艾曲波帕片的制备和溶出度评价

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以艾曲波帕(1)自制片和参比制剂Promacta在含0.2%Tween-80的pH 6.8磷酸盐缓冲液(PBS)中溶出曲线的相似因子(f2)为主要考察指标,采用单因素试验筛选了自制片处方;用正交设计优化了制粒工艺。采用优化后的处方工艺制备3批小试1片,分别比较了其与参比制剂在pH 1.0盐酸、pH 4.5乙酸盐缓冲液、pH 6.8磷酸盐缓冲液和水4种介质中的溶出行为相似性,用相似因子法进行评价。结果表明,4种介质中的f_2值均大于56,说明自制片与参比制剂体外溶出行为相似;且各批次间差异较小,说明处方工艺稳定,可进行进一步的放大研究。 The similarity factor (f2) of elmipat (1) self-made tablet and reference preparation Promacta in pH 6.8 phosphate buffered saline (PBS) containing 0.2% Tween-80 was taken as the main index and single factor Self-made tablets were tested in the experiment. The orthogonal design was used to optimize the granulation process. Three batches of small test tablets were prepared by the optimized prescription process, and their dissolution behaviors were compared with reference preparations in pH 1.0 HCl, pH 4.5 acetate buffer, pH 6.8 phosphate buffer and water respectively Similarity, using similarity factor method for evaluation. The results showed that the values ​​of f_2 in all four media were greater than 56, indicating that the in vitro dissolution behavior of self-made tablets was similar to that of reference tablets. The difference between batches was small, indicating that the pretreatment process was stable and further amplification studies were possible.
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