JPH0212925B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a novel preparation for preventing migraine cephalic eruption, so-called "dandruff", and the itching sensation associated therewith. Generally, the causes of dandruff are considered to be abnormal exfoliation of the epidermal keratin of the scalp and excessive secretion of sebum, and it is thought that the growth of microorganisms further worsens the problem. However, at present, there is currently no drug that is specifically effective for preventing abnormal exfoliation of the epidermis and excessive secretion of sebum, not only for topical preparations but also for oral administration. Therefore, at present, only indirect anti-dandruff agents are used that use disinfectants to suppress the growth of microorganisms. However, there is not necessarily a direct relationship between the growth of microorganisms and the occurrence of dandruff, and therefore, these conventional anti-dandruff agents not only do not have sufficient efficacy, but also have poor safety and formulation stability. However, there were many drawbacks such as odor, and no fundamental solution had been reached. In view of this current situation, the present inventors continued intensive research into the anti-dandruff effects of many compounds, and found, quite unexpectedly, that they were thought to have nothing to do with preventing dandruff. Furthermore, the histamine H ₂ receptor antagonist containing an imidazole ring, which had only been administered orally, has not only achieved its intended purpose as an anti-dandruff agent by topically administering it, but has also improved its safety, formulation stability, and They finally discovered that it was a substance that was completely satisfactory in terms of odor and other aspects. The present invention was completed based on such new findings, and relates to an anti-dandruff agent characterized by containing a histamine H ₂ receptor antagonist containing an imidazole ring. Any substance that can be used as an active ingredient in the present invention is widely used as long as it is a histamine H ₂ receptor antagonist containing an imidazole ring. For example, cimetidine, methyamide, brimamide, etc. represented by the following formula are preferred, but are not limited to these. These active ingredients are applied directly to the hair and/or scalp, and in that case, each ingredient may be used alone or several may be used in combination. These active ingredients can be formulated into any dosage form as long as they are applied as hair products. For example, these active ingredients may be dissolved in an appropriate solvent and used directly.
In addition, shampoo, hair, hair rinse,
Hair creams, hair oils, hair liquids, pomades and various other formulations can be used as appropriate without particular limitation. There is no particular restriction on the amount used, and it can be selected appropriately depending on the dosage form, compounding base, etc., but it is usually better to mix it at 0.5% or more, preferably within the range of 1 to 20%. is preferable. It is also possible to use it in combination with conventionally used anti-dandruff agents, especially fungicides, and particularly good results can be obtained when these are used in combination. For formulation, a histamine _H2 receptor antagonist containing an imidazole ring is dissolved, dispersed, or mixed in a suitable base or solvent, and then a surfactant and an additive are added to adjust the dosage form. Foaming agents, emulsifiers, thickeners, oils, hydrotropes, conditioning agents, bactericidal preservatives, pigments, fragrances, antiperspirants, deodorants, scalp stimulants, hair treatment agents, baldness treatment agents , hair tonic, etc. are added to formulate a formulation. Pharmaceutical ingredients that exhibit particularly excellent effects when used in combination with the active ingredient of the present invention include, for example, zinc pyrithione, β-naphthol, Hyamine (trade name of Rohm and Haas Company, USA), diuniper tar oil, tartaric acid, citric acid, adipine. acid,
Examples include fungicides, anti-dandruff agents, scalp stimulants, hair treatment agents such as lead acetate, selenium sulfide, African hot pepper, cantharis, pilocarpine nitrate, quinine hydrochloride, Balsam of Peru, Chiara, saponin and others. A histamine _H2 receptor antagonist containing an imidazole ring may be added and mixed at the same time as these disinfectants and other ingredients, or if necessary, each ingredient can be added and mixed little by little. .
As the preparation method, conventional methods in the art can be used as appropriate. Drugs, shampoos, hair styling products, etc. containing imidazole ring-containing histamine H ₂ receptor antagonists can completely prevent dandruff and the itching sensation associated with it when used in a conventional manner. It is clear from Test Examples 1 to ₃ described below that histamine H ₂ receptor antagonists have extremely outstanding effects as anti-dandruff agents. It is not only extremely stable, but also has excellent advantages in terms of safety and odor. In order to demonstrate that histamine _H2 receptor antagonists are extremely effective in preventing dandruff, test examples 1-
3 and then further describe embodiments of the invention. Test example 1 (1) Preparation of test solution

[Table] (2) Test method For 7 test subjects who complained of “dandruff,” they first washed their hair with commercially available soap, then applied about 10 c.c. of tonic (B) to their heads and rubbed it into the scalp thoroughly to prevent dandruff. The occurrence of itching was determined daily according to the following criteria. Then, when dandruff and itching clearly increased, the hair was washed again with soap and tonic (A) was applied in the same manner, and the occurrence of dandruff and itching was determined over time. Judgment criteria: (-) No dandruff or itching (±) Slight dandruff or itching (+) Dandruff or itching () Significant dandruff or itching The results are shown in the table. Test example 2 (1) Preparation of test solution

[Table] (2) Test method The hair of 7 subjects who complained of "dandruff" was first washed with Shampoo (B), and the occurrence of dandruff and itching was determined over time according to the criteria of Test Example 1.
Then, when dandruff and itching clearly appeared, the hair was washed with Shampoo (C), and dandruff and itching were similarly investigated. When the amount of dandruff and itching increases again, wash your hair with shampoo (B), conduct the same examination over time, and when the amount of dandruff and itching increases again, use shampoo.
Hair was washed in (A), and dandruff and itching were investigated in the same manner. The results are shown in the table. Test example 3 (1) Preparation of test solution

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[Table] (2) Test method The occurrence of dandruff and itching after using Tonic (D) and (C) was determined in the same manner as in Test Example 1 for 7 subjects who complained of "dandruff". The results are shown in the table. As is clear from the above test results, histamine H ₂ receptor antagonists such as cimetidine and methyamide have shown excellent preventive effects against dandruff and itching. Furthermore, the results of Test Example 2 show that the efficacy of cimetidine exceeds that of zinc pyrithione. In addition, at the same time as this experiment, the stability of tonics (A), (C), and shampoo (A) over time was monitored by thin layer chromatography, and it was found that they were stable in terms of formulation, with no spots of decomposition products observed. It was done.

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[Table] Examples of anti-dandruff agents according to the present invention are shown below, and the numerical values in the examples represent weight % unless otherwise specified. Example 1 Transparent Shampoo 1 Sodium lauryl sulfate 25 2 Lauric acid diethanolamide 5 3 Propylene glycol 5 4 Cimetidine 5 5 Preservatives, fragrances Appropriate amount 6 Purified water Add to make 100 ml The above ingredients are uniformly dissolved to prepare a product. Example 2 Weakly acidic shampoo 1 Amisoft CT-12 (manufactured by Ajinomoto) 50 2 Sodium lauryl sulfate 5 3 Lauric acid diethanolamide 5 4 Propylene glycol 5 5 Cimetidine 5 6 Zinc pyrithione 1 7 Flavoring, pigment Appropriate amount 8 Purified water Add to make 100 ml 1 to 5 and 8 are dissolved by heating at about 70°C. During cooling, 6 is added and thoroughly dispersed by high-speed stirring, and finally 7 is added to form a product. Example 3 Cream shampoo 1 Sodium lauryl sulfate 25 2 Lauric acid diethanolamide 5 3 Ethylene glycol monostearate 2 4 Methamide or preamide 5 5 Preservatives, pigments, fragrances Appropriate amount 6 Purified water Add to make 100 ml Mix the above ingredients uniformly and make it into a product. Example 4 Hair tonic 1 Ethanol 80 ml 2 Vegetable oil 2 3 Propylene glycol 5 4 Cimetidine 3 5 Purified water Add to make 100 ml The above ingredients are uniformly dissolved to obtain a product. Example 5 Hair rinse 1 Stearyldimethylbenzyl ammonium chloride 1.5 2 Stearyl alcohol 0.5 3 Glyceryl monostearate 2 4 Methyamide or ranitidine 3 5 Preservatives, pigments, fragrances Appropriate amount 6 Purified water Add to make 100ml Mix the above ingredients uniformly. and make it into a product. Example 6 Hair oil 1 Ethanol 3 2 Methyamide 2 3 Perfume Appropriate amount 4 Vegetable oil Add to make 100 ml The above ingredients are mixed uniformly to prepare a product. Example 7 Pomade 1 Wood wax 10 2 Castor oil 87.5 3 Cimetidine 2 4 Fragrance 0.5 After heating and dissolving 1 and 2 at 70°C, 3 and 4 are added and dispersed. It is then placed in a metal pan and rapidly cooled to solidify and form the product. Example 8 Hair liquid 1 Polyoxypropylene butyl ether 15 2 Ethanol 60 ml 3 Cimetidine 2 4 Perfume Appropriate amount 5 Purified water Add to make 100 ml Dissolve the above uniformly to obtain a product.

Claims (1)

[Claims] 1. An anti-dandruff agent characterized by containing a histamine _H2 receptor antagonist containing an imidazole ring as an active ingredient.