Comparison of pharmacokinetics and pharmacodynamics of a conventional and a new rapidly dissolving glibenclamide preparation

Abstract Glibenclamide is an oral hypoglycemie agent used in the treatment of non-insulin dependent diabetes. It is a weak acid and is poorly soluble in water. In this investigation, the pharmacokinetics and pharmacodynamics of a new rapidly dissolving formula (Oramide) containing only 3.5 mg of the drug was compared with a conventional 5 mg preparation (Daonil). The rate and extent of in vitro dissolution of Oramide was significantly higher than Daonil. Despite the higher amount of the drug in Daonil both preparations exhibited similar plasma glibenclamide concentration-time profiles. Furthermore, the release of insulin and the reduction of plasma glucose levels were not statistically different in both experimental groups. The faster dissolution rate of Oramide formulation has, therefore, rendered it bioequivalent to Daonil which contains a higher amount of active ingredient.