Injections

#The present invention relates to an injectable composition comprising a benzimidazole compound having an antiulcer action, and a process for producing the same.

#As injectable compositions comprising a 2-[(2-pyridyl)methylsulfinyl]benzimidazole compound having an antiulcer action, for example, the following injectable compositions have been reported.

#1) Japanese Patent Application Laid-Open No. 138213/1990 (JP-2-138213A) (EP 0356143) discloses an injectable solution which comprises a benzimidazole compound having an antiulcer action and at least one of ethanol, propylene glycol and polyethylene glycol. The literature also discloses an injectable solution which contains a freeze-dried product of the benzimidazole compound dissolved in a mixture solution of an acidic substance and a polyethylene glycol, and further contains a saccharide such as mannitol and N-methylglucamine. Further, in Example 4 of the literature, 1 g of lansoprazole was dispersed in a distilled water for injection, and 3 ml of 1N-aqueous sodium hydroxide solution was added thereto to dissolve lansoprazole, followed by addition of water to make up to the total of 50 ml. The mixture was subjected to sterile filtration. The resulting filtrate was filled in a portion into vials, followed by lyophilization. The lyophilized powder was dissolved in a dissolving solvent composed of N-methylglucamine, hydrochloric acid and a polyethylene glycol.

#FIG. 1 is the graph demonstrating the results of Experimental Example 5.

#FIG. 2 is the graph demonstrating the results of Experimental Example 6.

#The injectable composition of the present invention comprises the compound (I) and a strong alkali in equivalent ratio of about 1:1. That is, the injectable composition comprises about 1 equivalent of the strong alkali relative to 1 mol of the compound (I).

#In the compound (I), examples of the “substituent” of the “benzene ring which may have a substituent” shown by the ring A include, for example, a halogen atom, a cyano group, a nitro group, an alkyl group which may have a substituent, a hydroxyl group, an alkoxy group which may have a substituent, an aryl group, an aryloxy group, a carboxyl group, an acyl group, an acyloxy group, and a 5- to 10-membered heterocyclic ring. The benzene ring may be substituted with about 1 to 3 substituents. When substituted with two or more substituents, each of substituents may be same or different. Among these substituents, a halogen atom, an alkyl group which may have a substituent, and an alkoxy group which may have a substituent are preferred.

#As the halogen atom, there may be mentioned fluorine, chlorine, bromine atoms and the like. In Particular, a fluorine atom is preferred.