Fenofibrate microparticles
AssigneeJagotec AG
InventorINDU PARIKH
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Abstract
Fenofibrate microparticles are prepared using a combination of surface modifiers with a phospholipid. Particle size growth and stability are controlled while significantly smaller sized fenofibrate particles are produced.
Claims15
A pharmaceutical composition comprising fenofibrate containing microparticles produced by applying energy to fenofibrate in the presence of phospholipid and surface modifier(s), said microparticles consisting essentially of fenofibrate, a phospholipid and at least one surface modifier in which the surface modifier or surface modifiers provide volume-weighted mean particle size values of the water-insoluble compound about 50% smaller than particles produced in the presence of a phospholipid and without the presence of the surface modifier using the same energy input.
A pharmaceutical composition comprising fenofibrate containing microparticles produced by applying energy to fenofibrate in the presence of phospholipid and surfactant surface modifier, said microparticles consisting essentially of fenofibrate, a phospholipid and at least one non-ionic, anionic or cationic surfactant, in which the surfactant or surfactants provide volume-weighted mean particle size values of the water-insoluble compound about 50% smaller than particles produced in the presence of a phospholipid and without the presence of the surfactant using the same energy input.
In a process of preparing fenofibrate microparticles comprising reducing the particle size by sonication, homogenization, milling, microfluidization and precipitation, or recrystallization and precipitation of the fenofibrate using antisolvent and solvent precipitation or precipitation from supercritical fluids the improvement comprising the steps of:
- (1) prior to or during particle size reduction, mixing the fenofibrate 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 fenofibrate about 50% smaller than particles produced without the presence of the surfactant using the same energy input.
A process of stabilizing fenofibrate microparticles and preventing particles from aggregating or flocculating by coating or adhering onto the surfaces of the fenofibrate particles a mixture of a phospholipid together with at least one non-ionic, anionic or cationic surfactant, the process comprising the steps of:
- (1) mixing said particles with a phospholipid and 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 said compound about 50% smaller than particles produced without the presence of the surfactant using the same energy input.
Dependencies are inferred from the claim text.