NANOCRYSTALLINE FORMULATION OF HUMAN IMMUNODEFICIENCY VIRUS (HIV) PROTEASE INHIBITOR USING CELLULOSIC SURFACE STABILIZER, AND METHOD FOR PRODUCING THE FORMULATION

摘要

PPROBLEM TO BE SOLVED: To provide a stable nanoparticle-containing composition including a slightly soluble crystalline HIV protease inhibitor having a water solubility of less than 10 mg/ml, wherein nanoparticles do not flocculate or agglomerate due to interparticle attractive force. PSOLUTION: The composition includes the slightly soluble crystalline HIV protease inhibitor having the water solubility of less than 10 mg/ml and adsorbing, on its surface, a cellulosic surface stabilizer in an amount sufficient to maintain an effective average particle size of less than 1,000 nm. The surface stabilizer is preferably selected from the group consisting of hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), HPC super low viscosity (HPC-SL), and HPC-low viscosity (HPC-L). The HIV protease inhibitor is particularly VX478. PCOPYRIGHT: (C)2010,JPO&INPIT