Exploration of nanocrystal technology for the preparation of lovastatin immediate and sustained release tablets

Abstract

The objective of this study was to explore the feasibility of using nanocrystal technology for the design of immediate and sustained release tablets of poorly water soluble drugs. Nanocrystal aggregates comprised of lovastatin, a model drug, 20% PVP K17 and 5% SDS were prepared by spray drying. The nanocrystal aggregates were mixed with lactose, Avicel Ph 101 and Ac-Di-Sol® (blank granules) or 316 Fast Flo® lactose, MCC PH200, and Ac-Di-Sol ® (direct compression), where the composition was optimized by uniform design. The blank granules adsorption method had superior flowability, filling and plastic deformation as well as rapid release rates, and the tableting process did not affect the release rate of nanocrystals. An optimized sustained release tablets formulation was also identified, which decreased the difference of drug release behavior under sink and non-sink conditions. In conclusion, nanocrystal technology is promising for preparing both immediate and sustained release tablets for poorly water soluble drugs with robust drug dissolution and release.