Formulation and in vitro evaluation of an effervescent floating tablet of cefpodoxime proxetil prepared as an amorphous solid dispersion

Abstract

This study aimed to prepare an effervescent floating tablet to protect cefpodoxime proxetil (CP) from enzymatic hydrolysis and higher pH degradation in the lower parts of the gastrointestinal tract (GIT). CP was prepared as amorphous solid dispersion (ASD) with soluplus and Polyvinylpyrrolidone K30 (PVP K30) in a ratio of 1:1:1 by solvent evaporation technology. Effervescent floating tablet formulations were prepared in different compositions and ratios by direct compression techniques using polyethylene oxide (PEO), hydroxypropyl methylcellulose K4M (HPMC K4M), sodium alginate (Na alginate) as a hydrophilic matrix, sodium bicarbonate (NaHCO3), and citric acid as a gas-generating agent. These formulations were evaluated for floating ability and in vitro drug release. Then, an optimized tablet was performed to determine the hardness, friability, content uniformity, weight variation, and swelling index. The optimum formulation showed good buoyancy properties and extended drug release characteristics for 24 hours (hrs). The post-compression evaluation's parameters are within the limits of U.S. Pharmacopoeia. According to these results, the development of effervescent floating tablets of CP prepared as ASD could be effectively applied.