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Pharmacokinetics of Lusutrombopag, a Novel Thrombopoietin Receptor Agonist, in Rats by UPLC-MS/MS.
International Journal of Analytical Chemistry ( IF 1.8 ) Pub Date : 2020-05-30 , DOI: 10.1155/2020/7290470
Bo Wang 1 , Feifei Chen 2 , Quan Zhou 2 , Yunfang Zhou 2 , Deru Meng 2 , Peiwu Geng 2 , Ailian Hua 2 , Weiping Ji 1 , Changxiong Wang 2 , Shuanghu Wang 2 , Liming Hu 3
Affiliation  

Lusutrombopag is a second oral thrombopoietin (TPO) receptor agonist that selectively acts on human TPO receptors. In the study, UPLC-MS/MS was used to establish a selective and sensitive method to determine lusutrombopag with poziotinib as IS (internal standard) in rat plasma. Samples were prepared by precipitating protein with acetonitrile as a precipitant. Separation of lusutrombopag and poziotinib was performed on a CORTECS UPLC C18 column (2.1 ∗ 50 mm, 1.6 μm). The mobile phase (acetonitrile and water containing 0.1% formic acid) with gradient elution was set at a flow rate of 0.4 ml/min. The mass spectrometric measurement was conducted under positive ion mode using multiple reaction monitoring (MRM) of m/z 592.97 ⟶ 491.02 for lusutrombopag and m/z for poziotinib (IS) 492.06 ⟶ 354.55. The linear calibration curve of the concentration range was 2–2000 ng/ml for lusutrombopag, with a lower limit of quantification (LLOQ) of 2 ng/ml. RSD of interday and intraday precision were both no more than 9.66% with the accuracy ranging from 105.82% to 108.27%. The extraction recovery of lusutrombopag was between 82.15% and 90.34%. The developed and validated method was perfectly used in the pharmacokinetic study of lusutrombopag after oral administration in rats.

中文翻译:

通过UPLC-MS / MS,新型血小板生成素受体激动剂Lusutrombopag在大鼠体内的药代动力学。

Lusutrombopag是第二种口服血小板生成素(TPO)受体激动剂,可选择性作用于人TPO受体。在这项研究中,使用UPLC-MS / MS建立了选择性灵敏的方法,以poziotinib作为IS(内标)测定大鼠血浆中的鲁舒莫帕格。通过用乙腈作为沉淀剂沉淀蛋白质来制备样品。物上的CORTECS UPLC C18柱(2.1 * 50毫米,1.6进行lusutrombopag和poziotinib分离 μ M)。梯度洗脱的流动相(乙腈和含有0.1%甲酸的水)设定为0.4 ml / min的流速。质谱测量是在正离子模式下使用m / z 592.97⟶491.02的多发性多巴胺和多药监测进行的多反应监测(MRM)m / z代表poziotinib(IS)492.06⟶354.55。鲁邦通帕的浓度范围线性校准曲线为2-2000 ng / ml,定量下限(LLOQ)为2 ng / ml。日间和日内精度的RSD均不超过9.66%,精度范围为105.82%至108.27%。葡聚糖的提取回收率在82.15%至90.34%之间。这项经开发和验证的方法可完美地用于大鼠口服鲁舒托邦的药代动力学研究。
更新日期:2020-05-30
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