CONTROLLED RELEASE FLOATING ORAL IN SITU GEL OF ITOPRIDE HYDROCHLORIDE USING PH SENSITIVE POLYMER

Objective: In situ gels are suitable to overcome problems of immediate release and short gastrointestinal residence of liquids. These systems are liquids before administration and on contact with gastric contents are converted to gel. The present work deals with the formulation, evaluation and optimization of pH triggered floating oral in situ gel of Itopride hydrochloride by using sodium alginate as a gelling polymer and HPMC K100M as a release retardant polymer. Methods: A 3 2 factorial designs was carried out and the effect of variation in concentrations of sodium alginate and calcium carbonate on percent drug release at 1 h, 6 h, gel strength and T 50% i. e. time required for the release 50 % of loaded drug was evaluated. The gels were studied for their viscosity, in vitro buoyancy and drug release, in vitro gelling capacity, density, gel strength. Results: The results of a 3 2 full factorial design revealed that the concentration of sodium alginate and concentration of calcium carbonate significantly affected the dependent variables. A controlled release profile was observed for these formulations. The dissolution data were fitted to various kinetic models which indicated diffusion controlled release profile. In vivo studies revealed higher T max of gel compared to plain drug which is suggestive of slower absorption. However, the AUC 0-12 h was found to be nearly 90% higher than plain drug. Thus, bioavailability was found to be increased with in situ gel of Itopride hydrochloride. Conclusion: Floating oral in situ gelling system of amoxicillin can be formulated using sodium alginate as a gelling polymer to sustain the drug release for 12 h with diffusion controlled release kinetics.