Composition and method of preparing microparticles of water-insoluble substances

摘要

Pharmaceutical compositions containing cyclosporin microparticles are prepared by applying energy to cyclosporin particles in the presence of phospholipid and one or more surface modifiers. These microparticles consist essentially of cyclosporin, a phospholipid and at least one surface modifier. The surface modifier or surface modifiers yield particles of a volume-weighted mean particle size the cyclosporin about 50% smaller than cyclosporin particles produced in the presence of a phospholipid only and without the presence of the surface modifier using the same energy input.