Preparation of mucoadhesive microspheres for the controlled gastric release of metronidazole

Abstract

Background: Metronidazole (MZ) is a drug used in combination in the treatment of stomach ulcers with the aim of destroying Helicobacter pylori (HP). However, due to the short period of residence in the stomach, the drug is quickly transferred into the intestine without significant release to the gastric mucosa, requiring the drug to be administered several times a day. In order to store the drug for a longer time in the stomach, enhance the therapeutic efficacy, reduce the number of medications, the aim of this study is to formulate mucoadhesive microspheres for the controlled gastric release of MZ and to evaluate some quality properties of the prepared products. Reseach Methods: MZ was from China,…. Microspheres were prepared by ionic gelation method based on investigating the elements of the formula and the process, and at the same time, microsphereswere characterized. Results: Microspheres formulation includes MZ 0.575%, NaHCO3 0,6%, Sodium Alginate 1.6%, Carbopol 934P 0.3%, HPMC K100M 0.4% and other excipients. Microspheres properties were evaluated in typical terms of appearance, entrapment efficiency, in vitro adhesion, in vitro drug release. Conclusion: The study has been successful in preparing and characterizing mucoadhesive microspheres for the controlled gastric release of MZ. Key words: Metronidazole, microspheres, mucoadhesive.