In vivo Evaluation of Amoxicillin Trihydrate and Clarithromycin-Loaded Mucoadhesive Microspheres for H. pylori Eradication

摘要

Purpose: To evaluate in vivo H. pylori clearance efficacy of formulated mucoadhesive microspheres of amoxicillin trihydrate and clarithromycin. Methods: Amoxicillin trihydrate and clarithromycin mucoadhesive microspheres were prepared by solvent evaporation method using Carbopol 974P, HPMC K4M and Eudragit RS 100. In vivo clearance efficacy of the microspheres was evaluated in a Wistar rat model after induction of H. pylori infection. Amoxicillin and clarithromycin-loaded microspheres were administered twice daily for three days. H. pylori clearance was evaluated by assessing colony count. Results: Treatment with plain drug solution (90 mg/kg amoxicillin and 45 mg/kg clarithromycin) resulted in a colony count of log 1.25 ± 0.56 CFU and clearance rate of 60 %, while mucoadhesive microspheres-loaded dose of 45 mg/kg amoxicillin and 22.5 mg/kg clarithromycin resulted in complete (100 %) eradication of H. pylori infection. Conclusion: The developed mucoadhesive amoxicillin/clarithromycin microspheres can potentially be used to effectively eradicate H. pylori infection.