JPH04234804A - Hair restorer - Google Patents

Abstract

PURPOSE:To obtain a hair restorer having low skin irritation and effective for remarkably improving alopecia by compounding an alkylcarboxybetaine or its salt with a torpent. CONSTITUTION:The objective hair restorer contains (A) 0.1-40wt.% (preferably 0.5-5wt.%) of a compound of formula (R<1> is 6-26C saturated or unsaturated hydrocarbon group; R<2> and R<3> are H or lower alkyl; A is 1-3C alkylene which may be substituted with methyl or OH) or its salt, e.g. betaine dodecyldimethylaminoacetate and (B) 0.001-20wt.% (preferably 0.01-10wt.%) of a torpent such as glycyrrhizinic acid, hydrocortisone acetate, lysozyme chloride and berberine chloride.

Description

[Detailed description of the invention]

0001

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair growth agent with low skin irritation, which contains an alkylcarboxybetaine or a salt thereof and an irritation reliever.

0002

[Prior Art] Conventionally, carpronium chloride, estradiol, schwertiamarin, pentadecanoic acid glyceride, and ginseng extract have been used as hair tonics, hair growth agents, and hair growth agents, but none of them are sufficiently effective.
It was not possible to significantly improve alopecia.

Under these circumstances, the present inventors

00
04]

[Case 2]

(In formula 2, R1 represents a monovalent group of saturated or unsaturated hydrocarbon having 6 to 26 carbon atoms, and R2 and R3
represents a hydrogen atom or a lower alkyl group, and A has 1 to 3 carbon atoms, which may be substituted with a "methyl group or hydroxyl group"
represents an alkylene group. ) and its salts have been found to have excellent hair growth effects.

[0006]

[Problems to be Solved by the Invention] However, since the compound of Chemical Formula 2 has skin irritation properties, it was more desirable to develop a formulation that improves this point.

[0007]

[Means for Solving the Problems] The present inventors utilize the compound of chemical formula 2 that has an excellent hair growth effect to obtain a hair growth agent that has an excellent hair growth effect and is less irritating to the skin. As a result of intensive research, it was discovered that a hair growth agent containing the compound of chemical formula 2 and a certain irritation-reducing agent could achieve the objective, and the present invention was completed.

That is, the present invention is a hair growth agent containing the compound of formula 2 or a salt thereof and an irritation reliever.

The present invention will be explained in detail below. In the present invention, monovalent groups of saturated or unsaturated hydrocarbons having 6 to 26 carbon atoms include hexyl group, heptyl group, octyl group,
Nonyl group, decyl group, undecyl group, dodecyl group, tetradecyl group, bentadecyl group, hexadecyl group, octadecyl group, icosyl group, tetracosyl group, hexacosyl group, hexenyl group, decenyl group, tetradecenyl group, hexadecenyl group, octadecadienyl group etc., and may be linear, branched, or cyclic. Further, the lower alkyl group includes a methyl group, an ethyl group, a propyl group, a butyl group, etc., and may be linear or branched.

As irritation relievers, glycyrrhizic acid or its derivatives [for example, salts of glycyrrhizic acid (alkali metal salts such as dipotassium glycyrrhizinate, ammonium salts, alkanolamine salts, basic amino acid salts, pyridretin, etc.), glycyrrhetinic acid, glycyrrhetinic acid, etc. Stearyl, 3-stearyloxyglycyrrhetinic acid, 3
- disodium succinyloxyglycyrrhetinate, etc.], hydrocortisone acetate, dexamethasone acetate, betamethasone valerate, triamcinolone acetonide, α-
Chymotrypsin, lysozyme chloride, berberine chloride, shikonin, salicylic acid, acetylsalicylic acid, salicylic acid amide, guaiazulene, sodium guaiazulene sulfonate, ethyl guaiazulene sulfonate, tranexamic acid, indomethacin, hinokitiol, cholestanol, cholestanol phosphate, ibuprofen,
Ketoprofen, flubiprofen, epsilon aminocaproic acid, cholesterol, cholesterol acetate, cholesterol stearyl, cholesterol sulfate, cholesterol phosphate, O-acylceramide, animal-derived keratin or their hydrolysates,
diphenhydramine, isothipendyl, allantoin,
Examples include allantoin chlorohydroxyaluminum, allantoin-dl-bantothenyl alcohol, and the like.

[0011] The hair growth agent of the present invention may use one type of compound of formula 2 or a salt thereof, or two or more types thereof as an active ingredient. The amount of active ingredient is 0.1 of the total amount of the preparation.
-40% by weight, preferably 0.5-5% by weight. Further, the amount of the irritation-reducing agent varies depending on the amount of the compound of Chemical Formula 2, but is generally 0.001 to 20% by weight, preferably 0.01 to 10% by weight.

The hair growth agent of the present invention can be prepared into various dosage forms such as lotions, milky lotions, creams, gels, and aerosols according to commonly used methods (for example, methods specified in the 11th edition of the Japanese Pharmacopoeia). can.

In addition to the above-mentioned essential ingredients, the hair growth agent of the present invention contains substances commonly used in hair growth agents, such as humectants (brobylene glycol, glycerin, diglycerin, etc.), solvents (
Ethyl alcohol, isopropyl alcohol, 1,3-
butylene glycol, purified water, etc.), preservatives (paraben, benzoic acid, etc.), vitamins (vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, etc.), oils (liquid paraffin, cetyl alcohol, stearyl alcohol, squalane) , white petrolatum, olive oil, etc.)
, fungicides [sulfur, chlorhexidine gluconate, chlorhexidine hydrochloride, isopropylmethylphenol, quaternary
grade ammonium salts (such as benzalkonium chloride)
, dequalinium chloride, hinokitiol, etc.], nonionic surfactants (polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, glycerin monofatty acid ester, polyoxyethylene hydrogenated castor oil derivative, etc.), thickener (
polyvinylpyrrolidone, carboxymethylcellulose,
carboxyethyl cellulose, hydroxypropyl cellulose, carboxyvinyl polymer, etc.), pH adjusters (diisopropanolamine, citric acid, etc.), antioxidants (dibutylhydroxytoluene, sodium bisulfite, etc.), cooling agents (1-menthol, camphor, etc.) ) Peripheral vasodilators (tropherol acetate, benzyl nicotinate, schwertiamarin, capsicum extract, kabsaicin, etc.), local anesthetics (dibucaine hydrochloride, lidocaine hydrochloride, etc.), keratolytic agents (urea, salicylic acid, etc.), follicles Hormones (17β-estradiol, estrone, etc.), progesterone (progesterone, 17α-
hydroxyprogesterone, etc.), adrenocortical hormones (
dexamethasone acetate, hydrocortisone acetate, etc.)
Antihistamines (diphenhydramine hydrochloride, isothipendyl hydrochloride, etc.), antiandrogens (cyproterone acetate, 4-androsten-3-one-17β-carboxylic acid, etc.), fragrances, sequestering agents, ultraviolet absorbers, absorption enhancers ( Aison, monoester or diester of propylene glycol, diester or triester of glycerin, oleyl alcohol, 2
-hexyldecyl alcohol, dimethyl sulfoxide,
(alkyl-N,N-dialkylaminoacetic acid ester, isopropyl myristate, etc.) can be blended.

[0014]

[Effects of the Invention] According to the present invention, it has become possible to provide a hair growth agent that has an extremely high hair growth effect and has low skin irritation.

[0015]

[Examples] The present invention will be specifically explained below with reference to Examples and Test Examples.

(Example 1) Ingredients

Blend amount Dodecyldimethylaminoacetic acid betaine
2g hydrocortisone acetate

0.2g glycerin

5g dibutylhydroxytoluene
0.1g chlorhexidine gluconate

0.1g vitamin B6

0.5g polyoxyethylene monostearate
1.0g methylcellulose

0.2g dipotassium glycyrrhizinate

0.2g chili pepper tincture

0.1g purified water

A lotion was prepared by mixing and dissolving each component in a total of 100 g of solvent.

(Example 2) Ingredients

Blend amount Coconut oil dimethylaminobutyric acid betaine
2g berberine chloride

2g 1,3-butylene glycol

5g isothibenzyl hydrochloride

0.1g sulfur

3.0g estrone
0.00
08g ethyl alcohol

20g purified water

Total 100g A lotion was prepared according to Example 1.

(Example 3) Ingredients

Composition Coconut oil dimethylaminoacetic acid betaine
3g ibuprofen

1g propylene glycol

3g Decyl-N,N-dimethyl-
amino acetate
3g polyoxyethylene hydrogenated castor oil
3g
Isopropyl alcohol
5
g Purified water

Total 100g A lotion was prepared according to Example 1.

(Example 4) Ingredients

Blend amount Hexadecyldimethylaminobutyric acid betaine
1g allantoin

1g ethyl alcohol

20g propylene glycol

5g purified water

A lotion was prepared according to Example 1, totaling 100 g.

(Example 5) Ingredients

Blend amount Octadecyldimethylaminoacetic acid betaine 2.
5g Shikonin

1g ethanol

2g purified water

Total 100g A lotion was prepared according to Example 1.

(Example 6) Ingredients

Blend amount Octadecyldimethylaminobutyric acid betaine
2g wool keratin

1g vitamin E acetate

0.2g glycyrrhetinic acid

0.2g glycerin monocaprate

1g squalane

5g liquid paraffin
15g white petrolatum

3g polyoxyethylene (20) sorbitan monostearate 4g purified water

An oil-soluble component and a nonionic surfactant are dissolved by heating into an oil phase consisting of a total of 100 g of squalane, liquid paraffin, and white petrolatum,
To this was added an aqueous phase in which betaine octadecyldimethylaminobutyrate and water-soluble components were dissolved under heating, and the mixture was emulsified and cooled to prepare a cream.

(Example 7) Ingredients

Blend amount icosyldimethylaminoacetic acid betaine
1g cholesterol

0.5g squalane

8g stearyl alcohol

2g polyoxyethylene hydrogenated castor oil
5g polyoxyethylene sorbitan monostearate
2g benzalkonium chloride
0
．． 1g purified water

Oil-soluble components and nonionic surfactants were dissolved by heating in an oil phase consisting of 100 g of squalane and stearyl alcohol, and an aqueous phase in which icosyldimethylaminoacetic acid betaine and water-soluble components were dissolved by heating was added to emulsify. It was cooled and a milky lotion was prepared.

(Example 8) Stock solution components

Blend amount Hexadecyldimethylaminoacetic acid betaine
3g epsilon aminocaproic acid

2g squalane

2g stearyl alcohol
0.2g polyoxyethylene hydrogenated castor oil
1g polyoxyethylene sorbitan monostearate
0.5g paraben

0.15g purified water

A total of 100 g filler dimethyl ether A stock solution was prepared according to the emulsion manufacturing method of Example 7, and an aerosol was manufactured using the following formulation using a conventional filling method. Prescription stock solution: 30% by weight Filler: 70% by weight

(Example 9) Ingredients

Blend amount Dodecyldimethylaminoacetic acid betaine
2g ceramide

0.5g polyvinylpyrrolidone
3g carboxyvinyl polymer
0.5g paraben

0.1
5g purified water

After dissolving betaine dodecyldimethylaminoacetate, dipotassium glycyrrhizinate, and paraben in a total of 100 g of purified water, polyvinylpyrrolidone and carboxyvinyl polymer were added and dissolved to prepare a gel.

(Test Example) Hair Growth Effect Test Hair growth effect test of alkylcarboxybetaine was carried out using C3H
Using a group of 5 mice (male, 7 weeks old), their back hair was removed with clippers, and 0.2 ml of the sample shown in Table 1 was applied to the site once a day for 10 days. The degree of hair growth was visually evaluated in the following 6 grades. 0: No hair growth observed 1: Slight hair growth observed 2: Terminal hair growing 3: Terminal hair growing in 50% of the hair removal area 4: Terminal hair growing in 75% of the hair removal area 5%: Terminal hair is the hair removal site 10%
In addition, a group in which no sample was applied as a control was similarly evaluated. The results 42 days after the start of sample application are shown in Table 2 as the average value of the evaluation points.

[0026]

[Table 1]

[0027]

[Table 2]

Claims (1)

[Claims] Claim 1: Formula [Formula 1] (In Formula 1, R1 represents a monovalent group of saturated or unsaturated hydrocarbon having 6 to 26 carbon atoms, and R2 and R3 represent a hydrogen atom or a lower alkyl group) , A is "methyl group or hydroxyl group"
represents an alkylene group having 1 to 3 carbon atoms which may be substituted with ) or a salt thereof and an irritation reliever.