Cefuroxime axetil loaded gastroretentive floating tabletsbased on hydrophilic polymers: preparation and in vitro evaluation

Abstract

The aim of this work was to study the formulation and in vitro characterization of hydro dynamically balanced floating matrix tablets using Cefuroxime axetil (CA) as model drug. Different excipients such as hydroxy propyl methyl cellulose (HPMC) K15M, E5LV (gelling agent), sodium bicarbonate (gas generating agent) and sodium lauryl sulfate (SLS) (solubility enhancer) were used in order to optimize the drug release profile as well as floating property. Decrease in release characteristics with high viscous polymer were observed due to increased gel strength, tortuosity and length of drug diffusion path. Significant difference (p<0.5) in release rate was found at different concentration of SLS. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The release rate, extent and mechanism were governed by the content of polymer. The polymer content and amount of floating agent significantly affected the time required for 50%of drug release (t50%), mean dissolution time (MDT), release rate constant, and diffusion exponent (n).Kinetic modeling of dissolution profile revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was co-dominated by diffusion polymer erosion in the release mechanism.