JP7059671B2 - Hair growth agent - Google Patents

Description

The present invention relates to a hair growth agent containing minoxidil as an active ingredient.

Minoxidil has a chemical name of 6- (1-piperidinyl) -2,4-pyrimidinediamine-3-oxide, and its indication as a hair restorer has been reported (Patent Document 1), as well as hair growth, hair growth, and hair growth. There are numerous reports of its action.
Although the minoxidil preparation has an excellent hair growth effect, an even better one has been sought.
Conventionally, it has been reported that trehalose undecylenic acid has a hair-growth effect, but it has been reported that undecylenic acid has a low hair growth-promoting effect (Patent Document 2). Until now, it has not been known that the combined use of undecylenic acid and minoxidil enhances the hair growth effect.

U.S. Pat. No. 4,139,619 Japanese Unexamined Patent Publication No. 8-53326

An object of the present invention is to further improve the excellent hair growth effect of minoxidil.

As a result of various studies to further improve the excellent hair growth effect of minoxidil, the present inventors obtained an excellent hair growth effect that cannot be predicted from the effect of each component alone when minoxidil and specific undecylenic acids are combined. It was found that it had, and the present invention was completed.
That is, the present invention
(1) A hair growth agent characterized by combining minoxidil and at least one undecylenic acid selected from the group consisting of undecylenic acid, undecylenate, and undecylenic acid ester.
Is.

As is clear from the test examples described later, by combining minoxidil with specific undecylenic acids, an excellent hair growth effect was obtained as compared with the case of using it alone.

The hair growth agent of the present invention contains essential ingredients and other compounding ingredients if necessary, and is appropriately applied externally to lotions, aerosols, tonics, creams, ointments, gels, etc. by a usual method. It can be used as a formulation.
The blending amount of minoxidil blended in the present invention is 0.1 to 5 W / V% (hereinafter, "W / V%" is simply "%" of the entire formulation (in the undiluted solution in the case of an aerosol agent) from the viewpoint of hair growth effect. ”) Is preferable.

The undecylenic acids of the present invention are undecylenic acid, undecylenate, and undecylenic acid ester.

Examples of undecylenic acid acid include zinc undecylenic acid, potassium undecylenic acid, undecylenic acid triethanolamide, undecylenic acid diethanolamide, undecylenic acid monoethanolamide, and examples of undecylenic acid ester include undecylenic acid glyceryl, undecylenic acid polyglyceryl, and undecylenic acid. Examples thereof include methyl acid, ethyl undecylenate, and vinyl undecylenate.
The blending amount of the undecylenic acid compounded in the present invention is preferably 0.01 to 20%, more preferably 0.1 to 10% of the entire preparation from the viewpoint of promoting hair growth.
As the solvent of the hair growth agent of the present invention, ethanol, water or a mixed solution thereof is preferable. In this case, the blending amount is preferably in the range of about 40 to 80% for ethanol and about 5 to 30% for water with respect to the entire preparation. In particular, it is preferable to add ethanol because a good feeling of use can be obtained due to the volatilization of ethanol immediately after application.
The hair growth agent of the present invention further contains various active ingredients and auxiliary ingredients used in general external preparations, for example, excipients, vasodilators (carpronium chloride, benzyl nicotinate, assembly extract), if necessary. , Otaneninjin extract, Togarashi tincture, etc.), Antihistamines (isotipendyl hydrochloride, diphenhydramine hydrochloride, etc.), Anti-inflammatory agents (guaiazulene, etc.), Keratolytic agents (urea, salicylic acid, etc.), Bactericides (chlorhexidine gluconate, isopropylmethylphenol, etc.) Tertiary ammonium salt, pyrocton olamine, hinokithiol, glycyrrhetinic acid, etc.), moisturizer (sodium hyaluronate, chondroitin sulfate, etc.), various animals and plants (ichii, buttonpi, kanzo, otogirisou, tsukushi, biwa, kawarayomogi, confrey, etc. Extracts of Ashitaba, Saffron, Sanshishi, Rosemary, Sage, Mokko, Seimokko, Hop, Placenta, etc., Vitamins (Retinol acetate, Pyridoxin hydrochloride, Ascorbic acid, Thiamine nitrate, Cyanocobalamine, Biotin, Vitamin E acetate, Pantotenil ethyl Antioxidants (dibutylhydroxytoluene, sodium pyrosulfate, tocopherol, sodium edetate, ascorbic acid, isopropyl gallate, etc.), solubilizers (diisopropyl adipate, isopropyl myristate, various vegetable oils, various animal oils, alkyl glyceryl) Ethers, hydrocarbons, etc.), metabolic activators, gelling agents (water-soluble polymers, etc.), polyhydric alcohols (glycerin, 1,3-butylene glycol, etc.), adhesives, fragrances, refreshing agents (hakka oil) , Kamfur, menthol, etc.), dyes and other commonly used ingredients can be blended to the extent that the effects of the present invention are not impaired.
The amount of these selective components added is not particularly limited and can be experimentally determined in consideration of the feeling of use, the stability of minoxidil and undecylenic acid, the solvent-based composition, and the like.

Furthermore, the hair growth agent of the present invention can be used in combination with the active ingredient of other alopecia preventive or therapeutic agents. Examples of the drug that can be used in combination include, but are not limited to, finasteride, dutasteride, carpronium chloride, adenosine, pentadecanoic acid glyceride, t-flavanone, 6-benzylaminopurine and the like. In addition, with other agents such as hair growth agents / hair growth agents, vasodilators, antiandrogens, cyclosporin derivatives, antibacterial agents, anti-inflammatory agents, thyroid hormone derivatives, prostaglandin agonists or antagonists, retinoids, triterpenes and the like. It can be used together. The hair growth agent composition of the present invention and the active ingredient of another alopecia preventive agent or therapeutic agent may be used as separate formulations or may be used as one combination drug.

Hereinafter, the present invention will be described in more detail with reference to Test Examples.
Test Example 1
<Hair growth effect in mouse hair cutting model>
The back body hair of C57BL mice (female, 7 weeks old) was cut, and from 3 days after cutting, solvent (1,3-butylene glycol / ethanol / purified water), minoxidil 5% (solvent is the same as on the left), minoxidil 5% and Either 10% undecylenic acid (solvent on the same left) or undecylenic acid 10% (solvent on the left) was continuously applied once a day at 0.1 mL per animal for 45 days. The hair growth status of the cut hair was scored using the following hair growth score criteria on the first day of administration (1st day), 8th day, and every 2 or 3 days thereafter.
Hair growth score criterion 1 = Hair growth in less than 5% of the hair cut 2 = Hair growth in 5% or more of the hair cut, hair growth in less than 30% 3 = Hair growth in 30% or more of the hair cut, hair growth in less than 60% 4 = Hair growth in 60% or more and less than 90% of the hair cut part 5 = Hair growth in 90% or more of the hair cut part The scores on the 20th day after the start of administration are shown in Table 1.
In the table, "*" is p <0.05, "**" is p <0.01, which is significantly different from the base group (Steel multiple comparison), and "#" is p <0.05. Shows a significant difference from the minoxidil 5% group (Student's t-test).

From the results of this test example, the hair growth agent combining minoxidil and undecylenic acid has a hair growth and hair growth effect that promotes hair growth, and the effect is significantly superior to the test solution containing only minoxidil. I understood.
From this result, it is considered that the hair growth effect of minoxidil can be further improved by combining minoxidil and undecylenic acid.

Since the present invention has been able to further improve the hair growth effect of minoxidil, it can be used as a pharmaceutical product, a quasi-drug, a cosmetic product, or the like.

Claims (1)

A hair growth agent characterized by a combination of minoxidil and at least one undecylenic acid selected from the group consisting of undecylenic acid and undecylenate.