JPH06192047A - Hair tonic - Google Patents

Abstract

PURPOSE:To provide a hair tonic having strong hair-tonic effect and sufficiently exhibiting the falling-off preventing effect, hair-growth promoting effect, etc. CONSTITUTION:This hair tonic contains at least one kind of compound selected from xanthine derivatives of the formula (R1 and R2 are H or 1-6C alkyl), e.g. theobromin, theophylline, 3-methyl-7-propylxanthine and 3-methyl-1- propylxanthine. The amount of the compound is 0.0001-10wt.% (preferably 0.001-5wt.%) based on the total hair-tonic. The hair tonic may be incorporated with other components such as minoxidil, diazoxide and various antiandrogenic agents to improve the hair-growing and hair-tonic effects. It can be used in pharmaceutical field, quasi-drug field and cosmetic field.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hair nourishing agent, and more particularly to a hair nourishing agent which is used in the fields of pharmaceuticals, quasi drugs or cosmetics and which has excellent hair-preventing effects such as hair loss prevention and hair growth effect.

[0002]

2. Description of the Related Art Conventionally, hair nourishing cosmetics containing various chemicals have been known in order to remove or reduce the causes of baldness and hair loss. For example, female hormonal agents such as estradiol as an anti-androgen, and hinokitio-to improve scalp metabolism, such as assembly extracts and acetylcholine derivatives for improving blood flow to hair roots.
It is used for the prevention and treatment of alopecia. However, the mechanism of hair loss and hair growth is very complicated, and like conventional hair nourishing agents, for the purpose of promoting blood circulation and deactivating male hormones, it is sufficient to prevent the hair loss and prevent hair loss by simply blending these known agents. No hair growth effect. on the other hand,
Xanthine derivatives are used as diuretics (Co
llis. MG etal., J Pharm. Pharmacol., 38,11: 85O-8
52 (1986), Dorfman LJ, Clin. Pharmacol. Ther. 11,
6: 869-872 (1970)), and its hair-feeding effect is not known at all.

[0003]

That is, the present invention provides formula (I):

[0004]

[Chemical 2]

(Wherein R1 represents hydrogen or an alkyl group having 1 to 6 carbon atoms, R2 represents hydrogen or an alkyl group having 1 to 6 carbon atoms), and at least one compound selected from xanthine derivatives. The present invention provides a hair nourishing agent.

As the xanthine derivative represented by the formula (I) used in the present invention, theobromine (R1 = CH3, R2
= H), 3-methyl-7-propylxanthine (R1 =
C3H7, R2 = H), theophylline (R1 = H, R2
= CH3), 3-methyl-1-propylxanthine (R
1 = H, R2 = C3H7) are preferred, and particularly preferred compounds include theobromine and theophylline. The xanthine derivative used in the present invention is a substance known as a diuretic and is easily available commercially, and its content is 0.0001 to 10% by weight, and more preferably 0.001% with respect to the total amount of the hair restorer. ~ 5% by weight. If the blending amount is less than 0.0001, the hair loss preventing effect and the hair growth promoting effect are insufficient, and if the blending amount is more than 10%, an effect commensurate with the blending amount cannot be obtained. In addition, problems such as irritation also appear.

[0007] In the hair nourishing agent of the present invention, in addition to the xanthine derivative which is the active ingredient, minoxidil, diazoxide, and
Various antiandrogens, such as oxendron, 4-
Androstene-3,17-dione-17-cyclic ethylene ketal derivative and the like, nicotinic acid and its derivatives, carbronium chloride, vitamin E acetate, vitamin E nicotineate, pantothenic acid and its derivatives,
Biotin, glycyrrhizinic acid, glycyrrhetinic acid, Cordyceps sinensis extract, Korean ginseng extract, assembly extract, capsicum extract, cepharanthin, placenta extract,
Ethinyl estradiol, carpronium chloride, photosensitizer, other vitamins, amino acids and the like can be added at the same time.

Further, additives usually used in hair nourishing agents, such as hinokitiol, hexachlorophene, pheno-
, Benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, antibacterial agents such as trichlorocarbanilide and biothionol, cooling agents such as menthol,
Drugs such as salicylic acid, zinc and its derivatives, lactic acid and its alkyl esters, olive oil, squalane, liquid paraffin, isopropyl myristate, higher fatty acids,
Oils such as high-grade alcohol, other surfactants, fragrances,
Antioxidants, ultraviolet absorbers, dyes, ethanol, water, humectants, thickeners and the like can be appropriately added within a range that does not impair the effects of the present invention. The hair nourishing agent of the present invention can be produced according to a known method, and can have any shape applicable to the scalp, such as liquid, milky or ointment containing the above components.

[0009]

EXAMPLES The present invention will be described in more detail with reference to test examples and examples. Test Example 1 Test for Proliferation of Cultured Hair Mother Cells Hair tissues of mice were collected and cultured in serum-free medium (Tanigaki N. et al., Archives of Dermatological Research (Arch .Dermato
L. Res.) 282: 402-407 (1990)). 10-9 to 10-4 by dissolving each xanthine derivative in the medium
It was adjusted to have a molar concentration. Each xanthine derivative was added on the first day of the culture. After culturing for 6 days, the cells were detached from the dish and the number of cells was determined. The effect of xanthine derivatives is the control group (group cultured in serum-free medium only)
It was expressed as a relative ratio when the number of cells was 100%.
The results are shown in Table 1.

Table 1 ────────────────────────────── Relative value of test cell number (%) Growth promotion rate (%) ─ ──────────────────────────── Media only (control group) 100 Theophylline 10-9M 124 24 10-8M 155 55 10-7M 143 43 10-6M 121 21 10-5M 119 19 10-4M 102 2 Theobromine 10-9M 111 11 10-8M 161 61 10-7M 153 53 53-6-6M 137 37 37-10-5M 116 16 10-4M 1099 9 --- ────────────────────────── As is clear from Table 1, the xanthine derivative had a growth promoting effect on the cultured hair matrix cells.

Test Example 2 Hair Growth Promoting Test Using C3H Mice Each xanthine derivative was dissolved in water to prepare a concentration of 1% by weight. C3H male mice 8-week-old dorsal region was shaved to a size of about 2 × 4 cm, and the above solution was applied 1 day from the next day.
0.1 ml each was applied to the hair-cutting portion once a day for 15 days, and the effect on hair regeneration at that portion was examined. The effect of the xanthine derivative is that the hair weight of the control group (water application group) is 100%.
It was expressed as a relative ratio when it was defined as%. The results are shown in Table 2.

Table 2 ──────────────────────────── Test body hair weight relative value (%) Hair growth promotion rate (%) ─ ─────────────────────────── Water (control group) 100 Theophylline 195 95 Theobromine 187 87 ─────────── ───────────────── As is clear from Table 2, the xanthine derivative has an excellent hair growth promoting effect as compared with the control.

Example 1 A hair tonic was manufactured by a conventional method according to the following formulation. Blending amount (% by weight) Theobromine 0.03 95% Ethanol 70 Polyoxyethylene 1 Hydrogenated castor oil (60EO) Propylene glycol 5 Perfume Trace water 100

Example 2 A hair tonic was produced by a conventional method according to the following formulation. Blending amount (% by weight) 3-Methyl-7-propylxanthine 0.03 95% Ethanol 70 Polyoxyethylene hydrogenated castor oil (6OEO) 1 Propylene glycol 5 Perfume Trace water 100

Example 3 A hair tonic was produced by a conventional method according to the following formulation. Compounding amount (wt%) Theophylline 0.03 95% Ethanol 70 Polyoxyethylene hydrogenated castor oil (6OEO) 1 Propylene glycol 5 Perfume Trace amount of water 100

Example 4 A hair tonic was produced by a conventional method according to the following formulation. Blending amount (% by weight) 3-Methyl-1-propylxanthine 0.03 95% Ethanol 70 Polyoxyethylene hydrogenated castor oil (6OEO) 1 Propylene glycol 5 Perfume Trace water 100

Example 5 A lotion was prepared by a conventional method according to the following formulation. Blending amount (% by weight) Hydroxyethyl cellulose 0.4 Ethanol 5 Butane-1,3-diol 5 Paraoxybenzoic acid ester 0.2 Theobromine 0.05 Flavor 1 Water 100

Example 6 A lotion was prepared by a conventional method according to the following formulation. Blending amount (% by weight) Hydroxyethyl cellulose 0.4 Ethanol 5 Butane-1,3-diol 5 Paraoxybenzoic acid ester 0.2 Theophylline 0.05 Perfume 1 Water 100

Example 7 A hair cream was produced by a conventional method according to the following formulation. Blending amount (% by weight) Beeswax 5 Lanolin 4 Vaseline 5 Liquid paraffin 33 Polyoxyethylene (2OEO) Sol 4 Bitan monostearate Paraoxybenzoate 0.2 Perfume Trace theobromine 0.2 Borax 1 Water 100

Example 8 A hair cream was produced by a conventional method according to the following formulation. Blending amount (% by weight) Beeswax 5 Lanolin 4 Vaseline 5 Liquid paraffin 33 Polyoxyethylene (2OEO) sol 4 Bitan monostearate paraoxybenzoate 0.2 Perfume Trace theophylline 0.1 Borax 1 Water 100

[0021]

INDUSTRIAL APPLICABILITY According to the present invention, the xanthine derivative has a strong hair nourishing action and can significantly exhibit effects such as hair loss prevention and hair growth promotion.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁵ Identification code Internal reference number FI technical display location C07D 473/10

Claims (2)

[Claims] 1. Formula (I): (In the formula, R 1 is hydrogen or an alkyl group having 1 to 6 carbon atoms,
R2 represents hydrogen or an alkyl group having 1 to 6 carbon atoms. )
A hair nourishing agent containing at least one compound selected from the xanthine derivatives represented by. 2. The xanthine derivative is theobromine, theophylline, 3-methyl-7-propylxanthine, 3-
The hair nourishing agent according to claim 1, which is methyl-1-propylxanthine.