FORMULATION AND OPTIMIZATION OF BUPROPION HCl MICROSPONGES BY 23 FACTORIAL DESIGN

The rationale of the present study was to formulate & optimize the floating Bupropion HCl microsponges by 2³ factorial design. The concentration of ethyl cellulose (EC), polyvinyl alcohol (PVA) and Dichloromethane (DCM) were selected as independent variables. Floating lag time & % drug release were selected as independent variables. Factors, their levels (with values) were substituted in the design of experiment software (Sigma tech version 3.1). The effect of factors at different levels on response variable was predicted using poly nominal equations. FTIR studies revealed that no chemical interaction between drug & polymer used. DSC confirmed molecular dispersion of drug in the microsponges polymer matrix. Quasi emulsion solvent diffusion method was used to formulate microsponges. Bupropion HCl showed acceptable flow. The morphology of microsponges was studied using SEM and it was found that microsponges were spherical and porous. USP Type II dissolution apparatus with cellophane membrane was used to study in vitro drug release. Kinetic studies revealed that drug release from optimized formulation followed Higuchi’s model and diffusion is the controlled release mechanism. From Polynomial equations it was found that increase in concentration of PVA decreased floating lag time and % drug release. Optimized formulation studies showed satisfactory in vitro drug release for more than 16 h with less than 1 min floating lag time. Based on simulation (by DoE software) most economical batch (optimized) decided which were in desired range. The results demonstrated the effectiveness of proposed design for development of Bupropion HCl microsponges for the treatment of psychosis.