EVALUATION OF SUSTAINED CONTROLLED-RELEASE DOSAGE FORMS OF 3-HYDROXY-3-METHYLGLUTARYL COENZYME A (HMG-COA) REDUCTASE INHIBITORS IN DOGS AND HUMANS

Seven sustained/controlled-release dosage forms were designed for gastrointestinal delivery of lovastatin or simvastatin, two potent HMG-CoA reductase inhibitors for the treatment of hypercholesterolemia. The in vivo performance of these formulations was evaluated in dogs and healthy volunteers in terms of the cholesterol lowering efficacy and/or systemic concentrations of HMG-CoA reductase inhibitors. Results from the present and previous studies suggest that, through the controlled release of HMG-CoA reductase inhibitors, sustained lower plasma concentrations of HMG-CoA reductase inhibitors may result in an equal or better therapeutic efficacy.