Quantitative determination of regorafenib and its two major metabolites in human plasma with high-performance liquid chromatography and ultraviolet detection.
Quantitative determination of regorafenib and its two major metabolites in human plasma with high-performance liquid chromatography and ultraviolet detection.
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高效液相色谱-紫外检测法定量测定人血浆中瑞戈非尼及其两种主要代谢物。
DOI：
10.1002/bmc.3730
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Shibata H.
中科院分区：
文献类型：
--
作者：
Fujita K;Miura M;Shibata H.
开发了一种简单、高灵敏度和特异性的高效液相色谱（HPLC）方法，用于同时定量人血浆中的瑞戈非尼、N-氧化代谢物（M-2）和去甲基N-氧化代谢物（M-5）。采用Capcell PAK MG II色谱柱，以0.5 mL/min的流速和UV 260 nm处的测量值，使用0.5% KH 2 PO 4（pH 3.5）-乙腈（30：70，v/v）的移动的流动相分离瑞戈非尼、M-2、M-5和内标索拉非尼。对于每种分析物，瑞戈非尼、M-2和M-5的定量下限均为10 ng/mL。使用固相萃取的程序仅需要少量血浆（100 μL）进行一次分析，同时提供高提取回收率（所有化合物>81%）和良好的选择性。瑞戈非尼、M-2和M-5的日内和日间测定的变异系数分别<12.2%、<12.3%和<15.1%。在10 - 10，000 ng/mL的线性范围内，瑞戈非尼的日内和日间测定准确度<9.4%，M-2 <8.0%，M-5 <12.8%。该方法适用于瑞戈非尼的临床药代动力学研究。本HPLC方法目前用于我们对接受治疗的患者进行的观察性研究。版权所有© 2016约翰威利父子有限公司.
A simple, highly sensitive and specific high‐performance liquid chromatography (HPLC) method was developed for the simultaneous quantitation of regorafenib,N‐oxidemetabolite (M‐2) and the desmethylN‐oxide metabolite (M‐5) in human plasma. Regorafenib, M‐2, M‐5 and the internal standard sorafenib were separated using a mobile phase of 0.5% KH2PO4(pH 3.5)–acetonitrile (30:70, v/v), on a Capcell PAK MG II column at a flow rate of 0.5 mL/min and measurement at UV 260 nm. The lower limits of quantification for regorafenib, M‐2 and M‐5 were 10 ng/mL for each analyte. A procedure using solid‐phase extraction required only a small amount of plasma (100 μL) for one analysis while providing high extraction recovery (>81% for all compounds) and good selectivity. Coefficients of variation for intra‐ and inter‐day assays were <12.2% for regorafenib, <12.3% for M‐2 and <15.1% for M‐5. Accuracies for intra‐ and inter‐day assays were <9.4% for regorafenib, <8.0% for M‐2 and <12.8% for M‐5 over a linear range from 10 to 10,000 ng/mL. This HPLC assay is suitable for clinical pharmacokinetic studies of regorafenib. The present HPLC method is currently in use for our observational studies of patients under treatment. Copyright © 2016 John Wiley & Sons, Ltd.
血浆中多激酶抑制剂瑞戈非尼的液相色谱-串联质谱测定。
DOI：
--
发表时间：
2014
期刊：
Biomedical chromotography
影响因子：
--
作者：
D. Luethi;S. Durmuş;A. Schinkel;J. Schellens;J. Beijnen;R. Sparidans
通讯作者：
R. Sparidans
摘要 1666：瑞戈非尼 (BAY 73-4506)：临床前药理学及其主要代谢物的临床鉴定和定量
影响因子：
11.2
作者：
D. Zopf;Roland Dr. Heinig;K. Thierauch;C. Hirth‐Dietrich;F. Hafner;O. Christensen;Tiffany Lin;S. Wilhelm;M. Radtke
通讯作者：
M. Radtke
影响因子：
1.8
作者：
Hafner, Frank-Thorsten;Werner, Daniel;Kaiser, Michael
通讯作者：
Kaiser, Michael