Jain Akash, Pandey Vikas, Ganeshpurkar Aditya, Dubey Nazneen, Bansal Divya
Pharmaceutics Research Laboratory and.
Drug Deliv. 2015 May;22(3):306-11. doi: 10.3109/10717544.2014.891273. Epub 2014 Mar 7.
The purpose of the present study was to formulate and characterize Nizatidine-encapsulated microballoons for enhancing bioavailability and increasing the residence time of drug in the gastrointestinal tract.
Microballoons were prepared using emulsion solvent diffusion method using Eudragit S-100 and HPMC as the polymer. The formulation process was optimized for polymer ratio, drug: polymer ratio, emulsifier concentration, stirring speed, stirring time. Optimized formulation was subjected to scanning electron microscopy, drug entrapment, buoyancy studies, in-vitro drug release and in-vivo floating efficiency (X-ray) study. In-vivo antiulcer activity was assessed by ethanol-induced ulcer in murine model.
The microballoons were smooth and spherical in shape and were porous in nature due to hollow core. A sustained release of drug was observed for 12 h. Examination of the sequential X-ray images taken during the study clearly indicated that the optimized formulation remained buoyant and uniformly distributed in the gastric contents for a period of 12 h. In ethanol-induced ulcer model, drug-loaded Microballoon-treated group showed significant (p < 0.01) ulcer protection index as compared to free drug-treated group.
Nizatidine-loaded floating microballoons may serve as a useful drug delivery system for prolonging the gastric residence time and effective treatment of gastric ulcers.
本研究的目的是制备并表征尼扎替丁包封的微球，以提高生物利用度并延长药物在胃肠道中的停留时间。
采用乳液溶剂扩散法，以Eudragit S - 100和羟丙基甲基纤维素（HPMC）为聚合物制备微球。对聚合物比例、药物与聚合物比例、乳化剂浓度、搅拌速度、搅拌时间等制剂工艺进行了优化。对优化后的制剂进行扫描电子显微镜观察、药物包封率测定、漂浮性能研究、体外药物释放研究和体内漂浮效率（X射线）研究。通过乙醇诱导的小鼠溃疡模型评估体内抗溃疡活性。
微球形状光滑呈球形，由于具有中空结构而具有多孔性。观察到药物持续释放12小时。研究期间拍摄的连续X射线图像检查清楚地表明，优化后的制剂在12小时内保持漂浮状态并均匀分布在胃内容物中。在乙醇诱导的溃疡模型中，与游离药物治疗组相比，载药微球治疗组显示出显著（p < 0.01）的溃疡保护指数。
载尼扎替丁的漂浮微球可作为一种有用的药物递送系统，用于延长胃停留时间并有效治疗胃溃疡。
