KR20190134211A - A cosmetic composition for hair containing an extract of Spiraea prunifolia - Google Patents

Abstract

The present invention relates to a composition for preventing hair loss and promoting hair growth, which contains bridal wreath extract as an active ingredient. The present invention contains 0.0001 to 10% of bridal wreath extract as an active ingredient with respect to the total weight of a cosmetic composition for preventing hair loss. The composition for preventing hair loss: not only helps the proliferation of hair cells but also inhibits the expression of human SRD5A1 and SRD5A2 which are genes promoting the activation of dehydrotestosterone (DHT) by 5a-reductase; and reduces hair loss by increasing VEGF-A which is an angiogenesis-promoting factor and generating blood vessels in hair. Therefore, the present composition can be useful as a hair loss preventing agent for the prevention of baldness disease, alopecia areata, and masculine alopecia.

Description

Hair loss prevention and hair growth composition containing the extract as an active ingredient {A cosmetic composition for hair containing an extract of Spiraea prunifolia}

The present invention relates to a composition for preventing hair loss or promoting hair growth, containing a meadowsweet extract as an active ingredient.

Human hair is composed of about 150,000 pieces, and each hair repeats the process of growing and falling out through different hair cycles. The growth cycle of hair is divided into three stages: anagen, in which hair grows, catagen, which maintains hair after growth, and telogen, in which the hair papilla is contracted and hair follicles are gradually split and hair loss progresses. Repeat step 3 periodically (Herbal Extracts Induce Dermal Papilla Cell Proliferation of Human Hair Follicles, Ann Dermatol, 2015: 667-675). The hair growth cycle depends on internal factors such as family history, heredity, constitution, hormonal control, and external factors such as nutritional status, aging, surroundings, and stress.As hair growth progresses, the growth cycle is abnormally shortened and hair length is increased. You may notice shortening and thinning of the hair follicles.

The cause of hair loss is not only genetic, but also environmental factors. In recent years, hair loss caused by environmental factors is increasing, and these environmental factors are closely related to free radicals. Free radicals are oxidative oxygen produced by various metabolic processes. They are excessive due to environmental factors such as fatigue, poor diet, ultraviolet rays, chemicals, and stress. Oxidation promotes aging and reduces hair vitality. . Active oxygen binds to cholesterol and becomes lipid peroxide and adheres to the walls of blood vessels, which narrows the scalp blood vessels, blocks pores, reduces blood flow, making it difficult to supply nutrients to the hair roots, and attacks the cell membranes of the cells that make up the hair follicles. Causes hair loss by causing inflammation of the scalp. Therefore, in developing a hair loss treatment agent, the antioxidant ability to inhibit the generation of free radicals in the scalp and to remove or reduce the excess free radicals may be an important indicator.

In addition, one of the biggest causes of hair loss is male hormone, and testosterone, a testosterone, is converted to DHT (dehyrotestosterone) by the action of 5α-reductase in hair follicles, and the converted DHT is the androgen of the dermal papilla membranes in the frontal and head regions. When combined with the receptor, cell disruption signals are delivered to DNA of hair mother cells, resulting in cell death factors BMP, DKK-1, and TGF-β. The resulting cell necrosis factor attacks and destroys the hair cells, shortens the hair growth period and causes the degenerative stage to come early. 5α-reductase is mainly secreted by sebaceous gland type 1, lateral hair follicles of hair follicles and type 2 distributed in the dermal papilla. Type 2 enzymes are the main cause of hair loss. Therefore, if 5α-reductase can be inhibited or eliminated, androgenetic alopecia such as androgenetic alopecia can be prevented or treated.

In addition, external stress such as childbirth, disease, diet, blood circulation, and peroxidation have been reported to affect hair loss. In recent years, there has been a growing interest in hair loss due to the appearance of alopecia in women and women of low age, and hair loss is regarded as a disease, and various treatments for this are being released. ) And finasteride. Minoxidil, a representative product, acts on blood vessels, increases blood flow, promotes nourishment, promotes hair growth, and directly acts on hair follicles to induce hair growth effects, but it is cumbersome to apply it twice daily. Because it takes about 3 hours to show the effect of the scalp due to this, scalp itching, scalp irritation and other side effects, such as fluffy hair grows, but it is difficult to expect long hair growth effect. Finasteride, on the other hand, delays the progression of hair loss and induces hair loss by inhibiting DHT, a male hormone, but when it stops taking it back to its original condition, hair loss proceeds again, causing erectile dysfunction due to decreased libido in men. In women, side effects that cause birth defects are rarely reported, and their use is limited. As such, existing hair loss treatments, such as minoxidil and finasteride, are inhibited when they are discontinued. Therefore, hair loss treatments requiring long-term treatment are required to minimize side effects. Accordingly, it is necessary to develop a new natural material hair loss treatment agent that minimizes side effects that are not chemical treatments.

On the other hand, the poplar is a dicotyledonous plant of the Rosaceae family growing all over Korea, and it has been reported that young leaves, fruits and roots have been used in China as a diuretic, antidote, anti-inflammatory and analgesic agent in Korea. Inhibitory activity of plant extracts on nitric oxide synthesis in LPS-activated macrophages, Phytother.Res., 17 (5), 2003: 485-489, Pharmacognostical studies on the folk medicine, Kor.J. Pharmacogn. , 2012: 193-197).

Therefore, the present inventors have tried to alleviate the side effects and provide a high-efficacy hair loss treatment, as a result, the japonica extract promotes the growth of dermal papilla cells and inhibits the expression of an enzyme gene that induces the activation of DHT, a male hormone, to prevent hair loss and This invention was completed by confirming that it is effective in promoting hair growth.

KR 10-0998992 B1

The present invention has been made to solve the above problems, comprising the extract isolated from the meadowsweet as an active ingredient, and aims to provide a composition for preventing hair loss or promoting hair growth through human dermal papilla cell growth promotion and gene expression control. It is done.

The present invention provides a pharmaceutical composition for preventing hair loss and promoting hair growth or preventing hair loss and improving hair growth, comprising a crude extract of Japonica as an active ingredient, in order to achieve the above object. It is preferable to use a leaf, stem or a mixture of the two, and the crude extract is a fraction of 30% ethanol and 60% ethanol fraction after hot water extraction of the ethanol extract of the meadowsweet. More preferably, the 60% ethanol fraction is fractionated with 80% ethanol and then separated from the 60% ethanol fraction. Crude extracts reduce 5α-reductase gene expression and promote human papilla cell proliferation.

In another aspect, the present invention provides a composition in which the crude jaw extract is added in 0.0001 to 10% by weight relative to 100% by weight of the total composition.

As another example, the present invention comprises the steps of drying the leaves, stems or a mixture of the two of the poplars, followed by extraction with ethanol, filtration and concentration under reduced pressure; Suspending the concentrate with water and then repeatedly extracting twice each sequentially using purified water, 30% ethanol, 60% ethanol, and 80% ethanol to prepare a fraction of japonica corresponding to each of the solvents; It provides a method of producing a crude extract of japonica for hair loss prevention and hair growth comprising a; and step 3 of concentrating the 60% ethanol meadowsweet fraction prepared in step 2 under reduced pressure. More specifically, in the second step, the extraction was repeated two times with purified water, followed by repeated extraction twice with 30% ethanol, repeated extraction twice with 60% ethanol, and repeated extraction twice with 80% ethanol, followed by 60% ethanol fractions. Recover and proceed to Step 3.

The composition of the present invention is effective in promoting hair growth and hair loss as it affects the hair growth cycle by controlling the growth of human hair papilla cells and gene expression by including the extract of the japonica as an active ingredient, baldness disease, alopecia areata It can be usefully used as a pharmaceutical or cosmetic composition for the prevention, alleviation, treatment of.

Figure 1 shows the production process of (a) meadowsweet concentrate and (b) preparation of the meadowsweet fraction.
Figure 2 shows the chromatographic pattern separating the active ingredient from the 60% ethanol fraction of meadowsweet.
Figure 3 shows the papillary cells proliferation promotion and gene activity.
4 shows the test results for the gene expression level involved in the hair cycle.

EMBODIMENT OF THE INVENTION Hereinafter, this invention is demonstrated concretely.

The present invention provides a pharmaceutical composition for preventing hair loss and promoting hair growth or cosmetic composition for improving hair loss and hair growth, comprising crude extract of meadowsweet as an active ingredient.

The crude extract decreases 5α-reductase gene expression and is characterized by increasing the proliferation of human dermal papilla cells.

The japonica (Spiraea prunifolia) is a wild plant throughout most of Korea, the antioxidant effect (Korean Patent 10-1453609 B1, Korean Patent 10-1176526 B1) and anti-inflammatory activity (Korean J. Plant REs. 30 (4) ), 2017: 335-342). These, japonica has the effect of inhibiting the expression of human SRD5A1 and SRD5A2 genes that promote the activation of DHT by 5α-reductase, and increases blood vessel formation factors VEGF-A to generate blood vessels in the hair to cause hair loss It was confirmed that it can be mitigated.

More specifically, the present invention comprises the steps of preparing a meadowsweet extract by drying the leaves, stems or a mixture of the two and then adding ethanol, filtered and concentrated under reduced pressure; Suspension of the meadowsweet extract prepared in step 1 with water, and then purified water, 30% ethanol, 60% ethanol, 80% ethanol was added sequentially and repeated extraction twice each to prepare a fraction of the meadowsweet tree corresponding to each solvent 2 step; And 60% ethanol fractions of the meadowsweet fraction prepared in step 2 and concentrated under reduced pressure three steps.

In the first step, the japonica extract is preferably extracted at room temperature by 70% ethanol aqueous solution containing purified water.

In the present invention, the composition is a cosmetic, the cosmetic formulation is characterized in that it comprises a hair tonic, hair ampoule, hair gel, hair cream, hair lotion, hair skin, hair conditioner, hair shampoo, hair rinse.

In addition, the compositions of the present invention may be prepared in conventional formulations such as creams, lotions, tonics, solutions, suspensions, emulsions, skins, ampoules, and the like, further containing a cosmetically acceptable carrier. The composition of the present invention usually contains a base, and other components generally used as cosmetic raw materials may be appropriately blended as necessary. The base of the composition of the present invention includes purified water, ethanol, glycerin, butylene glycol, biotin, sodium hyaluronate, and examples of other components to be incorporated into the composition of the present invention include surfactants, emulsifiers, solubilizers, Thickeners, preservatives, antioxidants, fragrances, and the like, but are not limited thereto.

The composition of the present invention may include a component that may serve to supply nutrients to hair follicles in addition to the above components, or hair growth promoting auxiliary components that are commonly used, and include growth factors, vitamins, peptides, extracts, and the like. For example, but is not limited thereto. The amount thereof is preferably 0.0001 to 5% by weight of the total composition, particularly preferably 0.001 to 1% by weight.

The composition of the present invention can be used by the method of applying directly to the hair or scalp as a skin cosmetic formulation, and the hair to which the composition of the present invention is applied is the hair root and hair follicles of the hair, and the hair follicles and hair follicles throughout the body such as hair and eyebrows. Means a site.

The content of the composition according to the present invention may be appropriately determined in consideration of sex, age, alopecia, hair condition, and the like. 60% ethanol fraction with human dermal papilla cell proliferation promoting and gene expression control function can be added as a raw material of cosmetics which is an external preparation for skin. At this time, the 60% ethanol fraction is preferably added at 0.0001 to 5% by weight, more preferably 0.001 to 1% by weight based on the dry weight of the skin external preparation composition.

Hereinafter, preferred examples are provided to aid in understanding the present invention. However, the following examples are merely provided to more easily understand the present invention, and the contents of the present invention are not limited by the examples.

Preparation Example 1 Preparation of the Japonica Extract

10 kg of the leaves and stems of the maple tree were dried at room temperature for 168 hours, and 70% ethanol was added to 6.8 kg of the dried leaves and stems of the maple tree and then extracted by standing at room temperature for 168 hours. Then, the resultant was filtered and concentrated under reduced pressure to obtain 250 g of Maple Japonica 70% ethanol extract. (See Figure 1 (a))

[Preparation Example 2] Preparation spirea trees crude extract

Sufficiently suspended in the 70% ethanol extract prepared in Preparation Example 1 with water 10 times the purified water, 7 times the volume 30% ethanol, 5 times the volume 60% ethanol, 4 times the volume 80% ethanol sequentially The extract was added twice, and each extracted twice, water layer, 30% ethanol layer, 60% ethanol layer, 80% ethanol layer was separated, and the poplar fraction corresponding to each solvent was obtained. (See Figure 1 (b))

[Test Example 1] Growth of papilla cells and evaluation of gene expression regulation

Dermal palilla cells are the key cells responsible for hair growth. The dermal papilla is connected with capillaries to supply oxygen and nutrients to grow hair. The dermal papilla cells that are renoured from the dermal papilla divide and proliferate to produce keratin proteins. Hair loss is caused by androgen and free radicals stimulating the dermal papilla cells, so that the modulo cells secrete hair follicle-breaking substances or prevent the growth of hair growth factors.

Accordingly, in order to confirm the effect of the extract of the present invention on the growth promotion and gene expression control of dermal papilla cells, human dermal papilla cells (HDPC, purchased from Cefobio) were prepared in 1 × 10 ⁴ cells / well in a 96 well plate. After seeding with the preparations 1 and 2, the extract and fractions of the poplar tree obtained in the concentrations according to Table 2 were treated using a serum-free medium. After incubation at 37 ° C. for 24 hours in a 5% CO ₂ incubator, the absorbance was measured at 450 nm using the WST-1 reagent.

Treatment concentration (㎍ / ㎖) Incubation time (hr) Meadowsweet Extract (in DMSO)
2, 10, 50, 100, 200
24 Meadowsweet 30% Ethanol Fraction (in DMSO) Meadowsweet 60% Ethanol Fraction (in DMSO)

As a result, looking at Figure 3, even if all three samples were treated with each concentration and cultured little cytotoxicity was observed, when the 60% ethanol fraction treated with 100 ㎍ / ㎖ showed the highest survival rate relative to human The results of promoting dermal papilla cell proliferation were confirmed. When the 60% ethanol fraction was treated at 200 ㎍ / mL, the survival rate was slightly lower. This cytotoxicity result was that osmotic pressure or acidity was more dependent on the effect of 60% ethanol fraction on the culture than the 60% ethanol fraction itself. The effect on the cells is expected. Through the above results, it was confirmed that the Japonica fraction promotes the growth of human dermal papilla cells and positively affects gene expression control.

On the other hand, to determine the effect of each fraction of meadowsweet extract in human dermal papilla cells, the gene expression level involved in the hair cycle was checked.

[Test Example 2]

Human dermal papilla cells were seeded at 1.5x10 ^ 5cells / well and incubated in a CO2 incubator for 24 hours, then each sample was treated at 50ug / ml concentration with medium replacement with Serum free DMEM and then incubated in a CO2 incubator for 24 hours. The cells were then disrupted to obtain RNA. RT (Reverse transcription_reverse transcription) was performed to obtain cDNA using this RNA as a template. Primer of each gene was prepared by using the cDNA template thus prepared, followed by PCR (Polymerase chain reaction_polymerase chain reaction). After PCR, electrophoresis was performed on 1.5% agarose gel and detected by UV lamp.

 Experimental results show that the hSRD5A1 and hSRD5A2 genes were reduced in the cells treated with 60% ethanol fraction, and that the hBAX and hVEGF-A genes increased to affect the hair cycle, which in turn is an indirect basis for alleviating hair loss. 4)

The pharmaceutical composition according to the present invention may include 0.1 to 99% by weight of the crude extract based on the total weight of the composition.

Pharmaceutical compositions comprising the crude extract of the present invention may further comprise suitable carriers, excipients and diluents commonly used in the manufacture of compositions.

The pharmaceutical dosage forms of the crude extracts of the present invention may be used in the form of their pharmaceutically acceptable salts, or may be used alone or in combination with other pharmaceutically active compounds, as well as in a suitable collection.

The pharmaceutical composition comprising the crude extract according to the present invention may be prepared in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral formulations, external preparations, suppositories, and sterile injectable solutions, respectively, according to a conventional method. It can be formulated and used in the form.

Carriers, excipients and diluents that may be included in the composition comprising the crude extract include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, Calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil.

When formulated, diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants are usually used.

Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, which may comprise at least one excipient such as starch, calcium carbonate, sucrose in the crude extract. ) Or lactose, gelatin and the like are mixed. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used.

Liquid preparations for oral administration include suspensions, solvents, emulsions, and syrups, and may include various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, in addition to commonly used simple diluents such as water and liquid paraffin. have.

Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, suppositories. As the water-insoluble and suspending agents, propylene glycol, polyethylene glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate and the like can be used. As the base of the suppository, witepsol, macrogol, tween, cacao butter, laurin butter, glycerogelatin and the like may be used.

The preferred dosage of the crude extract of the present invention depends on the condition and weight of the patient, the extent of the disease, the form of the drug, the route of administration and the duration, and may be appropriately selected by those skilled in the art. However, for the preferred effect, the crude extract of the present invention is preferably administered at 0.0001 to 100 mg / kg, preferably 0.001 to 100 mg / kg. Administration may be administered once a day or may be divided several times. The dosage does not limit the scope of the invention in any aspect.

Drug Example 1: Powder  Produce

Maple Extract 20 mg

Lactose 100 mg

Talc 10 mg

The above ingredients were mixed and filled in airtight cloth to prepare a powder.

Pharmaceutical Example 2: Preparation of Tablets

Meadowsweet Extract 10 mg

100 mg corn starch

Lactose 100 mg

2 mg magnesium stearate

After mixing the above components was prepared by tableting according to the conventional tablet manufacturing method.

Cosmetic Formulation example  3. Hair Tonic Manufacturer

Hair tonic was prepared according to a conventional method in the amounts shown in Table 3 below.

content (%) Purified water 27.20 Panthenol 1.00 Maple Tree Extract 1.00 Niacinamide 2.00 Sphinginine 0.10 Capryloylsalicylic acid 0.20 ethanol 65.00 Fiji-60 Hydrogenated Castor Oil 0.50 Butylene Glycol 3.00

Cosmetic Formulation example  4. Hair ampoule  Produce

To prepare a hair ampoule according to the conventional method to the content shown in Table 4.

content (%) Purified water 96.4228 Cooper Tripeptide-1 0.0070 Sodium hyaluronate 0.4000 Biotin 0.1000 Arginine 0.0700 Oligopeptide-1 0.0001 Oligopeptide-3 0.0001 Maple Tree Extract 3.0000

The present invention has been described above by way of example, and those skilled in the art will appreciate that various modifications may be made without departing from the essential characteristics of the present invention. Accordingly, the embodiments disclosed herein are not intended to limit the present invention but to describe the present invention, and the spirit and scope of the present invention are not limited by these embodiments. The protection scope of the present invention should be interpreted by the following claims, and all the technologies within the equivalent scope should be interpreted as being included in the scope of the present invention.

Claims (8)

A pharmaceutical composition for preventing hair loss and promoting hair growth, which comprises a crude extract of Japonica as an active ingredient.
The pharmaceutical composition according to claim 1, wherein the maple tree is a leaf, a stem, or a mixture of the two.
According to claim 1, wherein the crude extract is a pharmaceutical composition, characterized in that the fraction of 30% ethanol fraction 60% ethanol after extracting the hot water ethanol extract of meadowsweet
The pharmaceutical composition according to claim 3, wherein the crude extract is a 60% ethanol fraction separated from the 60% ethanol fraction with 80% ethanol.
The method of claim 1,
Crude extract is a pharmaceutical composition, characterized in that to reduce the expression of 5α-reductase gene
The pharmaceutical composition of claim 1, wherein the crude extract of Japonica is added in an amount of 0.0001 to 10% by weight based on 100% by weight of the total composition.
Hair Loss Relief and Hair Growth Enhancement Composition
Drying the leaves, stems, or a mixture of the two of the poplars, followed by extraction with ethanol, filtration and concentration under reduced pressure;
Suspending the concentrate with water and then repeatedly extracting twice each sequentially using purified water, 30% ethanol, 60% ethanol, and 80% ethanol to prepare a fraction of japonica corresponding to each of the solvents;
And a step 3 for concentrating the 60% ethanol meadowsweet extract prepared in step 2 under reduced pressure; and a method for preparing a crude extract for preventing hair loss and promoting hair growth.

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