SUSTAINED-ACTION BUPRENORPHINE

BUPRENORPHINE HAS BEEN SHOWN TO SUPPRESS HEROIN USE BY ADDICTS, AND STUDIES INDICATE THAT IT MAY BE A USEFUL TREATMENT FOR OPIOID DEPENDENCE. THIS PARTIAL AGONIST-ANTAGONIST COMBINES THE ADVANTAGES OF BOTH METHADONE AND NALTREXONE, AND BUPRENORPHINE WAS PREFERRED BYPOSTADDICTS OVER METHADONE AND NALTREXONE. THE OVERALL OBJECTIVE OF THIS PROGRAM IS TO DEVELOP A SUSTAINED-ACTION FORMULATION OF MICROENCAPSULATED BUPRENORPHINE THAT IS EFFECTIVE FOR 1 MONTH AND TO PREPARE DOCUMENTATION TO SUPPORT AN IND APPLICATION FOR INITIAL CLINICAL TRIALS. PHASE I WILL DEMONSTRATE THE FEASIBILITY OF THE PROJECT. INJECTABLE BUPRENORPHINE MICROCAPSULES WILL BE PREPARED USING BIOTEK INC.'S, AIR-SUSPENSION COATING PROCESS AND EVALUATED FOR IN VITRO DRUG RELEASE KINETICS. PHARMACOKINETIC STUDIES WILL BE UTILIZED TO DETERMINE IN VIVO RELEASE RATES. IN VIVO AND IN VITRO RELEASE RATES WILLBE COMPARED AND CORRELATED TO PROCESS VARIABLES. PHASE I STUDIES WILL PROVIDE THE METHODOLOGICAL BASIS FOR FURTHER DEVELOPMENT OF THE FORMULATION IN PHASE II. DURING PHASE II, THE PROTOTYPE DEVELOPMENT WILL BE COMPLETED, EFFICACY AND SAFETY TESTS CONDUCTED, AND MANUFACTURING PROCEDURES DEFINED TO SUPPORT AN IND APPLICATION IN ANTICIPATION OF HUMAN TRIALS.