Development and Optimization of Amoxicillin Floating Raft System to effectively treat Helicobacter pylori infection

Abstract

Introduction: The aim of the present study was to develop and to characterize the Floating raft system (FRS) of Amoxicillin to enhance gastric residence time and drug release to target Helicobacter pylori effectively. Method: In the present study, guar gum, Glyceryl Monostearate (GMS), Calcium carbonate were selected as factors. Gelation duration (h), floating lag time (min), and % Cumulative drug release (CDR) were selected as responses. 23 factorial design with replicates was selected for experimentation. Results: It was observed that Guar gum and GMS were the major factors affecting gelation duration, increase in the quantity of both Guar gum and GMS increased gelation duration i.e., sustained gelation period (24 h). Floating time increased with an increase in the amount of guar gum and calcium carbonate, whereas an increase in the quantity of GMS decreased floating time. Guar gum, calcium carbonate, and GMS exhibited an antagonistic effect on % CDR. Contour plots were used to identify design space; further numerical analysis yielded 12 best solutions based on desirability. FRS exhibited greater AUCo-t, Cmax, tmax, and t1/2 when compared to marketed formulation approximately 2.30 folds enhancement and prolongation with a sustained release for greater than 24 h that might be due to better gelation. Conclusions: It can be concluded that the floating raft system was successfully developed by the Design of experiment (DoE) application with fewer trails and by utilizing easily available excipients for better floating, gelation, and sustained delivery of the drug.