PREFORMULATION, FORMULATION DEVELOPMENT AND DRUG RELEASE STUDIES OF CLOPIDOGREL BISULPHATE FLOATING MICROBALLOONS

Multi particulate systems are of greater importance than the single unit dosage forms in oral drug delivery. Floating micro balloons are among the best methods to increase gastric retention among all the multi particulate drug delivery systems. They offer more reproducible drug absorption, reduce the risk of local irritation and improve the bioavailability of the drug. In the current research work, clopidogrel, a BCS class – II drug, was formulated as controlled release micro balloons using ethyl cellulose as polymer and span 80 as the surfactant. The pre-formulation studies viz. solubility, partition coefficient, micromeritics were carried for the Clopidogrel bisulphate pure drug, and the drug excipient compatibility studies were carried using Fourier transform infrared spectrophotometer and Differential Scanning Calorimeter. Different formulations of floating micro balloons were prepared by solvent evaporation method by altering five process and formulation factors viz. concentration of surfactant, the volume of solvent, volume of internal phase, the concentration of polymer, speed of rotation. All the Clopidogrel micro balloons were subjected to in-vitro drug release and kinetic studies, and the results were analyzed suitably. The highest drug release rate was found to be 0.274 h -1 in the F15 formulation. The Peppas n values of all the formulations were above 0.5, indicating that the drug release mechanism of all formulated clopidogrel micro balloons was non-fickian diffusion.