Risperidone sustained release microsphere composition

摘要

A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

主权项

1. A pharmaceutical composition suitable for parenteral administration, comprising:
an active component selected from the group consisting of risperidone, or a salt thereof, and 9-hydroxy risperidone or a salt thereof; and a polymer blend consisting essentially of a first uncapped poly(lactide-co-glycolide) and a second uncapped poly(lactide-co-glycolide), wherein the weight content of the active component in the pharmaceutical composition is within a range from 10% to 60%; a weight content of the polymer blend in the pharmaceutical composition is within a range from 40% to 90%; and the pharmaceutical composition is present in the form of microspheres; and wherein the first uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.4-0.9 dl/g, a molar ratio of lactide to glycolide of 65:35 to 90:10; and the second uncapped poly(lactide-co-glycolide) has an intrinsic viscosity of 0.1-0.35 dl/g a molar ratio of lactide to glycolide of 50:50 to 75:25.