美托洛尔漂浮基质片的设计与表征

V. Bakshi, .S Swapna, D. Choudhary, C. Revanth, B. Praveen, C. Praveen
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引用次数: 0

摘要

目的:研制基质包埋型美托洛尔漂浮片,提高药物的持续活性和胃停留时间,提高药物的生物利用度。美托洛尔之所以被选为模型药物,是因为它在胃中比下消化道吸收得更好。方法:实验工作分为制剂前研究、制剂研制和评价三个阶段。药品和辅料的标准化确认了样品的真实性。对所有制剂进行漂浮试验,在溶出度测试仪- ii中进行体外溶出度研究,FTIR研究解释药物与辅料的相互作用。结果:对15个配方进行了浮动试验,其中有5个配方(F1、F3、F5、F7、F14)通过了浮动试验。体外释放动力学研究表明,美托洛尔为缓释药,体外8 h为零级释放,释药时间为95%。并与市售产品Metolar进行了药物释放谱比较。浮片将药物释放时间延长至8小时。用傅里叶变换红外光谱(FTIR)评价了药物与聚合物的相互作用。结论:F3方漂浮效果最佳。F3与Metolar(已上市产品)的比较研究表明,F3与Metolar具有相似的体外释药特征。因此,优化后的配方F-3可成功用于高血压的治疗。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design and characterization of metoprolol floating matrix tablet
Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract. Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction. Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro . The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR). Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.
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