JPS6219513A - Hair tonic - Google Patents

Abstract

PURPOSE:To provide a hair tonic having excellent hair tonic effect by using a cyclosporin compound as an active component. CONSTITUTION:The objective hair tonic having excellent hair tonic effect contains a cyclosporin compound known as an immunosuppressive agent, preferably cyclosporin A-D or G, etc., especially cyclosporin A, as an active component in an amount of 0.001-10wt%, preferably 0.01-5wt%. The hair tonic may contain other pharmacologically permissible additives or other drug components, and the mixture is administered transcutaneously by applying or scattering directly to the skin. The amount of the active compound to be applied to man is 0.0001-10mg, preferably 0.001-1mg per 1kg body weight daily, and administered once a day or in 2-4 divided doses.

Description

DETAILED DESCRIPTION OF THE INVENTION [Field of Industrial Application] The present invention relates to a novel hair nourishing agent. More specifically, the present invention relates to a hair tonic containing cyclosporins as an active ingredient.

[Conventional technology]

Conventionally, the causes of baldness and hair loss are (11) activation of male hormones in organs such as hair roots and sebaceous glands, (2) decreased blood flow to hair follicles, (3) excessive secretion of sebum, and production of peroxide. , scalp abnormalities due to bacterial growth, (4) genetic predisposition,
(5) Neurosis caused by stress, (6) secondary disease, and (7) aging.

For this reason, conventional hair nourishing products generally contain compounds that have the effect of eliminating or alleviating the above-mentioned causes. For example, compounds that have the effect of inhibiting the activation of male hormones or compounds that have the effect of increasing blood flow to the hair follicles are included.

[Problem that the invention seeks to solve]

However, the mechanism of hair loss and hair growth is extremely complex.
Simply inhibiting the activation of male hormones or increasing blood flow to hair follicles cannot sufficiently prevent baldness and hair loss.

In view of the above circumstances, the present inventor searched for substances that have an effective effect on hair loss, and as a result of searching for substances that have an excellent hair-nourishing effect, discovered that cyclosporin, which is known as an immunosuppressant, However, it was discovered that it has a surprisingly strong hair-growth effect.The object of the present invention is to provide a hair-growth agent containing a substance that has been newly discovered to have an excellent hair-growth effect.

[Means for solving problems]

That is, the gist of the present invention is a hair tonic containing cyclosporins as an active ingredient. The present invention will be explained in more detail below.

The cyclosporins used in the present invention are known substances, and it is of course not known that they have immunosuppressive effects, anti-inflammatory effects, and the like.

As used herein, "cyclosporins" refers comprehensively to a group of cyclic poly-N-methylated undecapeptides, such as cyclosporin A, cyclosporin B1 cyclosporin c1 cyclosporin D1 cyclosporin G, etc., as well as dihydrocyclosporins corresponding thereto, ■ isocyclosporins, (D)-serine-cyclosporin, (D)-heptin-dihydro■ cyclosporins , allylglycyl-cyclosborine, and the like. These are white powders at room temperature, and organic solvents such as ethanol, methanol,
It is soluble in acetone, ether, ethyl acetate, benzene, chloroform, etc., but almost insoluble in water.

Among the above-mentioned cyclosporins, cyclosporin A1 cyclosporin B1 cyclosorine C1 cyclosporin D, cyclosporin G, etc. are preferred, and cyclosporin A is particularly preferred.

Cyclosporins can usually be obtained from the culture filtrate of known bacterial strains capable of producing cyclosporins.

As the above-mentioned bacterial strains capable of producing cyclosporins,
For example, Tolypocadium
), genus Cylindrocarp
On) genus, Fusarium genus, and the like.

Examples of the above-mentioned strains of the genus Tribofragilum include Tribofragilum inflatum gums (T, 1nfla
Strains such as Cylindrocarbone lucidum (S, lucidum) can be suitably used.
As the Fusarium strain, for example, a strain such as Fusarium solani (F, 5olani) can be suitably used. The target cyclosporins can be obtained by extraction with an organic solvent such as ethyl acetate or chloroform from the culture filtrate of the above-mentioned strain capable of producing cyclosporin, and further purification by silica gel column chromatography. I can do it.

In addition, in the present invention, Japanese Patent Application Laid-Open No. 50-89598,
JP-A-52-59180, JP-A-53-139789
No., JP-A-55-55150, JP-A-56-1287
No. 25, JP-A-57-62210, JP-A-57-63
No. 093, JP-A-57-130905, JP-A-57-
Cyclosporins obtained by methods described in publications such as No. 140753 can also be used.

As used herein, "hair nourishing effect" or "hair nourishing effect" means prevention of hair loss, promotion of caterpillars and hair growth, and hair growth.

Next, the formulation of cyclosporins for use as a hair nourishing agent will be described.

The hair growth agent of the present invention is used in the form of a mixture containing pharmaceutically acceptable additives and other drugs in addition to cyclosporins.

Examples of the additives include antibacterial agents such as hinokitiol, hexachlorophene, phenol, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide, and bithionol, derivatives such as glycyrrhizinic acid and its ammonium salt, Anti-inflammatory cooling agents such as allantoin and menthol, drugs such as salicylic acid, zinc and its compounds, lactic acid and its alkyl esters, olive oil, macadamia nut oil,
Animal and vegetable oils such as squalane, hydrocarbon oils such as liquid paraffin, ester oils such as isopropyl myristate, cetyl isooctanoate, and 2-ethylhexyl palmitate, waxes such as beeswax and carnauba wax, higher fatty acids, higher Oils such as alcohol, water, derivatives such as lactic acid and its ethyl ester, polyhydric alcohols such as polyethylene glycol, glycerin, sorbitol, lower alcohols such as ethanol, mucopolysaccharides, humectants such as pyrrolidone carboxylates, carboxyvinyl polymers ,
Gelatin, gum arabic, thickeners such as polyvinyl alcohol, surfactants, fragrances, antioxidants, ultraviolet absorbers,
Examples include pigments, which may be used alone or in combination of two or more.

The hair growth agent of the present invention can be in any form as long as it can be used externally. For example, lotions, liniments, emulsion and other external liquids, creams, ointments, pasta,
Examples include external semi-solid preparations such as jelly and spray.

The hair tonic of the present invention contains 0.001 to 10% by weight, preferably 0.01 to 5% by weight of cyclosporins as active ingredients.
The hair tonic of the present invention, which is contained in a crotch-shaped dish in an amount within the range of % by weight, is administered by transdermal administration, in which it is applied or sprayed directly onto the skin.

The dosage of the hair tonic of the present invention cannot be clearly defined as it varies depending on age, individual differences, medical conditions, etc. However, in general, when targeting humans, the transdermal dosage of cyclosporins is 1 kg of body weight and 1 kg of body weight. The daily amount is o,oooi to 10 cm, preferably 0.001 to 1 cm.

The above amount can be administered once or in 2 to 4 divided doses per day.

〔Example〕

EXAMPLES Hereinafter, the formulation method and hair growth effect of the hair growth agent according to the present invention will be specifically explained with reference to Examples. % in the examples represents weight %.

■−Soil A lotion having the following composition was prepared.

95% ethanol 80.0 Cyclosporin A 0.001 Hinokitiol 0.01 Ethylene oxide (40 mol) adduct of N' castor oil 0.5 Purified water
19.0 Fragrances and Colors
Cyclosporin A1 hinokitiol, hydrogenated castor oil adduct with ethylene oxide (40 mol), fragrance and coloring matter were added to an appropriate amount of 95% ethanol, and dissolved with stirring. Purified water was then added to obtain a transparent liquid lotion.

This lotion can be easily applied to the skin once to four times a day.

Example 2 A milky lotion was prepared from Phase A and Phase B having the following compositions.

(Phase A) Whale wax 065 cetanol
2.0 Vaseline
5.0 Squalane 10
．． 0 Polyoxyethylene (10 mol) Monostearate 2.0 Sorbitan monooleate) 1.0 Dihydrocyclosporine D 0.5 (Phase B) Glycerin 10.0 Purified ice
69.0 Fragrances, Colors and Preservatives
Appropriate amounts of phase A and phase B are dissolved by heating and kept at 80°C. Both phases were mixed and emulsified, and cooled to room temperature while stirring to obtain a milky lotion.

This emulsion can be applied to the skin once to four times a day.

■−Yu A cream was prepared from Phase A and Phase B having the following composition.

(Phase A) Liquid paraffin 5.0 Cetostearyl alcohol 5.5 Vaseline
5.5 Glycerin monostearate 3.0 Polyoxyethylene (20 mol) 2-octyl dodecyl ether 3.0 Propylparaben 0.3 (Phase B) Isocyclosporin G 10.0 Glycerin 7.0 Dipropylene glycol
20.0 Polyethylene glycol 4000 5
．． 0 Sodium hexametaphosphate o, oos Purified water 35. Dissolve phase A by heating and keep at 70°C. Separately, heat and melt phase B at 70°C.
Keep it. Phase B was added to phase A and stirred, and the resulting emulsion was cooled to obtain a cream.

This cream can be applied to the skin from 1 to 4 times a day.

a Genkyomasu In order to investigate the hair-growth effect of the hair-growth agent of the present invention, a tricogram test and a road conversion rate test were conducted.

In both studies, 40 male subjects were tested in each
The subjects were divided into four groups of 0 subjects each, and four different test solutions were given to each subject in each group for comparison.

The four test solutions are shown in Table 1 below.

Table 1 Each of the above ethanol solutions was applied to the subject's scalp in two doses per day.

(1) Trichogram test The removed hair roots are observed under a microscope before and after using both ethanol solutions, and the number of telogen hair roots is counted based on the morphology of the hair roots. The hair growth effect was compared.

A telogen hair root is a hair root that has stopped growing.

People who complain of hair loss have more telogen hair roots than normal people, so the hair-nourishing effect was evaluated based on the reduction in telogen hair roots. The application of each ethanol solution to the scalp was continued for three months, and 60 hair roots were removed for each subject, immediately before the application and immediately after the end of the three-month application. The results are shown in Table 2.

□ (2) On-road conversion rate test 3 areas above the head of each of the 40 subjects with androgenetic alopecia
At several locations, the conversion rate from downy hair to pure hair was compared before and after application of each of the above-mentioned ethanol solutions. Pure hair refers to hair other than downy hair, that is, hair with a length of 14 cranes or more.
The conversion from downy hair to pure hair means a hair-nourishing effect. Immediately before application of each ethanol solution and immediately after completion of application for 4 months,
The conversion rate was measured by taking a close-up photograph of the upper part of the head. The conversion rate to pure wool is expressed as a percentage of the average of the three locations. The results are shown in Table 3.

Table 3: Final hair conversion rate test results As is clear from the above results, the effect of cyclosporins as a hair nourishing agent is remarkable, and the hair nourishing agent according to the present invention has an excellent hair nourishing effect.

Claims (1)

[Claims] 1. A hair tonic containing cyclosporin as an active ingredient.