Inclusion complex of nicardipine or its hydrochloride with beta-cyclodextrin and a sustained release pharmaceutical preparation containing the same

Abstract

There is described a new inclusion complex of nicardipine or its hydrochloride with beta-cyclohdextrin, which is prepared by admixing nicardipine or its hydrochloride with beta-cyclodextrin in a molar ratio of the compounds 1:0.9-1.1 under stirring at a temperature from about room temperature to the boiling temperature of the reaction mixture in an aqueous or ethanolic medium, cooling the reaction mixture to 0.degree. to 5.degree. C. and isolating the desired complex. The inclusion complex of nicardipine or its hydrochloride posesses cerebrovascular-vasodilatory and coronary-vasodilatory properties, which are equally well expressed as those of nicardipine or its hydrochloride themselves, yet owing to the better solubility of the complex at a higher pH range, such as it exists e.g. in the intestinal tract, the manufacture of sustained release pharmaceutical forms is made possible, whereby a greater extent of dissolution of the active substance is provided also in the intestinal juice.

Dependencies are inferred from the claim text.