FORMULATION AND EVALUATION OF IMPLANTABLE DRUG DELIVERY OF DISULFIRAM

Abstract

Disulfiram is widely prescribed to discourage alcoholics from drinking alcohol. The effectiveness of oral disulfiram as a treatment for alcoholism is severely limited due to its poor bioavailability and poor patient compliance. To minimize the failure of the orally administered drug, efforts have been made to prepare alternative dosage form of subcutaneously implantable disulfiram pellets or tablets. In the present study an attempt has been made to design and evaluate a disulfiram implant using plain drug. The disulfiram implants have been formulated by direct compression and the effect of parameters like pH of site of administration (6.0 and 7.4) and sterilization were studied on in-vitro release of implantable disulfiram pellets. In- vitro release has been studied by vial and rotary flask shaker methods. The release kinetic mechanism from all the formulation was found to be zero order. The in vitro release data of all the formulations was compared with that of marketed disulfiram implant (Esperal). In contrast to other formulation in vitro release from marketed formulation appeared to be independent of hydrodynamics of diffusion (volume of dissolution media and agitation speed). The present study had revealed that, in-vitro drug release from implants is unaffected by pH of site of administration and gamma ray sterilization. Both the methods (Vial Method & Rotating Flask Method) of in vitro dissolution testing are found significantly different for formulations prepared in laboratory but not for marketed formulation, indicating the different mechanism of release of marketed formulation.