abstract |
A new class of biodegradable pharmaceutical preparations useful as sustained release medicinal preparations, including the manufacturing and use processes of these preparations, as described and required. The process of making these preparations involves the steps of: a) dry mixing of a pharmaceutically active molecule with a biodegradable polymer; b) extrusion of the melt mixture to form a solid solution of the active molecule in the polymer; and c) grinding the solid solution to form the microparticles so that they can be formed into the injection formulations. Preferred embodiments include pharmaceutical preparations of polylactidic glycolide and (+) - α- (2,3-dimethoxyphenyl) -1- (2- (4-fluorophenyl) ethyl) -4-piperidinmethanol (active ingredient) and a process for their formation. These preparations release the active ingredient at a constant rate over a period of days to weeks. The active ingredient antagonizes the effects of serotonin on the 5HT2A receptor and is useful in treating a variety of conditions such as, for example, mental illness including schizophrenia, obsessive coercive disease, sleeping sickness, depression, anorexia, anxiety, drug propensity, and bipolar disease. |