Improved bioavailability through floating microspheres of lovastatin

Lovastatin is an antihyperlipidemic agent which has low bioavailability due to the extensive first pass metabolism. It was sought to increase gastric retention of lovastatin by development of a sustained release gastroretentive drug delivery system leading to reduced fluctuation in the plasma concentration and improved bioavailability. MEHODS: Floating microspheres were prepared by emulsion solvent diffusion technique, using various polymers and their blends. The in vitro performance was evaluated for drug-polymer compatibility, percent yield, particle size, drug entrapment efficiency, in vitro onset and duration of floatation, in vitro drug release as well as in vivo determination of serum cholesterol level.

The mean particle size of microspheres was observed to be between 6.9 to 9.5 µm and the maximum particle size was around 50 µm. In vivo studies of the selected batches indicated lower level of serum cholesterol compared to the marketed tablet at the same dose but was not significant.

The data obtained in this study suggested that a microparticulate floating dosage form of lovastatin can be successfully designed to yield controlled delivery with improved therapeutic efficacy.