abstract |
PURPOSE: To obtain a composition for percutaneous administration, containing emedastine and lower alkyl esters of an aliphatic carboxylic acid, useful for systemic treatment of various allergic diseases caused by histamine and excellent in percutaneous absorbability of the emedastine. n CONSTITUTION: The objective substance obtained by mixing and stirring 1-(2- ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole (referred to as emedastine) and a lower alkyl ester of an aliphatic monocarboxylic acid or a dilower alkyl ester of an aliphatic dicarboxylic acid at ambient temperature or while heating and preparing a pharmaceutical. The aforementioned esters are used in an amount of 0.5-20 times weight ratio based on the emedastine. The above-mentioned composition is mixed with normal pharmaceutical additives, prepared in the form of lipophilic ointment, gel, cream, lotion, spray, etc., applied or sprayed on the epithelium and percutaneously administered. n COPYRIGHT: (C)1991,JPO&Japio |