Prochlorperazine Maleate Loaded Sustained Release Floating Microspheres prepared by Ionotropic Gelation Technique: Morphology and Release Characteristics

Abstract

Once a daily oral sustained release microsphere based floating formulation of Prochlorperazine Maleate (PCZM) was prepared with intent of reduction in frequency of administration which will increase the bioavailability and further to enhance the patient compliance thus avoiding treatment failure. For treatment of vommiting and nausea, PCZM is a drug of choice. PCZM, phenothiazine antipsychotic, has low biological half life and required multiple dosing frequency (3–4 times daily). Ionotropic gelation technique was used to prepare a sustained release floating microsphere using calcium chloride as complexing agent, sodium alginate release retarding agent, and sodium bicarbonate as gas generation mediator. Different formulation batches F1 to F7 were prepared andevaluated for percent yield, entrapment efficiency, micrometric properties, floating lag time, total floating time and In-vitro dissolution study. Optimized formulation batch F6was subjected for physical characterization and morphological study like DSC, PXRD, FTIR and SEM respectively. Results of In-vitro dissolution study of optimized formulation batch F6 showed sustained release property with floating characteristic of PCZM microspheres for more than 24 hrs. Release study of Optimized formulation F6 followed Korsmeyer's Peppas model release kinetics with non-fickian diffusion. SEM study revealed spherical shape of the microspheres with rough and porous surface.