Preparation and characterization of sodium alginate-carbopol-934Pbased mucoadhesive microbeads

[摘要] The purpose of the research work was to formulate and evaluate oral sustained release microspheres of clarithromycin for the treatment of Helicobacter pylori. The stomach specific alginate carbopol microbeads were selected in order to improve patient compliance by simplifying its administration, improving its therapeutic effect and reducing its dose related side effects. To eradicate the H. pylori, stomach specific alginate carbopol microbeads were prepared, by orifice ion-gelation process using different ratio of polymers. The microbeads were characterized by particle size, percentage drug entrapment efficiency, % adhering, antibacterial activity in terms of % Growth Inhibition [GI] and stability study. Sizes of microbeads were found in the range of 800-980 μm, SEM photomicrograph showed microbeads with smooth surface and spherical shapes. The percentage drug entrapment was up to 80 %. In vitro drug release studies were performed in phosphate buffer saline [PBS, pH 7.4] and simulated gastric fluid [SGF, pH 1.2] at 37±20C. In vitro and in vivo mucoadhesive study was performed on albino rats, which showed that microbeads were remained adhered to mucus membrane of stomach for longer period of time. The efficacy of formulation was determined in term of its percentage growth of inhibition on H. pylori. The Stability studies were performed at different storage conditions. The site specific as well as sustained release of antibiotic could decrease the likelihood of significant systemic toxicity and may provide selective delivery of biologically active molecules on the site of action. The developed systems could possibly improve site specific release of drug at bacterial site and selectively kill the micro organism.

[学科分类] 药理学