维特克拉体内体外相关性研究

发布时间：2018-05-15 17:20

  本文选题：维特克拉 + 溶出曲线　； 参考：《中国药学杂志》2017年17期

【摘要】：目的考察维特克拉(venetoclax)制剂的体外释药行为和在比格犬体内的药动学过程,进行体内体外相关性(IVIVC)的研究。方法研究测定了维特克拉制剂在不同溶出介质中的溶出曲线;建立维特克拉在比格犬血浆样品中的HPLC测定方法,并对市售的维特克拉片进行饱腹和空腹下比格犬体内的药动学研究;将药物在体外累积溶出度数据与在体内的累积吸收百分数数据进行线性回归,进行IVIVC研究。结果维特克拉制剂在4种不同溶出介质中体外的释药行为存在明显差异;建立了维特克拉比格犬血样测定方法,该方法简单、准确;维特克拉制剂饱腹和空腹的AUC_(0→∞)分别为(32.38±5.87)和(27.70±6.32)mg·h·L~(-1),达峰浓度分别为(4.04±0.78)和(3.72±0.69)μg·m L~(-1),达峰时间分别(6.01±1.04)和(4.27±0.92)h,其中AUC_(0→∞)和达峰时间的差异具有显著性(P0.05);体内吸收百分数与在0.2%SDS pH 6.8介质中的体外溶出度有良好的IVIVC。结论食物可提高维特克拉制剂的生物利用度;本实验筛选出的0.2%SDS pH 6.8介质(桨法,75r·min~(-1))可以作为与该制剂体内释药相关的体外溶出条件。
[Abstract]:Objective to investigate the in vitro drug release behavior and pharmacokinetic process in Beagle dogs, and to investigate the in vivo and in vitro correlation of Vitamin B venetoclax (IVIVC). Methods the dissolution curve of Vitela preparation in different dissolution media was determined, and the HPLC method was established for the determination of Vitela in Beagle's plasma samples. The pharmacokinetics of Viterka tablets on the market was studied in full and empty stomach, and the cumulative dissolution data in vitro and the cumulative absorption percentage data in vivo were linear regressed, and the IVIVC study was carried out. Results there were significant differences in drug release behavior in vitro among the four different dissolution mediums, and a simple and accurate method was established for the determination of blood samples in Vitro Clapiga canines. The AUC_(0 鈭，

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