Abstract

The formation of a stable inclusion complex between tolbutamide and permethyl-β cyclodextrin was systematically studied. It shows that permethyl-β-CD forms a 1 : 1 complex with tolbutamide. Its molecular structure was elucidated by physicochemical methods including IR and high field NMR analysis. The influence of pennethyl-β-cyclodextrin on the hypoglycemic effect of tolbutamide was evaluated by measuring the blood glucose level. The reduction in plasma glucose was significantly greater when the rabbits were treated with the complex than with tolbutamide alone. The enhancement of the bioavailability of tolbutamide by permethyl-β-cyclodextrin is likely attributed to the molecular inclusion effect.

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