使用UHPLC-MS/MS在人血中同时量化巴洛克萨维尔马博西尔及其活性代谢物:应用于与不同抗凝剂的人类药理学研究的应用
Haiyan Liu1, Simeng Xu1, Tingting Yang2
1Hunan Creates Med Technology Co., Ltd, Changsha 410205, China.
Journal of pharmaceutical and biomedical analysis
|July 31, 2024
概括
与肝素管相比,乙二胺四酸 (EDTA) 抗凝管可能会低估50%的巴洛克萨维尔酸 (BXA) 水平. 这种差异是由于EDTA造成的.
科学领域:
- 药理动力学和药物新陈代谢
- 分析化学 分析化学
- 临床药理学 临床药理学
背景情况:
- 巴洛克萨维尔马博西尔 (BXM) 是一种抗病毒前药物,通过代谢转化为其活性形式,巴洛克萨维尔酸 (BXA).
- 精确量化血中的BXA对于药理动力学研究至关重要.
- 乙二胺四酸 (EDTA) 和肝素是常见的抗凝剂,但使用EDTA的BXA药理动力学数据有限.
研究的目的:
- 开发和验证一种敏感的超高性能液体染色学-并联质谱法 (UHPLC-MS/MS) 方法,用于同时量化人体血中的BXM和BXA.
- 为了比较使用EDTA收集的血中BXA的药理动力学参数与肝素抗凝管.
主要方法:
- 开发了一种快速的UHPLC-MS/MS方法,用于在50μL人体血样本中量化BXM和BXA.
- 用酸的氨和酸用于蛋白质沉.
- 染色分离是在C18柱上进行的,该柱具有梯度移动相,并使用三重四极质谱仪进行检测.
主要成果:
- 在UHPLC-MS/MS方法中,在BXM和BXA量化方面表现出卓越的线性,精度和准确性.
- 提取回收和矩阵效应都在可以接受的范围内.
- 药理动力学研究显示,EDTA血中的BXA测量比肝素血低约50%,这可能是由于EDTA的金属离子化特性.
结论:
- 一种经过验证,高效和敏感的UHPLC-MS/MS方法能够准确量化人体血中的BXM和BXA.
- 抗凝剂的选择显著影响BXA的药物动力学参数,EDTA管导致低估的药物度与肝素管相比.
- 这一发现强调了在BXA治疗药物监测和临床研究中考虑抗凝剂类型的重要性.
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