Antimycotic pharmaceutical composition

Abstract

In a pharmaceutical composition for external use containing a compound such as luliconazole and / or a salt thereof in an amount of 5% by mass or more, comprised is / are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and / or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and / or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and / or a salt thereof produced under a preservation condition of 60° C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and / or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C. immediately after manufacture; and 3) no crystal is deposited when the preparation is preserved at 5° C. for 2 weeks after manufacture.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application is the U.S. National Phase under 35 U.S.C. §371 of International Application PCT / JP2010 / 056881, filed Apr. 9, 2010, which claims priority to JP Application No. 2009-111551, filed Apr. 9, 2009 and JP 2009-111552, filed Apr. 9, 2009.TECHNICAL FIELD [0002] The present invention relates to a pharmaceutical composition, and more specifically, to an antimycotic pharmaceutical composition for external use useful for treatment of mycoses. BACKGROUND ART [0003] A compound represented by the general formula (1) as typified by, for example, luliconazole has an excellent antimycotic activity, and it has been pointed out that the compound may be applied to treatment of onychomycosis, which could not be treated by external administration hitherto (for example, see Patent document 1). However, in the case of producing such formulation for treatment of onychomycosis, there is a demand to further increase the content of the compound rep...

AI Technical Summary

Benefits of technology

The present invention provides a pharmaceutical composition for external use that contains a compound represented by the general formula (1) and / or a salt thereof in an amount of 5% by mass or more. The composition has good solubilization and steric stabilization properties, and it is clear and stable without any crystal deposition at different temperatures. Furthermore, the composition contains a low amount of impurities and the amount of stereoisomer of the compound is low after preservation.

Problems solved by technology

However, there was a situation in which only a few solvents could be used for producing a formulation containing such compound in a high concentration because of its high crystallinity.

That is, some kinds of solvents caused deficiency including crystal deposition when a low temperature condition such as 5° C. and crystal deposition during application.

However, such solvents may also be blended in a limited amount because of medicinal effects such as anti-inflammatory effects inherently possessed by the solvents, and it has been desired to develop a novel solvent for a formulation of luliconazole or the like as an alternative of the solvents.

However, there has been no finding that acetone serves as a solvent for stably solubilizing luliconazole or the like while maintaining a steric structure of luliconazole or the like, in the pharmaceutical composition for external use containing luliconazole or the like.

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