KR20050102345A - Hair growth agent composition - Google Patents

Abstract

The present invention relates to a hair loss prevention and hair growth promoter composition containing the extract of Pulsatilla koreana , and to shorten the cycle of transition from the resting phase to the growth phase of the hair growth cycle as an active ingredient, hair to grow new hair faster. The composition of the present invention containing a baekduong extract with excellent hair follicle cell activity with growth-phase induction promoting effect has little side effects and shows excellent hair growth promoting and hair loss preventing effects, and simultaneously contains a component having a 5α-reductase activity inhibiting effect. Even when it is very safe and has excellent hair loss prevention and hair growth promoting effect.

Description

Hair growth promoter composition {HAIR GROWTH AGENT COMPOSITION}

The present invention relates to a hair loss preventing and hair growth promoter composition containing the extract of Pulsatilla koreana , more specifically, the present invention is to reduce the cycle of transition from the resting phase to the growth phase of the hair growth cycle as an active ingredient, The present invention relates to a hair growth accelerator containing an extract of baekduong which has excellent hair follicle cell activation, along with a hair growth induction promoting effect that makes hair grow faster.

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 male hormone since it is dependent on male hormones, and thus, many studies have recently been reported to prevent and treat hair loss through inhibition of male hormone 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 that can confirm the growth-induction promoting action of hair among the effects on various mechanisms, and the hair growth-phase induction promoting effect in the Baekduong extract It was found to be excellent, and also in the experiment evaluating the hair follicle cell activity of the baekduong extract, very excellent results were achieved to complete the present invention.

Specifically, the present inventors selected dozens of plant extracts having the effects of preventing hair loss and promoting hair growth for alopecia and securing safety to the human body, and then conducted a study on the hair growth induction promoting effect. 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, the extract of Baekduong was also very good in vitro evaluation of the activity of hair follicle cells.

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 a baekduong (白頭翁, Pulsatilla koreana ) extract as an active ingredient.

Here, the extraction solvent of the baekduong extract may be one kind or a mixture of two or more kinds of lower alcohols, and the content of the baekduong extract is preferably 0.01 to 10% by weight of the total weight of the composition as a solid content.

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 baekduong extract, the baekduong extract not only has a definite mechanism of action of promoting hair growth phase, but also has an active action on hair follicle cells, thereby exhibiting hair growth promoting effect. In addition, when including a 5α-reductase activity inhibitory ingredient as an active ingredient together with the baekduong 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 the baekduong extract has excellent hair growth induction promoting action and hair follicle cell activity. In addition, it was also found that the composition containing the 5α-reductase activity inhibitory ingredient for controlling male hormone action together with the baekduong extract has not only a very good 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, Baekduong is a herbal medicine using the root of Pulsatilla koreana or other related plants (Ranunculaceae), and the herbal name is Pulsatillae Radix. The shape of Baekduong is columnar, 6-20 cm long and 5-20 mm in diameter. The outer surface is yellowish brown to brown with irregular vertical wrinkles, the skin is easily peeled off, the yellow neck is exposed, and there is a netting pattern. Roots have white soft hairs with stems and leaves. The quality is hard and crumbly, so it is easily bent and the face is flat. The old roots rot and become hollow. Representative active ingredients include saponin, akebioside, okinalin, hederagenin, oleanolic acid, etc. . Pharmacological action is antipyretic, astringent, anti-inflammatory, bactericidal action, has been used in the treatment of neuralgia, blood clots, dysmenorrhea, lymphangitis.

Looking at the production method of the extract of Baekduong included in the composition of the present invention, first purified and finely chopped the roots of the Baekduong and cooled for 5 days in about 10 times the amount of the extraction solvent, and then the extraction extract is filtered, concentrated and lyophilized methods Through dry powder of baekduong 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, lower alcohols such as methanol, ethanol and n-butanol are preferably used as extraction solvents, and one or two or more kinds of these solvents may be mixed and used for extraction.

Baekduong 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 component which may be included with the Baekduong 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, in order to enhance the action of the baekduong extract or 5α-reductase activity inhibitory ingredients and to impart additional functions suitable for use by alopecia patients, supplements such as anti-dandruff, keratin softeners, softening agents, moisturizing agents 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 of Baekduong Extract

Baekduong extract used in the examples of the present invention was prepared as follows:

First, the roots of Baekduong were chopped and passed through a sieve No. 10, followed by adding about 10 times the amount of ethanol of the Korean medicine, and then cooled 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 4.4%.

Effect Test Example 1 Evaluation of Hair Growth Induction Promoting Effect of Baekduong Extract

The hair growth phase induction promoting effect experiment was used 42-56 days old mice (C57BL / 6, male), which is 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 baekduong 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 Baekduong extract prepared in Preparation Example was diluted with 40% ethanol and used 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 baekduong extract, shows the effect according to the concentration.

Baekduong extract concentration 0.001% 0.01% 0.1% One% 10% Control Area ratio (%) 20.2 38.4 58.8 78.2 82.0 12.0

As shown in Table 1, the Baekduong extract showed a very good hair growth phase 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 Baekduong Extract

Human scalp tissue after scalp surgery was obtained from plastic surgery and hair follicle tissue was separated therefrom. That is, the scalp tissue was sterilized by immersion 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 out 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, remove the culture medium containing FBS, exchange it with the culture medium containing no FBS, and culture medium containing Baekduong extract, and incubate for 24 hours, and then add 10 μCi of radiation-labeled thymidine to each 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 sulfonate 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 baekduong extract through the thymidine uptake measurement method, it showed a very good hair follicle activity at a relatively low concentration (10 ^-4 to 10 ^-6 %). The following Table 2 shows the results of hair follicle activity evaluation of baekduonggi extract, the effect of the concentration.

Baekduong extract concentration Control 0.000001% 0.00001% 0.0001% Activity (%) 100 116 138 142

As can be seen from the above results, the baekduong extract acts directly on the hair follicle epithelium and is believed to have a hair growth promoting effect.

Examples 1-4 and Comparative Examples 1 and 2

According to the formulation of Table 3, Examples 3 and 4 further comprising the composition of Examples 1 and 2, including the Baekduong extract, and the Ginseng extract or the active extract known as 5α-reductase activity inhibiting ingredient, in addition to the Baekduong extract The composition of Comparative Examples 1 and 2, which did not include the extract and Baekduong, were prepared.

Compounding ingredient / weight (%) Example 1 Example 2 Example 3 Example 4 Comparative Example 1 Comparative Example 2 ethanol 40 40 40 40 40 40 Baekduong Extract 0.5 1.0 0.5 0.5 - - Ginseng extract - - 0.5 - 0.5 - Revitalization Extract - - - 0.5 - 0.5 Polysorbate 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 composition prepared in the composition ratio as shown in Table 3 above, the hair growth promoting effect experiment was conducted in the same manner as in the evaluation of the hair growth phase induced action of the baekduong 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 (%) 50 42 70 76 86 84

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 the extract alone showed excellent hair growth promoting action, and furthermore, in Examples 3 and 4 simultaneously containing the red ginseng extract or the active extract in combination with the Baekduong extract, It showed more excellent hair growth promoting action than when used alone.

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

As can be seen from the above experimental results, in the embodiment containing both ginseng extract or active extract together with the baekduong extract, hair growth phase induction promoting action, 5α-reductase activity inhibition, respectively, which is related to hair loss prevention or hair growth promoting action, respectively. Through different mechanisms, such as action, showed very good hair growth promoting effect, and none of the components showed the effect without affecting the action of other active ingredients. Therefore, when appropriately used in combination with a baekduong extract and a component having an inhibitory activity of 5α-reductase activity, by providing a variety of actions for the hair loss phenomenon entangled by a variety of complex mechanisms, rather than showing a single action by any one component It is expected that much better hair loss prevention or hair growth promoting effect can be expected.

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

Example 5

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

0.5 wt% of baekduong 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 3: Clinical Evaluation of a Composition Containing Ginseng Extract and Other Auxiliary Components with Baekduong 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 confirmation was carried out from at least 1 month 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 54321 Significant Decrease Moderate Decrease Hardness Decrease Significant improvement Moderate improvement Hardness improvement Unchanged Significant improvement Moderate improvement Hardness improvement Unchanged

division Hair Loss at Tricycle Subjective symptoms Visual judgment Overall improvement Example 3.6 4.0 3.7 3.8

As shown in Table 6 above, the composition of Example 5 containing the 5α-reductase activity inhibitory component and other auxiliary components together with the baekduong extract according to the present invention, the improvement of hardness in the amount of hair loss during hair removal, 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 baekduong extract was found to have an excellent effect on the hair follicle cells as well as promoting hair growth induction in the animal model. In addition, when the combination of the 5α-reductase activity inhibitory ingredients in combination with the baekduong extract, it showed a very excellent effect in the experiments with animals and clinical trials for hair loss 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, the hair growth accelerator composition containing the baekduong extract excellent in the growth phase induction promoting action and hair follicle cell activation action of the hair 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 the inhibitory action of 5α-reductase activity together with the baekduong extract, and has an excellent hair loss prevention and hair growth promoting effect.

Claims (7)

Hair loss prevention and hair growth promoter composition comprising Baekduong (白頭翁, Pulsatilla koreana ) extract as an active ingredient. The composition of claim 1, wherein the content of the extract is 100 to 10% by weight of the total weight of the composition as a solid. The composition of claim 1 or 2, wherein the extraction solvent of the baekduong extract is one kind or a mixture of two or more kinds of lower alcohols. 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 inhibiting ingredient is a ginseng extract, Euiin extract, cloves extract, Bupyeongcho extract, birch extract, gall bladder extract, active extract, honbon extract, rhubarb extract, caine extract, One of baekseng extract, white powder extract, betel nut extract, leaflet extract, turmeric extract, peony extract, red peony extract, sculptural extract, thyme extract, fennel extract, ground extract, mold extract, cow extract, tea extract and bovine extract The composition characterized by the above. A transdermal topical formulation for application to the scalp, comprising the hair loss prevention and hair growth promoter composition of claim 1.