Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar 470 003, Madhya Pradesh, India.
J Pharm Sci. 2009 Nov;98(11):4229-36. doi: 10.1002/jps.21742.
A multiparticulate system having pH-sensitive property and specific enzyme biodegradability for colon-targeted delivery of metronidazole was developed. Pectin microspheres were prepared using emulsion-dehydration technique. These microspheres were coated with Eudragit(R) S-100 using oil-in-oil solvent evaporation method. The SEM was used to characterize the surface of these microspheres and a distinct coating over microspheres could be seen. The in vitro drug release studies exhibited no drug release at gastric pH, however continuous release of drug was observed from the formulation at colonic pH. Further, the release of drug from formulation was found to be higher in the presence of rat caecal contents, indicating the effect of colonic enzymes on the pectin microspheres. The in vivo studies were also performed by assessing the drug concentration in various parts of the GIT at different time intervals which exhibited the potentiality of formulation for colon targeting. Hence, it can be concluded that Eudragit coated pectin microspheres can be used for the colon specific delivery of drug.
开发了一种具有 pH 敏感性和特定酶可生物降解性的多颗粒系统,用于甲硝唑的结肠靶向递送。采用乳化-脱水技术制备果胶微球。然后使用油包油溶剂蒸发法,用 Eudragit(R) S-100 对这些微球进行包衣。SEM 用于对这些微球的表面进行特征描述,可以看到微球上有明显的涂层。体外药物释放研究表明,在胃 pH 条件下没有药物释放,但在结肠 pH 条件下,制剂中可以观察到药物的持续释放。此外,在存在大鼠盲肠内容物的情况下,制剂中药物的释放量更高,表明结肠酶对果胶微球的作用。通过在不同时间间隔评估胃肠道各部位的药物浓度也进行了体内研究,这表明该制剂具有结肠靶向的潜力。因此,可以得出结论,Eudragit 包衣果胶微球可用于药物的结肠特异性递送。