替米沙坦快溶片的制备及评价

A. Shatla, M. Osman
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引用次数: 0

摘要

目的:提高替米沙坦的溶出度,研制舌下给药快速崩解片(fdt)。方法:采用溶剂蒸发技术,分别以胶脲44/14 (A式)、聚乙二醇4000 (PEG4000) (B式)、Pluronic F68 (C式)、羟丙基甲基纤维素E5 (HPMC E5) (D式)为原料制备药物二元固体分散体系(SDS),最后用碳酸氢钠与药物在(0.5:1)比例(公式E)和(1:1)比例(公式F)。利用FTIR光谱、热分析和x射线衍射评估这些体系的药物溶出度以及药物的物理化学变化。结果:采用碳酸氢钠制备的制剂与采用不同类型聚合物制备的制剂相比,可显著提高药物的溶出率。药物前5min溶出度增强顺序为:E式> F式> D5,各剂型药物溶出率分别为88.94±1.31、84.77±1.1、72.6±0.81(平均值+ SD)。快速溶出的替米沙坦片剂之所以选用E式,是因为与聚合物制备的固体分散体相比,E式药物的溶出性增强,口腔口感更佳,材料相对便宜,易于加工。结论:碳酸氢钠可用于替米沙坦FDT的制备,且溶出速度快。结论:碳酸氢钠可用于替米沙坦FDT的制备,且溶出速度快
本文章由计算机程序翻译,如有差异,请以英文原文为准。
PREPARATION AND EVALUATION OF RAPIDLY DISSOLVING ‎TABLET OF TELMISARTAN
Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT ‎with fast dissolution rate.‎
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