KR101825603B1 - Composition of skin external application for improving alopecia containing Oldenlandia Diffusa Willd extracts - Google Patents

Abstract

The present invention relates to a composition for external application for skin which can improve hair loss, and more particularly, to a composition for external application for skin which contains white blood powdery extract as an active ingredient and improves hair loss through excellent 5-alpha-lyudactase inhibitory effect .

Description

[0002] The present invention relates to a skin external application composition for improving hair loss, which contains an extract of Bacillus subtilis,

The present invention relates to a composition for external application for skin which can improve hair loss, and more particularly, to a composition for external application for skin which contains white blood powdery extract as an active ingredient and improves hair loss through excellent 5-alpha-lyudactase inhibitory effect .

5-alpha reductase is an enzyme involved in the metabolism of testosterone, one of the male hormones, testosterone, into dihydrotestosterone, which exists in the male hormone-responsive tissues of sebaceous gland, hair follicle, prostate and epididymis. Conversion requires NADPH. (Diane et al., J.I.D. 1995). The testosterone is involved in male sexual dysfunction, skeletal muscle increase, male genitalia, scrotum growth, and spermatogenesis, and acne, sebum increase, hair loss and enlargement of the prostate are involved in the tissues of dihydrotestosterone. Therefore, researches are being actively carried out to develop a drug capable of inhibiting the enzyme and to develop it as an acne treatment agent, an sebaceous gland inhibitor, and an anti-hair loss agent. After puberty, excessive secretion of male hormone causes acne and hair loss. Studies to develop hair restorer or anti-hair restorer with 5-alpha-reductase inhibitory activity to prevent the production of dihydrotestosterone excess in follicular dermal papilla cells are actively conducted It is progressing.

Traditionally, female hormones such as estrogen have been used for the treatment of acne and for the treatment of male pattern baldness or have used 5-alpha reductase inhibitors. However, female hormones have been reported to cause skin irritation and side effects due to hormone administration, and they are currently being discontinued or using extremely low doses. In recent years, Merck has limited the use of finasteride, a synthetic 5-alpha reductase inhibitor, due to the fact that it is commercially available as a hair restorer, and the side effects caused by synthetic products .

Accordingly, the inventors of the present invention have searched for natural products superior in the inhibitory effect of 5-alpha reductase, and found that white freunds were inhibited 5-alpha reductase and thus had excellent hair loss improving effect.

Accordingly, an object of the present invention is to provide a composition for external application for skin which is superior in improving hair loss by inhibiting 5-alpha reductase.

In order to accomplish the above object, the present invention provides a composition for external application for skin for improving hair loss, which comprises an extract of Bacillus subtilis as an active ingredient.

The composition for external application for skin provided by the present invention contains an extract of Bacillus subtilis as an effective ingredient to effectively inhibit the action of 5-alpha reductase and thus is very safe for the human body by using natural products. Therefore, the present invention can provide a skin external composition for hair loss improvement.

The present invention provides a composition for external application for skin for improving hair loss comprising an extract of Bacillus subtilis (Oldenlandia Diffusa Willd) as an active ingredient.

Hereinafter, the present invention will be described in more detail.

In the present invention, Bacillus specialis used as an active ingredient is one of herbal medicine widely known and used not only in Oriental medicine but also in folk medicine. Baekhwa is a Rubiaceae plant that grows in the lush and shady forests of southern China, Southeast Asia, and Jeju Island. It has been used in traditional Chinese medicine for the treatment of liver cancer, lung cancer, rectal cancer, Betulin, Betulinic acid, Ursolic acid, Oleanolic acid, Stigmasterol, Beta-sitosterol, etc. are contained in the Baekhwa exclusive use. , Β-Glycyrrhetinic acid, p-Coumaric acid, Glucoside, Hentriacontane, etc., and have anticancer activity, anti-inflammatory effect and antiviral effect Lt; / RTI >

The whitened callus extract of the present invention can be prepared by a method known in the art, and the method is not particularly limited. Specific examples of the solvent include water, a lower alcohol (methanol, ethanol), a mixture of water and a lower alcohol, acetone, 1,3-butylene glycol, n-propanol , Isopropanol, n-butanol, and mixed solvents thereof are added in a volume of 5 to 20 times by volume, and the mixture is extracted by filtration. The filtrate is concentrated under reduced pressure. Water is added to the concentrate and dispersed, and then an equal amount of a low-polarity organic solvent such as ethyl acetate, chloroform, or diethyl ether is added to the dispersion and shaken. The organic layer is separated and concentrated under reduced pressure to obtain an excellent extract. As the extraction method, 12 to 96 hours in the case of cold beating and percolation, or anhydrous or lower alcohol having 1 to 4 carbon atoms, ethyl acetate or diethyl ether as a solvent, the mixture is allowed to stand at 4 to 25 ° C for 3 to 20 days The active ingredient may be extracted by aging. In the case of warming, it is preferable that the heating is carried out at a temperature close to the reflux temperature of the solvent for 5 to 24 hours, depending on the kind of the solvent to be used and the temperature.

The thus-prepared white-fly reed extract has a strong effect on alleviating hair loss by inhibiting 5-alpha reductase, and can be provided as an external preparation for skin, harmless and safe to human body.

The composition for external application for skin of the present invention contains 0. 5% to 50% by weight, more preferably 0.01% to 20% by weight, based on the total weight of the composition. If the content is less than 0.0001% by weight, the effect is insignificant. If the content is more than 50% by weight, the effect is not increased more than the content is increased.

The composition for external application for skin according to the present invention may be formulated containing a cosmetically or dermatologically acceptable medium or base. It may be any formulation suitable for topical application, for example, as a solution, a gel, a solid, a paste anhydrous product, an emulsion obtained by dispersing an oil phase in water, a suspension, a microemulsion, a microcapsule, Such as cream, skin, lotion, powder, ointment, spray, pack, cone stick, hair tonic, hair nutritional lotion, hair treatment, hair conditioner, hair shampoo, hair lotion Lt; / RTI > May also be used in the form of a foam or in the form of an aerosol composition further containing a compressed propellant. These compositions may be prepared according to conventional methods in the art.

In addition, the composition for external application for skin according to the present invention may further comprise at least one selected from the group consisting of a fatty substance, an organic solvent, a solubilizing agent, a thickening agent, a gelling agent, a softening agent, an antioxidant, a suspending agent, a stabilizer, a foaming agent, a fragrance, Or any other conventionally used in cosmetics such as nonionic emulsifiers, fillers, sequestering agents, chelating agents, preservatives, vitamins, barrier agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles or cosmetics ≪ RTI ID = 0.0 > cosmetics < / RTI > such as botanical ingredients, or adjuvants conventionally used in the field of dermatology. Such adjuvants are introduced in amounts commonly used in the cosmetics or dermatological fields.

Hereinafter, the constitution and effects of the present invention will be described in more detail with reference to test examples and examples. However, these test examples and examples are provided for illustrative purposes only in order to facilitate understanding of the present invention, and the scope and scope of the present invention are not limited thereto.

[Preparation Example 1] Preparation of Baekhwasa reed extract

100g of crushed white shrimp powder was added to 1L of ethanol, boiled for 12 hours in an extractor equipped with a cooling condenser, filtered through a 300 mesh filter cloth, and the filtrate was filtered at 4 to 15 ° C for 7 days After being left to stand for aging, insoluble matter was removed by filtration through Wattman No. 2 filter paper. The obtained filtrate was concentrated under reduced pressure at 60 占 폚 using a distillation apparatus equipped with a cooling condenser. The mixture was dispersed in 50 ml of water and further extracted with 300 ml of ethyl acetate. The organic layer was concentrated and lyophilized to obtain 19.4 g of white freunds extract of dry weight.

[Test Example 1] Evaluation of 5-alpha reductase inhibitory efficacy

The adult male Sprague-Dawley Rat (7-8 weeks old) was killed with diethylether, and the abdominal prostate was removed to remove connective tissue. To this solution, a buffer solution (0.32 M sucrose, 0.1 mM dithiothreitol, 20 mM sodium acetate) was added, and the mixture was finely pulverized and suspended in a pulverizer. The suspension filtered through gauze was centrifuged at 1500 × g, pellet was taken, and the buffer solution was mixed and suspended at a concentration of 20 to 30 mg / ml.

A portion of the suspension was taken in 0.02 M phosphate buffer and reacted with substrate testosterone, which is an isotope, 3 H, to determine the amount of product dihydrootestosterone produced. The reaction solution contained 1 mM dithiothreitol, 20 mM phosphate buffer (pH 6.5), 50 μM NADPH, [1,2,6,7-3H] testosterone 0.1 μCi / testosterone (1 × 10 ^-7 M) An enzyme suspension was added to prepare a total reaction solution of 565 占 퐇.

An aliquot of the above-prepared white freunds extract was dissolved in 10% dimethylsulfoxide (DMSO) and added to 10 μl of the reaction. The same volume of the solvent was used as the control, and the white porcelain extract was used as the positive control. The white porcelain extract was prepared in the same manner as in Preparation Example 1, except that white porcelain was used instead of white freckle.

The reaction was carried out at 37 ° C for 30 minutes by adding the prepared enzyme suspension, and then 600 μl of ethyl acetate was added to stop the reaction, and the product was dried through nitrogen gas. After dissolving in 50 μl of ethyl acetate, the whole amount was dropped on a silica plastic sheet kiesel gel 60 F 254 (Silica plastic sheet kieselgel 60 F 254), and the developing solvent, ethyl acetate: cyclohexane (1: 1) Respectively. After the silica plastic sheet was dried in a natural state, a system of Bas (Fujifilm, Japan) was used to measure the amount of isotopes. The dried plastic sheet and the exposure film were put in a cassette for 1 week The amount of testosterone exposed to the film and the amount of isotopes of dihydrotestosterone produced were quantitated using the exposed intensity. The IC ₅₀ values were repeated two times and averaged. The results are shown in Table 1 below.

division IC ₅₀ Untreated group - Baekhwasa reed extract 1.6 x 10 ^-5 % White potato extract 2.1 x 10 ^-5 %

As can be seen from the above Table 1, the Bacillus subtilis extract according to the present invention showed a high inhibitory effect on 5-alpha reductase as similar to the positive control group of white porcelain extract. Thus, it was confirmed that the white freckle extract of the present invention exhibits excellent 5-alpha reductase inhibitory effect.

[Examples 1 to 2 and Comparative Example 1]

Examples 1 to 2 and Comparative Example 1 were produced according to the compositions shown in Table 2 below. The following compositions are O / W formulations and the units are wt.%.

division Raw material name Example 1 Example 2 Comparative Example 1 Paid
ingredient Stearic solution seed 1.0 1.0 1.0 Cetearyl alcohol 0.2 0.2 0.2 Hydrogenated oil 0.7 0.7 0.7 Chin type glyceryl stearate 0.5 0.5 0.5 Hydrogenated lecithin / C12-16 alcohol / palmitic acid liquid seed 1.0 1.0 1.0 antiseptic 0.3 0.3 0.3 Polydensen 4.0 4.0 4.0 Meadow Foam Seed Oil 1.0 1.0 1.0 Pentaerythrityl tetraisostearate 3.0 3.0 3.0 Dimethicone 0.5 0.5 0.5 Cetyl octanoate 2.0 2.0 2.0 Decyl cocoate 1.0 1.0 1.0 Cyclomethicone 3.0 3.0 3.0 Tocopheryl acetate 0.1 0.1 0.1 Awards
ingredient Purified water To 100 To 100 To 100 Butylene glycol 5.0 5.0 5.0 Disodium iodide 0.02 0.02 0.02 Tiei 0.15 0.15 0.15 antiseptic 0.2 0.2 0.2 Baekhwa private plant extract (Preparation Example 1) 1.0 10.0 -

≪ Preparation methods of Examples 1 and 2 and Comparative Example 1 >

(1) The oil components were heated (70 to 75 ° C) and mixed uniformly.

(2) The aqueous phase components were heated (70 to 75 캜) to uniformly dissolve and mix.

(3) The emulsion was prepared by adding the above-mentioned (1) to the above (2) while maintaining the temperature at 70 to 75 캜 under stirring, and the emulsion was cooled to 28 to 30 캜.

[Test Example 2] Evaluation of acne improvement efficacy

Twelve individuals with acne were allowed to use Examples 1 and 2 and Comparative Example 1 for one month.

Acne improvement scale is from 1 point to 5 points, 1 point is 'No', 3 points are 'Normal' and 5 points are 'Very agree'. The experimental results are shown in the following Table 3 as the average score of 12 persons.

The acne extermination period was based on the number of days of disappearance readings, and the results were based on the results after 1 month with or without recurrence of acne.

The reduction of sebaceous secretion was from 1 point to 5 points, 1 point was 'No', 3 points were 'Normal' and 5 points were 'Very agree'. Experimental results are shown in Table 3 below with an average score of 12 persons.

The presence or absence of skin irritation was evaluated as (number of stimuli) / (total number of test subjects).

division Inflammatory acne improvement Acne-blooding period (days) Recurrence of acne Decrease sebaceous glands Presence or absence of stimulation Example 1 4.2 5.2 none 4.5 radish Example 2 4.8 3.4 none 4.8 radish Comparative Example 1 2.3 16.8 Observed 2.5 radish

As can be seen from Table 3, the composition for external application for skin containing the extract of Bacillus subtilis according to the present invention (Examples 1 and 2) showed no recurrence of acne, a mean score of 4.2 or higher for improvement of inflammatory acne, To 3.4 days and an average of 4.5 points for the reduction of sebum secretion, and showed excellent effect on acne improvement without skin irritation. On the other hand, the composition for external application for skin, which does not contain the extract of Paeonia spp. Of the present invention (Comparative Example 1), did not have the effect of improving acne and reducing sebum secretion.

[Test Example 3] Test for improving hair loss

20 male subjects aged 25 to 40 years with relatively high hair loss amount were selected and the shampoo composition described in Table 4 was used once a day for one month. Then, sensory evaluation was performed to evaluate the effect of improving hair loss according to the following evaluation criteria And the results are shown in Table 5.

ingredient Example 3
(weight%) Example 4
(weight%) Comparative Example 2
(weight%) Sodillauryl sulphite 36.0 36.0 36.0 Cocamidopropyl betaine 8.0 8.0 8.0 Palmitidine dimalate 2.0 2.0 2.0 Glycollosteralate 1.5 1.5 1.5 Polyquaternium 10 0.5 0.5 0.5 Saitric Acid 0.1 0.1 0.1 glycerin 2.0 2.0 2.0 Baekhwa private plant extract (Preparation Example 1) 1.0 10.0 - Preservative, fragrance, pigment Suitable amount Suitable amount Suitable amount Purified water to 100 to 100 to 100

<Evaluation Criteria>

1: It was not improved.

2: Just so.

3: A little improved.

4: Some improvement.

5: Significant improvement.

division Example 3 Example 4 Comparative Example 2 Hair loss improvement effect 4.2 4.5 2.1

As can be seen from the above Table 5, Examples 3 to 4 containing the white freund's extract of the present invention showed better hair loss improving effect than Comparative Example 2 containing no active ingredient.

[Formulation Example 1] Nutritional lotion

Nutrition lotion was prepared according to a conventional method according to the composition shown in Table 6 below.

Raw material name Content (% by weight) Purified water Balance glycerin 8.0 Butylene glycol 4.0 Hyaluronic acid extract 5.0 Beta Glucan 7.0 Carbomer 0.1 Baekhwasa reed extract 1.0 Caprylic / capric triglyceride 8.0 Squalane 5.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 antiseptic Suitable amount incense Suitable amount Pigment Suitable amount Triethanolamine 0.1

[Formulation Example 2] Nutrition lotion

Nutrition lotions were prepared in a conventional manner according to the composition shown in Table 7 below.

Raw material name Content (% by weight) Purified water Balance glycerin 3.0 Butylene glycol 3.0 Liquid paraffin 5.0 Beta Glucan 7.0 Carbomer 0.1 Baekhwasa reed extract 3.0 Caprylic / capric triglyceride 3.0 Squalane 5.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Polysorbate 60 1.5 antiseptic Suitable amount incense Suitable amount Pigment Suitable amount Triethanolamine 0.1

[Formulation Example 3] Nourishing cream

Nutritive creams were prepared according to the compositions listed in Table 8 below in a conventional manner.

Raw material name Content (% by weight) Purified water Balance glycerin 3.0 Butylene glycol 3.0 Liquid paraffin 7.0 Beta Glucan 7.0 Carbomer 0.1 Baekhwasa reed extract 3.0 Caprylic / capric triglyceride 3.0 Squalane 5.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Polysorbate 60 1.2 antiseptic Suitable amount incense Suitable amount Pigment Suitable amount Triethanolamine 0.1

[Formulation Example 4] Pack

Packs were prepared in a conventional manner according to the composition shown in Table 9 below.

Raw material name Content (% by weight) Purified water Balance glycerin 4.0 Polyvinyl alcohol 15.0 Hyaluronic acid extract 5.0 Beta Glucan 7.0 Allantoin 0.1 Baekhwasa reed extract 0.5 Nonyl phenyl ether 0.4 Polysorbate 60 1.2 antiseptic Suitable amount incense Suitable amount Pigment Suitable amount ethanol 6.0

[Formulation Example 5] Ointment

Ointments were prepared in a conventional manner according to the composition shown in Table 10 below.

Raw material name Content (% by weight) Purified water Balance glycerin 8.0 Butylene glycol 4.0 Liquid paraffin 15.0 Beta Glucan 7.0 Carbomer 0.1 Baekhwasa reed extract 1.0 Caprylic / capric triglyceride 3.0 Squalane 1.0 Cetearyl glucoside 1.5 Sorbitan stearate 0.4 Cetearyl alcohol 1.0 antiseptic Suitable amount incense Suitable amount Pigment Suitable amount Wax 4.0

[Formulation Example 6] Hair tonic

A hair tonic was prepared according to the composition shown in Table 11 by a conventional method.

Raw material name Content (% by weight) ethanol 50 menthol 0.02 glycerin 3 Salicylic acid 0.05 Baekhwasa reed extract 1.0 Preservatives, fragrances and pigments Suitable amount Purified water Balance

[Formulation Example 7] Hair lotion

Hair lotions were prepared in a conventional manner according to the composition shown in Table 12 below.

Raw material name Content (% by weight) Cetostearyl alcohol 2.0 EDTA 2Na 0.2 Hydroxyethyl cellulose 0.5 Mineral oil 5.0 Baekhwasa reed extract 1.0 Preservatives, fragrances and pigments Suitable amount Purified water Balance

[Formulation Example 8] Hair rinse and treatment

Hair rinses and treatments were prepared in a conventional manner according to the composition shown in Table 13 below.

Raw material name Content (% by weight) Propylene glycol 2.0 Cetyltrimethylammonium chloride 1.0 Cetyl alcohol 3.0 Stearyl alcohol 3.0 Mineral oil 0.5 Saitric Acid 0.2 Polydimethylsiloxane 1.0 Baekhwasa reed extract 1.0 Preservatives, fragrances and pigments Suitable amount Purified water Balance

Claims (6)

A cosmetic composition for improvement of underwater type (O / W) hair loss comprising an extract of Baekhwa exclusive use as an active ingredient,
The Baekhwasa reed extract is obtained by extracting Baekhwasaeol with ethanol and aging at 4 ~ 15 ℃ and then re-extracting with ethyl acetate.
The cosmetic composition according to claim 1, wherein the whitening agent extract is present in an amount of 0.01 to 20% by weight based on the total weight of the composition.
The cosmetic composition according to claim 1, wherein the white freckle extract inhibits 5-alpha reductase.
The cosmetic composition according to claim 1, wherein the white freckle extract is contained in an amount of 1% by weight or 10% by weight based on the total weight of the composition.
The composition of claim 1, wherein the composition is selected from the group consisting of fats, organic solvents, solubilizers, thickeners, gellants, softeners, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, At least one selected from the group consisting of nonionic emulsifiers, fillers, sequestering agents, chelating agents, preservatives, vitamins, wetting agents, oils, dyes, pigments, hydrophilic active agents, lipophilic active agents and lipid vesicles &Lt; / RTI &gt;
The composition of claim 1, wherein the composition is in the form of a gel, an emulsion, a suspension, a microemulsion, a microcapsule, a fine granule, a cream, a skin, a lotion, a powder, an ointment, a spray, a pack, a cone stick, Wherein the cosmetic composition is formulated into any one selected from the group consisting of hair, hair, hair shampoo, hair lotion, and aerosol.
A cosmetic product produced by the cosmetic composition for improving hair loss according to any one of claims 1 to 5.