JPH06211632A - Hair-growing agent - Google Patents

Abstract

PURPOSE:To obtain a hair-growing agent exhibiting remarkable effect as a trichogen and for the treatment of alopecia such as male alopecia and alopecia areata. CONSTITUTION:This hair-growing agent contains kinetin as an active component. A synergistic trichogenic effect can be attained by using kinetin in combination with one or more compounds selected from cyclic adenosine monophosphate, its derivative, cyclic guanosine monophosphate, its derivative, forskolin, carpronium chloride, pentadecanoic acid glyceride, minoxidil, female hormone, adrenocorticotropic hormone, peripheral vasodilator, cytotonic agent and photosensitive material.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair restorer having an excellent effect on promoting hair growth.

[0002]

2. Description of the Related Art Conventionally, various hair-growing agents have been used for preventing and treating baldness and thinning hair. Generally, the ingredients contained in hair restorers are mainly scalp blood circulation promotion, scalp cleaning, anti-inflammatory and sterilization, activation of enzymes in hair follicles and cells around hair follicles, improvement of energy metabolism of hair mother cells. ,
The purpose is to suppress male hormone action in the scalp.

[0003] For example, carpronium chloride, vitamin E, capsicum extract, assembly extract, garlic extract, etc. are intended to increase the blood flow in the hair follicle portion by the action of peripheral vasodilator and activate hair matrix cells. , Antibacterial agents such as hinokitiol and resorcin, and anti-inflammatory agents such as glycyrrhizin and allantoin are known to contribute to hair loss. To suppress inflammation of the scalp part, dandruff and sebum caused by bacteria that cause inflammation Vitamin A group, vitamin B group, biotin, pantothenic acid derivative, and other vitamins for the purpose of activating the enzymes of hair matrix cells and promoting hair synthesis. Female hormones such as estradiol and ethinyl estradiol are considered to be the main causes of male pattern baldness. It has been used to inhibit the action.

[0004]

However, although the above-described conventional hair-growth agent components have some hair-growth-promoting effects and hair loss-preventing effects, none of them are satisfactory, and hair-growth-promoting effects are particularly high. The effect was insufficient.

[0005]

OBJECTS OF THE INVENTION It is therefore an object of the present invention to provide a hair-growth agent which, when applied to the scalp, can exert an excellent effect in promoting hair growth.

[0006]

The present invention has been proposed in order to achieve the above-mentioned object, and has been conventionally used as a plant growth regulator for plant growth.
As can be seen in Japanese Patent No. 9646, kinetin, which is known to be used as a cosmetic for moisturizing dry skin, has a surprising finding that it has a hair-growing effect. It was completed in.

[0007] That is, according to the present invention, there is provided a hair restorer characterized by containing kinetin as an active ingredient.
The kinetin includes cyclic adenosine monophosphate and its derivative, cyclic guanosine monophosphate and its derivative, forskolin,
The hair-growth effect is further enhanced by the combined use of one or more compounds selected from the group consisting of carpronium chloride, pentadecanoic acid glyceride, minoxidil, female hormones, vitamins, peripheral vasodilators, cell activating agents, and photosensitizers. It will be outstanding.

[0008]

[Detailed Description of the Invention] The cause of alopecia has not been elucidated in detail, but it is impaired in blood circulation around the papillae and follicles, androgen action, inheritance, nutritional disorders, endocrine disorders, mental stress, etc. Are said to be involved. The present inventors have conducted various studies on many compounds in order to analyze various factors of the above-mentioned alopecia and eliminate them. As a result, as described above, kinetin, which is conventionally used as a growth regulator for plant growth and is known to be used as a cosmetic to moisturize dry skin, has an excellent effect on promoting hair growth, Further, they have found that it also has a hair loss treatment effect on alopecia such as androgenetic alopecia and alopecia areata, and completed the present invention.

Kinetin is a derivative of purine and is also called 6-furfurylaminopurine. The kinetin of the present invention is chemically synthesized and obtained, for example, by a reaction between adenine and furfuryl chloride, a reaction between 6-methylmercaptopurine and furfurylamine, and the like. Kinetin can also be obtained, for example, by high-pressure heating a natural product containing a large amount of DNA such as herring sperm. As described above, the kinetin of the present invention can be used either as a substance synthesized by a chemical synthesis method or as a high pressure heated product of a natural product containing a large amount of DNA.

Further, kinetin is cyclic adenosine monophosphate and its derivative, cyclic guanosine monophosphate and its derivative, forskolin, carpronium chloride, pentadecanoic acid glyceride, minoxidil, female hormone, adrenocortical hormone, vitamins. The combined use of one or more compounds selected from the group consisting of a peripheral vasodilator, a cell activating agent, and a photosensitizer can further enhance the effects of promoting hair growth and treating alopecia.

Derivatives of cyclic adenosine monophosphate (c-AMP) and cyclic guanosine monophosphate (c-GMP) include dibutyryl cyclic adenosine monophosphate (dbc-AMP) and 8-bromo. Cyclic adenosine monophosphate (8-Br-c-AMP),
Examples thereof include dibutyryl cyclic guanosine monophosphate (dbc-GMP) and 8-bromocyclic guanosine monophosphate (8-Br-c-GMP).

Examples of female hormones include estradiol and its ester, estrone, ethinyl estradiol, diethylstilbestrol, and hexstrol.

As the corticosteroid, cortisone,
Hydrocortisone, prednisolone, prednisone,
Examples thereof include 9-α-hydrofluorocortisone.

As vitamins, vitamin A acid, 13
-Vitamin A such as cis retinoic acid and etretinate
Group, vitamin E, vitamin E nicotinate, vitamin E
Examples thereof include vitamin E group such as acetate, vitamin B group such as nicotinic acid, nicotinic acid amide and benzyl nicotinate, pantothenic acids such as pantothenic acid, pantothenyl alcohol, and pantothenyl ethyl alcohol, and biotin.

Examples of the peripheral vasodilator include ginger tincture, capsicum tincture, cepharanthin, life-prolonging herbs, ginseng extract and the like.

As the cell activating agent, sea bream extract, garlic extract, carrot extract, rosemary extract,
Aloe extract, placenta extract, bamboo shoot carrot extract, ginger, safflower, ougi, peach kernel, bone replenisher, toki, senkyu,
An example is a crude drug such as Danshen.

The photosensitive elements are a photosensitive element 101 and a photosensitive element 2.
01, the photosensitive element 301, and the photosensitive element 401 can be illustrated.

The external preparation for hair of the present invention includes pharmaceuticals, quasi-drugs and cosmetics, and its dosage forms include various externally applicable forms such as cream, lotion, emulsion, ointment, gel and hair. It can be used by formulating it into a known form such as tonic, hair liquid, liniment, hair rinse, hair shampoo, hair treatment, hair conditioner, aerosol and mousse, and its base is any liquid or solid form acceptable for hair application. A wide range of raw materials can be used. At that time, if necessary, within a range that does not impair the hair-growing effect of kinetin, a known anti-hair graying agent, bactericidal anti-inflammatory agent, fragrance, stabilizer, coloring agent, ultraviolet absorber, antioxidant, moisturizer, thickener It is also possible to add various additives such as.

Examples of bactericidal anti-inflammatory agents include isopropylmethylphenol, diphenhydramine hydrochloride, glycyrrhizic acid derivative, hinokitiol, benzoate, salicylate, sorbate, dehydroacetate, paraoxybenzoate, 2,4,4. '-Trichloro-2'
-Hydroxydiphenyl ether, 3,4,4'-trichlorocarbanide, benzalkonium chloride, resorcin, ethanol, undecylenic acid and the like can be exemplified.

Examples of the stabilizer include chelating agents such as ethylenediaminetetraacetate, pyrophosphate, hexametaphosphate, citrate, tartaric acid and gluconic acid.
Examples of pH adjusting agents such as sodium hydroxide and potassium hydrogen phosphate can be given.

Examples of the ultraviolet absorber include 4-methoxybenzophenone, octyldimethylparaaminobenzoate, ethylhexylparamethoxycinnamate,
Titanium oxide, kaolin, talc, etc. can be illustrated.

Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, propyl gallate and the like.

Examples of moisturizers include polyhydric alcohols such as glycerin, propylene glycol, 1,3 butylene glycol, sorbitol, mannitol, polyethylene glycol and dipropylene glycol, NMF such as amino acids, sodium lactate and sodium pyrrolidonecarboxylate. Ingredients, hyaluronic acid, collagen, elastin, chondroitin sulphate, dermatan sulphate, fibronectin, ceramides, heparin-like substances, water-soluble polymeric substances such as chitosan, sasanishiki extract, Cordyceps sinensis,
Duke extract etc. can be illustrated.

Further, as the thickener, for example, sodium alginate, xanthan gum, aluminum silicate, quince seed extract, tragacanth gum, starch,
Examples thereof include natural polymer substances such as kefiran, semi-synthetic polymer substances such as methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, soluble starch and cationized cellulose, and synthetic polymer substances such as carboxyvinyl polymer and polyvinyl alcohol.

The amount of kinetin, which is an active ingredient of the hair restorer of the present invention, may be appropriately changed depending on the degree of symptoms, dosage form and the like, but is usually about 0.001 to 20% by weight, preferably 0.1 to. About 10% by weight is added to the formulation. The amount of the component used in combination with kinetin is usually about 0.01 to 20% by weight, preferably about 0.1 to 10% by weight.

[0026]

[Examples] Next, formulation examples of the hair-growth agent of the present invention and test examples of its effect will be shown, but these do not limit the present invention at all. In the prescription examples, "appropriate amount" means an amount that makes the total prescription amount 100% by weight.

<Formulation Example 1> Hair cream (% by weight) A Liquid paraffin 10.0 Squalane 7.0 Jojoba oil 3.0 Solid paraffin 3.0 Polyoxyethylene cetyl ether 2.0 Sorbitan sesquioleate 1.0 Potassium hydroxide 0.1 Minoxidil 0.5 Kinetin 5.0 B Glycerin 3.0 Ethyl Paraben 0.1 Purified water Appropriate amount The ingredients belonging to A are dissolved by heating. Separately, the components belonging to B are melted by heating. After adding B to A, stirring and emulsifying, cooling was carried out to produce a hair cream.

<Formulation Example 2> Heartonic (% by weight) A Polyoxyethylene hydrogenated castor oil 1.0 dbc-AMP 1.0 Isopropylmethylphenol 0.05 Ethanol 55.0 Kinetin 4.0 B Glycerin 2.0 Purified water Appropriate amount A component belonging to A is uniformly stirred and dissolved. Then, separately, the components belonging to B, which were uniformly dissolved, were gradually added, and the mixture was uniformly stirred to produce a hair nick.

<Formulation Example 3> Hair treatment (% by weight) A Avocado oil 5.0 Squalane 5.0 Liquid paraffin 10.0 Stearic acid 3.0 Glycerin monostearate 3.0 Lanolin alcohol 5.0 Kinetin 2.0 B Assemblage extract 1.0 1,3-Butylene glycol 5.0 Triethanol Amine 1.0 Methylparaben 0.2 Purified water Appropriate amount A component belonging to A is dissolved by heating. Separately, the components belonging to B are melted by heating. After adding B to A, stirring, emulsifying, and cooling, a hair treatment was manufactured.

<Formulation Example 4> Hair shampoo (% by weight) A Forskolin 0.05 N-coconut oil fatty acid-L-glutamic acid 40.0 Triethanolamine (30%) Coconut oil fatty acid diethanolamide 3.0 Polyoxyethylene methyl dioleate 2.0 Glucoside (120 EO) Kinetin 2.5 B Ethyl paraoxybenzoate 0.3 Disodium edetate 0.1 Purified water Appropriate amount A component belonging to A is uniformly stirred and dissolved, and separately heated and uniformly added to a component belonging to B, A hair shampoo was prepared by stirring uniformly.

<Formulation Example 5> Aerosol (wt%) A Benzyl nicotinate 0.01 Vitamin E acetate 0.05 Cetanol 1.2 Kinetin 0.05 Propylene glycol 4.0 Ethanol 8.0 Purified water Appropriate amount B Freon 123 / 141b (57:43) 7.0 A component belonging to A The mixture was uniformly mixed and dissolved, placed in an aerosol container, and B was filled in the container by an ordinary method to produce an aerosol.

<Formulation Example 6> Air foam (% by weight) A Hinokitiol 0.1 Cetanol 1.2 Propylene glycol 2.0 Dimethyl silicone oil 2.0 Polyoxyethylene hydrogenated castor oil 2.5 Liquid paraffin 1.0 Polyvinylpyrrolidone 0.5 Kinetin 3.0 Methylparaben 0.2 Ethanol 10.0 Purified water qs B Liquefaction Petroleum gas (propellant) 4.0 Ingredients belonging to A were uniformly mixed and placed in a container, and B was filled in the container by an ordinary method to produce an air foam.

<Formulation Example 7> Hair liquid (% by weight) A Polyoxypropylene butyl ether (40 P.0.) 15.0 Diisopropanolamine 0.5 Kinetin 8.0 Ethanol 50.0 B Propylene glycol 3.0 Purified water Appropriate amount of components belonging to A at room temperature A component belonging to B, which was stirred, dissolved, and uniformly dissolved, was gradually added, and the mixture was stirred uniformly to produce a hair liquid.

<Formulation Example 8> Milk lotion (wt%) A Polyoxyethylene behenyl ether (20E.0.) 0.5 Tetraoleic acid polyoxyethylene sorbit (60E.0.) 1.0 Lipophilic glyceryl monostearate 1.0 Stearin Acid 1.5 Behenyl ether 1.5 Avocado oil 3.0 Natural vitamin E 0.02 Carpronium chloride 0.5 Kinetin 1.0 B 1,3-Butylene glycol 5.0 Purified water Appropriate amount The ingredients belonging to A are dissolved by heating. Separately, the components belonging to B are melted by heating. After adding B to A, stirring and emulsifying, cooling was performed to produce a milk lotion.

[0035]

[Test Example] Mouse hair growth effect test The effect of kinetin alone and the effect of combined use of kinetin with other known active ingredients were examined by the following methods. <Sample> The base of Formulation Example 8 containing 1% of kinetin, which is the active ingredient of the present invention, was used. Only the base was used as a control, and 1% pentadecanoic acid glyceride was used as a positive control. When examining the effect of combined use, the base of Formulation Example 8 was used in which 0.3% of kinetin and a known active ingredient were mixed at a predetermined concentration.

<Method> The back hair of a ddY white mouse (male, 7 weeks old, weight 32 g) with whole back resting hair was shaved with an electric clipper, and each sample was applied to the skin of the test area from the day after the hair cutting. 0.2 ml was applied twice a day, 5 days a week, once per animal. Ten animals per group were used for one sample. The hair growth effect was determined by comparing the number of hair growth animals and the area of hair growth 35 days after the treatment with the control group. The hair-growth area ratio was obtained by cutting out a photograph of the test area and calculating the weight ratio after 35 days to 0 days after the treatment and calculating the average of one group and comparing it with the control group. In the control group, only the base was used, and 1% pentadecanoic acid glyceride was used as a positive control.

<Results> The effects of each sample are shown in Tables 1 to 4. In addition, the test result of only the base material as a control is
The number of hair-growing animals was 2/10, and the hair-growth area ratio was 15.2%. The kinetin of the present invention was not only found to have a hair-growth effect when blended alone, but a synergistic hair-growth effect was also observed when kinetin was used in combination with other known hair-growth active ingredients.

[0038]

[Table 1]

[0039]

[Table 2]

[0040]

[Table 3]

[0041]

[Table 4]

[0042]

INDUSTRIAL APPLICABILITY According to the present invention, there is provided a hair-growing agent containing kinetin as an active ingredient, which is used for promoting hair growth and treating alopecia such as androgenetic alopecia and alopecia areata. It is able to exert outstanding effects. Further, the above kinetin, cyclic adenosine monophosphate and its derivatives, cyclic guanosine monophosphate and its derivatives, forskolin, carpronium chloride, pentadecanoic acid glyceride, minoxidil, female hormone, adrenocortical hormone, vitamins,
When used in combination with one or more compounds selected from the group consisting of peripheral vasodilators, cell activators, and photosensitizers, a synergistic hair growth promoting effect can be achieved.

Claims (2)

[Claims] 1. A hair restorer comprising kinetin as an active ingredient. 2. Kinetin, cyclic adenosine monophosphate and its derivative, cyclic guanosine monophosphate and its derivative, forskolin, carpronium chloride, pentadecanoic acid glyceride, minoxidil, female hormone, adrenocortical hormone, vitamins, A hair restorer characterized by comprising, as an active ingredient, one or more compounds selected from the group consisting of peripheral vasodilators, cell activators, and photosensitizers.