替米沙坦胃保留给药系统的研制与评价

M. Goyal, A. Dubey, L. Yadav
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引用次数: 0

摘要

目的:研究替米沙坦的胃保留系统,延长其胃停留时间和生物利用度。材料与方法:采用非水溶剂蒸发法制备含kollidon sr的替米沙坦漂浮微球,以不同浓度的kollidon sr配制共5个配方,并对制备的漂浮微球进行粒径测定、SEM、收率、包封效率、体积和密度、可压缩性指数、静置角、体外可浮性、FT-IR研究和体外药物释放等评价参数。结果:各配方均表现出良好的流动性能。在pH为1.2的盐酸缓冲液中进行体外溶出研究,以评估制备的漂浮微球制剂的释放情况。5种制剂均表现出药物缓释。配方F3的FT-IR光谱显示出与纯药物相似的所有峰,排除了对药物与辅料配伍性的怀疑。结论:用kollidon SR可成功制备替米沙坦漂浮微球,提高了替米沙坦在胃中的停留时间和生物利用度。关键词:悬浮微球,Kollidon SR,非水溶剂蒸发法,PEG 4000,固体分散
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Evaluation of Gastroretentive Drug delivery System of Telmisartan
Purpose: The aim of the present study was to develop a gastro retentive system of telmisartan to prolong its gastric residence time and bioavailability. Materials and Methods: Non aqueous solvent evaporation method was used to prepare floating microspheres of telmisartan with kollidon SR. Total five formulations were made with varying concentration of kollidon SR. Prepared floating microspheres were subjected to various evaluation parameters, such as particle size determination, SEM, percent yield, entrapment efficiency, bulk and tapped density, compressibility index, angle repose, In vitro floatability, FT-IR study and In vitro drug release. Results: All the formulations displayed good flow properties. In vitro dissolution studies in HCl buffer pH 1.2 were performed to assess the release profile of prepared floating microsphere formulations. All the five formulation displayed sustained release of drug. FT-IR spectra of formulation F3 exhibited all the peaks as similar to the FT-IR spectra of pure drug, rejecting any doubts about the compatibility between drug and the excipients. Conclusion: We can conclude that kollidon SR can be successfully used to prepare floating microspheres of telmisartan to increase its gastric residence time and bioavailability. Key words: Floating microsphere, Kollidon SR, Non aqueous solvent evaporation method, PEG 4000, Solid dispersion.
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