Sustained delivery formulations of risperidone compounds

摘要

The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite, or a prodrug thereof.

主权项

1. A method for treating schizophrenia in a human in need thereof comprising administering a flowable composition to the human once per month by subcutaneous injection to treat the schizophrenia;
wherein the flowable composition comprises: (a) about 15 wt % risperidone base in (b) about 45 wt % of an 80/20 poly(DL-lactide-co-glycolide) biodegradable thermoplastic polyester with a terminal carboxy group having an average molecular weight of about 10,000 Daltons to about 50,000 Daltons; and (c) about 55 wt % of N-methyl-2-pyrrolidone.