FORMULATION AND EVALUATION OF NOVEL FLOATING IN SITU GELLING SYSTEM OF MACROLIDE ANTIBIOTIC USING DIFFERENT GELLING POLYMERS

Abstract

Floating drug delivery system comes with the advantage of sustained release of drugs over a prolonged period of time thereby maximising the oral absorption of drugs with narrow absorption window, thus, it overcomes the challenges of conventional oral drug delivery system. In situ gelling system is a novel approach towards this. The aim of the present work was to develop a novel floating in situ gelling system for sustained drug delivery of Azithromycin dihydrate for eradication of H. pylori. In situ gelling system were prepared by dissolving different concentrations of gelling polymers like sodium alginate, xanthan gum, gellan gum in deionized water at 80 0 C. After cooling to 40 0 C fixed amount of drug and calcium carbonate were dispersed in it with continuous stirring. Compatibility between drug and polymers were confirmed by FTIR studies. All formulations showed pH in the range of 6.4 to 6.9, drug content was found to be in the range of 97.29% to 99.27%, floating lag time was less than 1 min, duration of floating was more than 24 h for all the prepared formulations. It was observed that the gelling capacity, viscosity and water uptake by the gel increased with the increase in polymer concentration. In vitro drug release was found to be in between 82.11% to 89.49%, up to 8 h, and the maximum drug release was shown by formulation F1. Drug release responded inversely with the increase in polymer concentration. The release kinetics of all the formulations followed Higuchi diffusion mechanism. Hence, a floating in situ gelling system of Azithromycin dihydrate could be prepared using different concentrations of gelling polymers to increase the patient compliance with reduced dosing frequency and increased residence time of drug in the stomach for better eradication of H. pylori.