Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles

Abstract

Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.

1 . A formulation, comprising: 
 sustained-release microparticles comprising a biodegradable and biocompatible polymer and an active agent selected from the group consisting of risperidone, 9-hydroxy-risperidone, and pharmaceutically acceptable acid addition salts of the foregoing, wherein the formulation is administered by injection and has a duration of action for the treatment of psychotic disorders of from about 7 days to about 200 days.    
   
   
       2 . A formulation, comprising: 
 sustained-release microparticles produced by dissolving in a solvent an active agent and a biodegradable and biocompatible polymer to form an organic phase, wherein the active agent is selected from the group consisting of risperidone, 9-hydroxy-risperidone, and pharmaceutically acceptable acid addition salts of the foregoing, and extracting the solvent to form microparticles, wherein the formulation is administered by injection and has a duration of action for the treatment of psychotic disorders of from about 7 days to about 200 days.