Oral dosing formulations of dideoxy purine nucleosides

摘要

Improved oral dosage formulations for acid-labile dideoxy purine nucleoside derivatives such as ddA, ddI, and ddG, have been developed by incorporating selected water-insoluble buffering systems in the formulation. These novel formulations provide reduced mass dosage units in the form of convenient, palatable chewable/ dispersible tablets or a dry powder sachet. The reduced mass requirement, necessary to allow tablets of reasonable size, was achieved in part by an unexpected 20 to 25% increase in drug bioavailability resulting from use of the selected buffering systems comprised of an insoluble magnesium antacid agent and either dihydroxyaluminum sodium carbonate or calcium carbonate.