Formulation and Evaluation of Gastroretentive Floating Beads of Cefuroxime Axetil

Abstract

Cefuroxime axetil is a second generation antibacterial agent belongs to cephalosporin group. It undergoes rapid metabolism in the intestinal mucosa due to change in pH environment and hence decreased oral bioavailability. A gastro retentive floating beads of cefuroxime axetil were formulated to increase the bioavailability. The floating beads were prepared by Ionotropic gelation method in which drug and calcium carbonate were dispersed in four different concentrations into a polymer mixture of three different combinations such as sodium alginate along with guar gum, sodium alginate with HPMC K4M, and sodium alginate with hydroxy ethyl cellulose solution and then dropping the dispersion into an acidified solution of 3% (w/v) calcium chloride. The prepared beads were evaluated for bead size, entrapment efficiency, in-vitro drug release, swelling study, buoyancy test, SEM, X-ray diffraction, FTIR and in vivo gastric retention time in albino rats. The drug entrapment efficiency was found to be in the range of 54.76 to 81.87%. The in-vitro drug release was observed up to 8 hr. The drug release followed Fickian transport. In vivo studies indicated that a significant increase in gastric residence time of beads.