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Formulation and evaluation of novel stomach specific floating microspheres bearing famotidine for treatment of gastric ulcer and their radiographic study

机译:新型法莫替丁治疗胃溃疡的胃特异性漂浮微球的制备,评价及影像学研究

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摘要

Objective: To develop and characterize multiple-unit-type oral floating microsphere of famotidine to prolong gastric residence time and to target stomach ulcer. Methods: The floating microspheres were prepared by modified solvent evaporation method. Eudragit S-100 was used as polymer. Microspheres were characterized for the micromeritic properties, floating behavior, entrapment efficiency and scanning electron microscopy. The in-vitro release studies and floating behavior were studied in simulated gastric fluid at pH 1.2. Different drug release kinetics models were also applied for all the batches. Selected formulations were also subjected for X-ray radiographic study. Results: Floating microspheres were successfully prepared by modified solvent evaporation technique. Microspheres showed passable flow properties. The maximum yield of microspheres was up to (95.11±0.35)%. On the basis of optical microscopy particle size range was found to be ranging from (52.18±182.00) to (91.64±5.16) µm. Scanning electron microscopy showed their spherical size, perforated smooth surface and a cavity inside microspheres. Microspheres were capable to float up to 20 h in simulated gastric fluid. X-ray radiographic studies also proved its better retention in the stomach. Conclusions:On the basis of the results, such dosage forms may be a good candidate for stomach targeting and may be dispensed in hard gelatin capsules.
机译:目的:开发和表征法莫替丁的多单元型口腔漂浮微球,以延长胃停留时间并靶向胃溃疡。 方法:采用改进的溶剂蒸发法制备漂浮微球。 Eudragit S-100用作聚合物。表征了微球的微团性质,漂浮行为,包封效率和扫描电子显微镜。在pH 1.2的模拟胃液中研究了体外释放研究和漂浮行为。不同批次的药物释放动力学模型也都适用。选定的制剂也要进行X射线放射照相研究。 结果:通过改进的溶剂蒸发技术成功制备了漂浮微球。微球显示出合格的流动性质。微球的最大产率高达(95.11±0.35)%。根据光学显微镜,发现粒径范围为(52.18±182.00)至(91.64±5.16)μm。扫描电子显微镜显示其球形大小,穿孔的光滑表面和微球内部的空腔。微球能够在模拟胃液中漂浮长达20小时。 X射线射线照相术研究也证明其在胃中的保留更好。 结论:根据结果,此类剂型可能是靶向胃的良好候选药物,可以分配在硬明胶胶囊中。

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