Enhancement of percutaneous absorption of molsidomine.

Abstract

Molsidomine, which is effective in treating angina pectoris, was poorly absorbed through the skin from a simple solution in oleic acid or propylene glycol, and its bioavailability was below 1% in rats. However, molsidomine was efficiently absorbed from a two-component system consisting of oleic acid and propylene glycol. Maximum absorption enhancement was observed in the two-component system containing 10% oleic acid; the bioavailability was about 95% within 6 h. Remarkable percutaneous absorption enhancement was also observed in the presence of linoleic acid when a series of unsaturated straight fatty acids with different carbon numbers were substituted for oleic acid. Lauric acid was the most effective in the series of saturated straight fatty acids. Effective percutaneous absorption enhancement also occurred with lauryl alcohol and oleyl alcohol, but little enhancement was observed with any fatty acid ester or sodium oleate. The two-component system is also effective for some water-soluble drugs and poorly water-soluble drugs, besides molsidomine.