KR20170113487A - Hair growth activating composition - Google Patents

Abstract

The present invention provides a hair loss preventing and hair growth promoting composition containing refuge as an active ingredient.

Description

HAIR GROWTH ACTIVATING COMPOSITION < RTI ID = 0.0 >

More particularly, the present invention relates to a hair growth inhibitor composition containing, as an active ingredient, a refining agent having an excellent effect of shortening the period of transition from a resting period to a growing period in the hair growth period as an active ingredient, .

The human hair has about 100,000 to 150,000 hairs, and each hair has a different cycle and grows through anagen, catagen, and telogen. This cycle repeats over 3-6 years, with an average of 50-100 hairs per day dropping 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 hair loss have been discussed, such as male hormone excess, seborrheic scalp, stress, obesity, peroxidation, and bacterial dysfunction. However, the cause of hair loss has not been clarified to date. Recently, the number of people suffering from hair loss due to changes in diet and stress due to social environment has been increasing, and the age of women has also been lowered. Is also increasing.

Recent studies have shown that dihydrotestosterone, a reduced form of androgen, a male hormone, is a major factor in hair loss. Testosterone, a male hormone, is converted to dihydrotestosterone by the action of 5α-reductase (5α-reductase). It is known that hair follicles in hair loss patients have high 5α-reductase activity and thus cause hair loss.

In order to cure the cause of such hair loss, Merck has developed and commercialized pinasteride as a drug that inhibits the action of 5α-reductase to inhibit the production of dihydrotestosterone, but various side effects have been reported.

Therefore, in the present invention, a variety of compounds were tested to see if they had the effect of inhibiting the activity of 5α-reductase, which promotes the production of dihydrotestosterone, thereby developing a composition having the effect of preventing hair loss and promoting hair growth.

SUMMARY OF THE INVENTION Accordingly, the present invention has been made in order to solve the above-mentioned problems, and its object is to provide a composition which effectively inhibits 5α-reductase causing hair loss, thereby preventing hair loss and promoting hair growth.

The technical problem of the present invention as described above is achieved by the following means.

(1) A hair growth inhibitor composition which contains refuge as an active ingredient.

(2) In the above (1)

Wherein the content of the refuse is 0.001 to 10% by weight based on the total weight of the composition.

(3) In the above (1)

A pine needle extract, a pine needle extract, a fir leaf extract, and a cedar leaf extract.

(4) In the above (1)

A hair growth inhibitor composition, comprising:

(5) In the above (1)

Wherein the extract comprises 1 to 5% by weight of a mixed extract having a weight ratio of 1: 3 to 3: 1.

The composition according to the present invention can be effectively used as a composition for preventing hair loss or promoting hair growth by effectively inhibiting 5a-reductase that causes hair loss.

The hair growth inhibitor composition according to the present invention is characterized by containing pinane (Formula 1 or 2) as an active ingredient.

(One)

(2)

Hereinafter, the present invention will be described in detail.

The evacuation according to the present invention may be carried out by separating and purifying the leaves of coniferous trees using a predetermined solvent, or by purchasing the form of synthesized or commercially available finished products.

When an extraction method using a solvent is used, extraction, concentration and purification processes are performed.

[Extraction process]

First, softwood leaves are ground and extracted with 5 to 10 times of hexane at room temperature for 2 to 5 days, followed by filtration using 1 μm and 0.5 μm filter paper to obtain an extract.

[Concentration Process]

Hexane remaining in the extract obtained through the extraction step is reduced in pressure and concentrated to obtain a concentrated liquid at a high concentration.

[Purification step]

100 to 200 ml of ethyl acetate is added to the concentrate obtained through the concentration step, and 100 to 200 ml of purified water is added to the concentrate.

The washed organic layer is washed twice with 1N NaOH and the pH is neutralized with 1N HCl. Then, the organic layer is washed once with water, and then the organic layer is washed with a saturated sodium chloride solution (Brine). The finally obtained organic layer is concentrated in a round bottom flask and placed in a vacuum distillation apparatus. The undiluted concentrate is reduced in pressure and purified by ordinary distillation at an external temperature of 80 캜, and the sample is distilled at a steam temperature of about 60 캜. Primary distillation Purification of the distillation product is carried out in a second distillation under the same conditions to obtain refined pine (Pinane) in high purity.

The hair removal composition containing the refuse of the present invention as an active ingredient can be used as an external preparation for skin, such as a paste, cream, gel, foundation, spray, essence, pack, soap, patch, spray, ointment, It may be manufactured by using a composition in the form of an external preparation for skin, such as, but not limited to, a skin irritant, an irritant, a lotion, a liniment, a pasta or a cataplasm.

When the formulation of the present invention is a paste, cream or gel, animal fiber, plant fiber, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide may be used as the carrier component .

When the formulation of the present invention is a foundation or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as the carrier component, and in the case of spraying additionally, chlorofluorohydrocarbons, propane / Propane or dimethyl ether.

In the case of the solution or emulsion of the present invention, a solvent, a solvent or an emulsifier is used as a carrier component, and examples thereof include water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, , 3-butyl glycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan fatty acid esters.

When the formulation of the present invention is a suspension, a carrier such as water, a liquid diluent such as ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Cellulose, aluminum metahydroxide, bentonite, agar or tracant, etc. may be used.

When the formulation of the present invention is an interfacial active agent-containing cleansing, the carrier component may include aliphatic alcohol sulfate, aliphatic alcohol ether sulfate, sulfosuccinic acid monoester, isethionate, imidazolinium derivative, methyltaurate, sarcosinate, fatty acid amide Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, linolenic derivatives or ethoxylated glycerol fatty acid esters.

When the hair growth inhibitor composition according to the present invention is to be manufactured into cosmetics, the cosmetic composition may include a composition selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymer peptides, polymer polysaccharides, sphingolipids and seaweed extracts.

The hair growth inhibitory composition according to the present invention may be blended with other components which are usually added to cosmetics, if necessary, in addition to the above components. Examples of the compounding ingredient that can be added include a stabilizer, a preservative, a moisturizer, an emollient, a surfactant, an organic and inorganic pigment, an organic powder, an ultraviolet absorbent, a preservative, a bactericide, an antioxidant, a plant extract, a pH adjuster, , A blood circulation accelerator, a cold agent, an antiperspirant agent, and purified water.

In addition, any of the above components may be blended within the range that does not impair the objects and effects of the present invention, but is preferably 0.01 to 5% by weight, And preferably 0.01 to 3% by weight.

In the hair growth inhibitor composition according to the present invention, the blending amount of the refuse according to the present invention is preferably 0.0001 to 20% by weight, more preferably 0.001 to 10% by weight based on the total weight of the composition. There is a possibility of deterioration. If it exceeds 20% by weight, it is difficult to expect an increase in the effect even if it is blended.

The hair extract composition according to the present invention may be prepared by mixing 1 to 3% by weight of a phytase or 40 to 60 ° Brix of a hot water extract of Bombyx mori and an extract of hot water of a Bombyx mori extract in a weight ratio of 1: 3 to 3: 5% by weight, it is possible not only to enhance the hair growth promoting activity of the refuge, but also to stably maintain the activity for a longer period of time.

The pharmaceutical dosage forms of the present invention may also be used in the form of their pharmaceutically acceptable salts and may be used alone or in combination with other pharmacologically active compounds as well as in suitable aggregates.

Desirable dosages of the refuse of the present invention vary depending on the condition and the weight of the user, the degree of symptoms, the formulation, the route of administration and the period of time, but can be appropriately selected by those skilled in the art. However, for the desired effect, the compound of the present invention is preferably administered at 0.00001 to 1000 mg / kg per day, preferably 0.001 to 10 mg / kg per day. The administration may be carried out once a day or divided into several times. The dose is not intended to limit the scope of the invention in any way.

Hereinafter, the present invention will be described in more detail with reference to Examples. It is to be understood, however, that these examples are provided so that the scope of the present invention is not limited thereto.

[Example 1]

The pine needle was grinded, extracted with hexane of 5 times at room temperature for 3 days, and filtered successively with 1 탆 and 0.5 탆 filter paper to obtain an extract. Hexane remaining in the extract obtained through the extraction step was reduced in pressure and concentrated to obtain a concentrated liquid at a high concentration. 100 ml of ethyl acetate was added to the concentrate obtained through the above-mentioned concentration step, followed by washing with 100 ml of purified water. The washed organic layer was washed twice with 1N NaOH and the pH was neutralized with 1N HCl. Then, the organic layer was washed once with water, and then the organic layer was washed with a saturated sodium chloride solution (Brine). The finally obtained organic layer was concentrated in a round bottom flask and placed in a vacuum distillation apparatus. The non-purified concentrate was reduced in pressure and purified by ordinary distillation at an external temperature of 80 ° C, and the sample was distilled at a steam temperature of 60 ° C. The primary distillation purified material thus obtained was subjected to a second distillation purification under the same conditions to obtain high purity pinane (purity: 98%).

[Example 2]

The fir leaves were grinded and extracted with 5 times of hexane at room temperature for 3 days, and filtered with 1 ㎛ and 0.5 ㎛ filter paper to obtain an extract. Hexane remaining in the extract obtained through the extraction step was reduced in pressure and concentrated to obtain a concentrated liquid at a high concentration. 100 ml of ethyl acetate was added to the concentrate obtained through the above-mentioned concentration step, followed by washing with 100 ml of purified water. The washed organic layer was washed twice with 1N NaOH and the pH was neutralized with 1N HCl. Then, the organic layer was washed once with water, and then the organic layer was washed with a saturated sodium chloride solution (Brine). The finally obtained organic layer was concentrated in a round bottom flask and placed in a vacuum distillation apparatus. The non-purified concentrate was reduced in pressure and purified by ordinary distillation at an external temperature of 80 ° C, and the sample was distilled at a steam temperature of 60 ° C. The primary distillation purified material thus obtained was subjected to a second distillation purification under the same conditions to obtain high purity pinane (purity: 98%).

[Example 3]

The leaves of the perennials were grinded and extracted with 5 times of hexane at room temperature for 3 days and filtered sequentially using 1 ㎛ and 0.5 ㎛ filter paper to obtain an extract. Hexane remaining in the extract obtained through the extraction step was reduced in pressure and concentrated to obtain a concentrated liquid at a high concentration. 100 ml of ethyl acetate was added to the concentrate obtained through the above-mentioned concentration step, followed by washing with 100 ml of purified water. The washed organic layer was washed twice with 1N NaOH and the pH was neutralized with 1N HCl. Then, the organic layer was washed once with water, and then the organic layer was washed with a saturated sodium chloride solution (Brine). The finally obtained organic layer was concentrated in a round bottom flask and placed in a vacuum distillation apparatus. The non-purified concentrate was reduced in pressure and purified by ordinary distillation at an external temperature of 80 ° C, and the sample was distilled at a steam temperature of 60 ° C. The first distillation purified material thus obtained was subjected to a second distillation purification under the same conditions to obtain a high purity distillate (purity: 97%).

[Example 4]

A mixture was prepared by mixing the refuse obtained in Example 1 and the physiside in a weight ratio of 1: 1.

[Example 5]

To the concentrated concentrate obtained in Example 1 was added 2% by weight of a mixed extract having a ratio of 1: 3 by weight of a bifid leaf extract and an extract of an extract of 50 Brix.

[Experimental Example 1] Evaluation of 5α-reductase (5α-reductase) inhibitory effect on evacuation

Dermal papilla cells (DPCs) were dispensed into a 24-well plate at a concentration of 5 × 10 ⁵ / ml in an amount of 1 ml, cultured for 24 hours, and then the evacuation obtained according to the method described in Examples 1 to 3, The mixture of physeide was treated with 50 μg / ml, 10 μg / ml and 0 μg / ml in each well and stimulated with 50 nM testersterone (DMSO dissolved) 1 hour later. After 24 hours of incubation, the supernatant was discarded to obtain a DPCs pellet. Dihydrotestosterone (DHT) (DB52021, Hamburg, Germany) content was measured by enzyme-linked immuno-sorbent assay. Rabbit Anti-DHT Antibody Coated dihydrotestosterone (DHT) ELISA 100 μL of DPCs cell pellet was dispensed into microtiter strips, and 25 μL of DHT antiserum was added to all wells. After 15 hours of reaction at 8 ° C, the cells were washed three times . 100 μl of DHT-HRP enzyme conjugate was added to all wells and reacted at room temperature for 30 minutes on shaker and washed three times. 100 μL of the substrate was dispensed, reacted on a shaker for 20-30 minutes at room temperature, treated with 100 μL of a stop solution, and the absorbance was measured at 450 nm. The amount of DHT produced was expressed as the absorbance (repeated three times) (%), And the results are shown in Table 1. The results are shown in Table 1. < tb >< TABLE >

The inhibitory effects of 5α-reductase on evacuation of Examples 1 to 4 sample Sample concentration (/ ml) Inhibition rate (%) Control group - - Example 1 10 22 50 48 Example 2 10 23 50 46 Example 3 10 22 50 46 Example 4 10 28 50 52

As can be seen from the results shown in Table 1, the 5α-reductase inhibition rate of the mixture of refinement and physiside extracted and purified in each Example is excellent.

[Experimental Example 2] Evaluation of inhibitory effect of 5α-reductase (5 alpha-reductase) on the extract concentrate

The results of evaluating 5α-reductase (5-alpha-reductase) inhibitory effects by the same conditions and methods as in Experimental Example 1 using the concentrates obtained in Examples 1 to 3 and Example 5 are shown in Table 2 below same.

The 5α-reductase inhibition rate of the extract concentrates of Examples 1 to 3 and Example 5 sample Sample concentration (/ ml) Inhibition rate (%) Control group - - Example 1 10 8 50 12 Example 2 10 8 50 11 Example 3 10 9 50 13 Example 5 10 11 50 15

As can be seen from the results shown in Table 1, the 5α-reductase inhibition rate of the concentrate obtained in each of the Examples was also excellent.

[Experimental Example 3] Evaluation test of induction of hair growth during evacuation

In order to evaluate the induction effect of hair growth, 7 - week - old mice (C57BL / 6, female) were used. First, the hair of the back part of the mouse was removed using an electric razor, and each mouse was weighed and divided into five to distribute the weight uniformly. At the epilating site, an excipient, a control drug and a test drug were applied. In this case, 95% ethanol was used as a buccal medicine, 2% minoxidil as a control drug, reflux of Examples 1 to 3 and mixture Were each diluted with 95% ethanol to a final concentration of 0.5%. It was applied once a day to the dorsal area per mouse individual well with a brush.

The overall treatment efficacy was judged to be four stages of improvement (++), improvement (+), a little improvement (ㅁ), and no response (-) compared to those before the administration Respectively.

Evaluation results of stimulation of induction of hair growth sample Marie ++ + - Addiction - - One 4 Control agent (Minoxidil 5%) - 2 2 One Example 1 3 2 - - Example 2 3 2 - - Example 3 3 2 - - Example 4 4 One - -

As shown in the above Table 3, it can be seen that the mouse having the evacuation obtained in each Example and the mixture of Example 4 applied rapidly to the epilating site.

[Experimental Example 4] Experimental evaluation of induction promoting action of hair growth on extract concentrate

The concentrate obtained in each of Examples 1 to 3 and Example 5 was used to evaluate the hair growth promoting action by the same conditions and methods as in Experimental Example 3, and the results are shown in Table 4 below.

Evaluation results of stimulation of induction of hair growth sample Marie ++ + - Addiction - - One 4 Control agent (Minoxidil 5%) - 2 2 One Example 1 - 3 2 - Example 2 - 3 2 - Example 3 - 3 2 - Example 5 One 4 - -

As can be seen from the results of Table 4, it can be seen that the concentrate obtained by extracting in each Example is also excellent in promoting hair growth period induction.

While the present invention has been particularly shown and described with reference to exemplary embodiments thereof, it will be understood by those skilled in the art that various changes and modifications may be made without departing from the spirit and scope of the invention as defined in the appended claims. It can be understood that

Claims (1)

0.0001 to 10% by weight of refuse,
A hair growth inhibitor composition comprising 1 to 5% by weight of a mixed extract having a weight ratio of 1: 3 to 3: 1 of a bovine leaf extract and an extract of bovine leaf of 40 to 60 ° Brix as an active ingredient.