Composition and method of preparing microparticles of water-insoluble substances
AssigneeResearch Triangle Pharmaceuticals
InventorsIndu Parikh, Ulagaraj Selvaraj
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Abstract
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.
Claims5
In a process of preparing cyclosporin microparticles, the process comprising reducing the particle size by sonication, homogenization, milling, microfluidization and precipitation, or recrystallization and precipitation of the cyclosporin using antisolvent and solvent precipitation
- the improvement comprising the steps of:
- (1) prior to or during particle size reduction, mixing the cyclosporin particles with (a) a natural or synthetic phospholipid and (b) at least one non-ionic, anionic or cationic surfactant, and thereafter
- (2) applying energy to the mixture sufficient to produce volume-weighted mean particle size values of cyclosporin about 50% smaller than particles produced without the presence of the surfactant using the same energy input.
Dependencies are inferred from the claim text.