Abstract

The aim of the present investigation was to increase the gastric residence time of cefuroxime axetil by preparing gastro retentive mucoadhesive tablet, thereby improving bioavailability of cefuroxime axetil. Tablets were prepared using different mucoadhesive polymers such as hydroxypropylmethyl cellulose K4M, carbopol 974P, sodium alginate, and chitosan in combination ratios by wet granulation method. All the batches were subjected to various evaluation parameters such as physicochemical properties, swelling index, in vitro residence time, and in vitro drug release. Optimized formulation containing carbopol 974P and chitosan in combination (F6) exhibited maximum in vitro residence time of 10.05 h and in vitro release up to 45.89% in 10 h. The F6 formulation was further subjected to in vitro permeation, scanning electron microscope (SEM), stability studies and in vivo residence time. SEM revealed smooth surface characteristics with increasing pore diameter, indicating the diffusion mechanism of release. Stability was conducted as per International Conference on Harmonisation (ICH) guidelines at 40 ± 20°C/75 ± 5% relative humidity (RH) and the values were within permissible limits. In vivo X-ray photographs taken during the experiment showed mucoadhesion to the gastric mucosa up to 10 h.

Key words: Cefuroxime axetil, gastro retentive, mucoadhesive polymers, X-ray study.