extract;

0.05% by weight of hinokithiol, 1.0% by weight of red pepper tin, 0.01% by weight of benzyl nicotinate, 0.1% by weight of pyrotonolamine, 0.1% by weight of salicylic acid, 0.1% by weight of L-menthol;

Ethanol 40.0 wt%, purified water 57.64 wt%; (100 wt% total)

Effect Test Example 4: Clinical Evaluation of a Composition Containing Ginseng Extract and Other Auxiliary Components with Seokgok Extract

For the composition prepared in Example 5, in order to confirm the effect in human clinical trials were selected and tested for alopecia subjects.

Thirty-five drops (approximately 2 ml) were applied to the hair loss site for 15 males and females with male or female alopecia or daily average hair loss of 100 or more. It was carried out in a manner that was carried out, depending on the degree of effect confirmed from a minimum of 2 months to a maximum of 4 months.                     

To determine the effect, the average daily hair loss at trituration, gross findings, and the degree of improvement of subjective symptoms were evaluated in five stages according to the following evaluation scale (Table 5), and overall overall improvement was taken as the average of the evaluation scale. The final verdict was that the overall improvement was 3.0 points or more, and the results are shown in Table 6 below.

Phase division Hair Loss at Tricycle Subjective symptoms Visual judgment 5 4 3 2 1 Significant decrease moderate decrease hardness hardness worse (increase) Significant Improvement Moderate Improvements Hardness Improvements Constant Deterioration Significant Improvement Moderate Improvements Hardness Improvements Constant Deterioration

division Hair Loss at Tricycle Subjective symptoms Visual judgment Overall improvement Example 3.7 3.9 3.6 3.7

As shown in Table 6 above, the composition of Example 5 containing 5α-reductase activity inhibitory component and other auxiliary components together with the Seokgok extract according to the present invention, the improvement of hardness in the amount of hair loss during hair loss, subjective symptoms and visual determination It can be seen that the effect of more than moderate to moderate improvement is very excellent in preventing hair loss and promoting hair growth. In addition, no adverse effects were found in all subjects during the trial period, indicating that the composition is safe for humans.

Taken together, the Seokgok extract was found to have an excellent effect on hair follicle cells as well as promoting hair growth induction in an animal model. In addition, the combination of the 5α-reductase activity inhibitory component with the Seokkok extract showed a very good effect in experiments using animals and clinical trials in alopecia patients compared to when used alone. Therefore, when appropriately used in combination of these two components, by providing a variety of actions to the hair loss phenomenon entangled by various complex mechanisms, it is much better to prevent hair loss and promote hair growth than to exhibit a single action by any one component It can be seen that.

According to the present invention, a hair growth accelerator composition containing a grain extract having excellent hair growth induction promoting action and hair follicle cell activation action as an active ingredient for promoting hair growth has almost no side effects and exhibits excellent hair growth promoting and hair loss prevention effects. In addition, the composition according to the present invention is very safe even when it contains a component having a 5α-reductase activity inhibitory action at the same time with the Seokkok extract and has an excellent hair loss prevention and hair growth promoting effect.

Claims (7)

Hair loss prevention and hair growth promoter composition comprising an extract of Seokgok (石斛, Dendrobium nobile ) as an active ingredient. The composition of claim 1, wherein the content of the grain extract is a solid content of 0.01 to 10% by weight of the total weight of the composition. The composition according to claim 1 or 2, wherein the extraction solvent of the grain extract is one or two or more mixed solvents of a lower alcohol and a hydrocarbon solvent. The composition of claim 1, further comprising a 5α-reductase activity inhibiting component. The composition according to claim 4, wherein the content of the 5α-reductase activity inhibiting component is 0.001 to 10% by weight. The method according to claim 4 or 5, wherein the 5α-reductase activity inhibitory ingredients are red ginseng extract, Euiin extract, cloves extract, Bupyeongcho extract, birch extract, gall bladder extract, active extract, botanical extract, rhubarb extract, cabbage extract 1 of zinnia extract, white powder extract, betel nut extract, leaflet extract, turmeric extract, peony extract, red peony extract, sculptural extract, thyme extract, fennel extract, garden extract, mold dog extract, cow extract, tea extract and bovine extract A composition characterized in that the species or more. A transdermal topical formulation for application to the scalp, comprising the hair loss prevention and hair growth promoter composition of claim 1.