Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

Abstract

Background and Objectives: The prevention and treatment of peptic ulcers has become an important challenge in the current medicine world. Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time. Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials and Methods: Nine batches of the light liquid paraffin entrapped emulsion gel beads were prepared by a new emulsion gelation technique using sodium alginate and xanthan gum as polymers. The polymeric solution was extruded into Calcium chloride solution by the use of 21G needles. Morphology of beads, drug content, drug entrapment efficiency, floating lag time and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results: Mean surface diameter were between 1.220 ± 2.259% (F1) to 1.230 ± 2.316% (F9) and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric fluid at 37ºC. The drug content and drug entrapment efficiency among the formulations were between 17.48%~19.68% and 71.06% ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion: The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12