Studies of the Interaction of Betacyclodextrin with Ampicillin, Methicillin and Phenytoin

The interaction of betacyclodextrin with ampicillin, methicillin and phenytoin has been investigated. All three drugs, (in the unionized form) interact strongly with betacyclodextrin. It is suggested that the interaction of all three drugs with betacyclodextrin could perhaps be exploited to pharmaceutical advantage. For ampicillin it is possible that the complex may have an improved bioavailability and a reduction in the incidence of gastro-intestinal side effects in comparision with the uncomplexed drug. For methicillin the significant extension of the hydrolytic half life for the complex makes the oral route a possibility for this drug, which is normally given intravenously because of stability problems. The interaction of phenytoin with betacyclodextrin produces a complex with a substantially enhanced solubility likely to give greatly improved bioavailability and a reduction in intra and inter subject blood level variation.