Sustained delivery formulations of risperidone compound

Abstract

The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating to 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 a solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite or a prodrug thereof.

1 - 65 . (canceled) 
     
     
         66 . A pharmaceutical composition comprising risperidone base in a solution which comprises a means for achieving sustained release of the risperidone. 
     
     
         67 . The composition of  claim 66 , wherein the composition comprises about 10 wt % to about 50 wt % of the risperidone base. 
     
     
         68 . The composition of  claim 67 , wherein the composition comprises about 10 wt % to about 20 wt % of the risperidone base. 
     
     
         69 . The composition of  claim 68 , wherein the composition comprises about 15 wt % of the risperidone base. 
     
     
         70 . The composition of  claim 66 , wherein the composition comprises about 90 mg of risperidone base. 
     
     
         71 . The composition of  claim 66 , wherein the composition comprises about 120 mg of risperidone base. 
     
     
         72 . The composition of  claim 66 , wherein the means provides steady-state risperidone plasma levels for four to six weeks after subcutaneous injection into a human subject. 
     
     
         73 . The composition of  claim 66 , wherein the means produces a steady state plasma level of risperidone within about three days after injection into a human patient. 
     
     
         74 . The composition of  claim 66 , wherein the means produces a steady state plasma level of risperidone from about three days to about forty-two days after injection into a human patient. 
     
     
         75 . The composition of  claim 74 , wherein the steady state plasma level of risperidone is from about 28.9 ng/mL to about 50.7 ng/mL. 
     
     
         76 . The composition of  claim 66 , wherein the means produces maximum plasma concentration (C max ) levels of risperidone within about six hours of subcutaneous injection into a human subject. 
     
     
         77 . The composition of  claim 66 , wherein the means produces maximum plasma concentration (C max ) levels of risperidone within about two hours of subcutaneous injection into a human subject. 
     
     
         78 . The composition according to  claim 66 , wherein the means produces a risperidone concentration of at least 15.8 ng/mL for about twenty-eight days after injection into a human patient. 
     
     
         79 . The composition according to  claim 66 , wherein the means produces a linear sustained release of risperidone for at least twenty-eight days. 
     
     
         80 . A method of treating schizophrenia in a human subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of the composition of  claim 66 . 
     
     
         81 . The method of  claim 80 , comprising subcutaneously injecting the human subject with the composition once every twenty-eight days. 
     
     
         82 . The method of  claim 80 , comprising subcutaneously injecting the human subject with the composition once per month. 
     
     
         83 . The method of  claim 80 , wherein the composition comprises about 90 mg of risperidone base. 
     
     
         84 . The method of  claim 80 , wherein the composition comprises about 120 mg of risperidone base. 
     
     
         85 . The method of  claim 80 , wherein the human subject is not administered a supplemental daily oral dose of risperidone. 
     
     
         86 . The method of  claim 80 , wherein the human subject is not administered a supplemental daily oral dose of risperidone for the first twenty-one days of the method of treating schizophrenia. 
     
     
         87 . The method of  claim 80 , wherein the method provides therapeutic plasma risperidone levels immediately after administration. 
     
     
         88 . The method of  claim 80 , wherein the means provides steady-state risperidone plasma levels for four to six weeks after subcutaneous injection into a human subject. 
     
     
         89 . The method of  claim 80 , wherein the means produces a steady state plasma level of risperidone within about three days after injection into a human patient. 
     
     
         90 . The method of  claim 80 , wherein the means produces a steady state plasma level of risperidone from about three days to about forty-two days after injection into a human patient. 
     
     
         91 . The method of  claim 90 , wherein the steady state plasma level of risperidone is from about 28.9 ng/mL to about 50.7 ng/mL. 
     
     
         92 . The method of  claim 80 , wherein the means produces maximum plasma concentration (C max ) levels of risperidone within about six hours of subcutaneous injection into a human subject. 
     
     
         93 . The method of  claim 80 , wherein the means produces maximum plasma concentration (C max ) levels of risperidone within about two hours of subcutaneous injection into a human subject. 
     
     
         94 . The method according to  claim 80 , wherein the means produces a risperidone concentration of at least 15.8 ng/ml for about twenty-eight days after injection into a human patient. 
     
     
         95 . The method according to  claim 80 , wherein the means produces a linear sustained release of risperidone for at least twenty-eight days. 
     
     
         96 . The method of  claim 80 , wherein the composition comprises about 10 wt % to about 50 wt % of the risperidone base. 
     
     
         97 . The composition of  claim 96 , wherein the composition comprises about 10 wt % to about 20 wt % of the risperidone base. 
     
     
         98 . The composition of  claim 97 , wherein the composition comprises about 15 wt % of the risperidone base.