Formulation development of an oral dosage form for an hiv protease inhibitor, AG1284

Several preformulation characteristics of a series of novel HIV protease inhibitors were examined as a prelude to expedient oral dosage form development. Initial studies indicated that these compounds were orally bioavailable in rats (≤ 39%), but chemically unstable at low pH. AG1284 was selected as the lead compound from the series for further preclinical development based on its relatively high oral bioavailability and stability. The pH-rate...