Evaluation of Prepared Sustained Release Floating Tablet of Cefpodoxime Proxetil

Author(s): Krishna Murari, Amresh Gupta, Ajay Kumar Dubey, Umesh Kumar Mishra and Arpita Singh

Abstract: Cefpodoxime proxetil (CP) is an orally active broad spectrum, third generation cephalosporin ester prodrug. It has been widely used in the treatment of mild to moderate respiratory tract infections; pharyngitis and tonsillitis. In spite of its favorable clinical response, Cefpodoxime proxetil is a prodrug with poor bioavailability because of its metabolism to Cefpodoxime acid in the luminal contents and intestinal epithelial cells. However, the high solubility, chemical and enzymatic stability, and absorption profile of CP in acidic pH values (of stomach) and time dependent killing of bacteria’s, points to the potential of a sustained release gastro retentive dosage form in altering the absorption profile of Cefpodoxime proxetil and to maximize the duration of exposure to the bacteria’s. Thus the objective of the present study was development and optimization of sustained release gastro retentive drug delivery system (bi-layered floating tablet) for Cefpodoxime proxetil. HPMC is a semi-synthetic polymer selected for the study because it is nontoxic, nonirritant stable in wide pH range and freely available. The solubility and solution stability studies of Cefpodoxime proxetil were conducted in different dissolution media. The drug excipients compatibility studies were carried out by FT-IR analysis. Bi-layered floating tablets were prepared by direct compression method. The tablets were subjected to physicochemical, buoyancy, swelling index and in-vitro release studies. Other excipients like sodium bicarbonate and citric acid were added in floating layer to achieve desired buoyancy. Microcrystalline cellulose and lactose were added in the release layer to achieve a sustained release product with drug release profile as uniform as possible. The results concluded that stable and persistent buoyancy was achieved by trapping the gas by the hydration of high viscosity grade HPMC K100M. This study showed that there is a potential for this novel intragastric, floating two-layer tablet to remain in the stomach for a longer time. Moreover, the two distinct layers allow separate regulation of the floating ability and drug release kinetics.

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