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Assessment of a developed HPLC-MS/MS approach for determining plasma eupatorin in rats and its application in pharmacokinetics analysis

机译:评估用于测定大鼠血浆Eupatorin的发达的HPLC-MS / MS方法及其在药代动力学分析中的应用

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摘要

Eupatorin, a bioactive compound extracted from Java tea (Orthosiphon stamineus), possesses potent anti-cancer, anti-inflammatory and vasodilation activities. To date, no pharmacokinetics studies on eupatorin have yet been performed. Here, we established and validated a sensitive and selective LC-MS/MS (liquid chromatography-tandem mass spectrometry) approach for determining plasma eupatorin in rats. Chromatographic fractionation was conducted on a Wonda Cract ODS-2 C18 Column (4.6 mm x 150 mm, 5 mu m) with a mobile phase containing aqueous 0.1% formic acid and acetonitrile using a flow rate of 0.8 ml min(-1). In multiple reaction monitoring mode, precursor-to-product ion transitions for quantification of eupatorin and the internal standard were set at 343.1 -> 328.1 and 252.0 -> 155.9, respectively. The intra- and inter-day precision and accuracy were found to be below 6.72% and within +/- 8.26% in rat plasma, respectively. Meanwhile, all values of the matrix effect, recovery and stability were within the accepted ranges. Furthermore, we carried out the pharmacokinetic analysis using the developed method. The pharmacokinetic study revealed that while theC(max)(maximum plasma concentration) of eupatorin and time for reaching theC(max)(T-max) were 974.886 +/- 293.898 mu g L(-1)and 0.25 h, respectively, the half-life was 0.353 +/- 0.026 h. This study will be of great significance to the research on the pharmacology, clinical pharmacy and drug action mechanism of eupatorin.
机译:Eupatorin,从Java茶(肾茶)中提取的生物活性化合物,具有强效的抗肿瘤,抗炎和血管舒张活性。迄今为止,尚未执行上eupatorin无药代动力学研究。在这里,我们建立和验证一个灵敏的和选择性的LC-MS / MS(液相色谱 - 串联质谱法),用于确定在大鼠血浆eupatorin方法。色谱分离物上的网达Cract ODS-2 C18柱(4.6毫米×150毫米,5微米)用含有含水0.1%甲酸的流动相和乙腈使用为0.8ml分钟(-1)的流速进行。分别> 155.9, - > 328.1 252.0和 - 在多反应监测模式中,对于eupatorin的量化和内标前体到产物离子跃迁在343.1分别设置。帧内和日间精密度和准确度被发现是低于6.72%,并且在+/- 8.26%大鼠血浆中,分别。同时,基体效应,恢复和稳定性的所有值在可接受的范围内。此外,我们还进行了使用所提出的方法的药代动力学分析。药代动力学研究显示,虽然eupatorin和时间到达theC(最大值)的theC(最大)(最大血浆浓度)(T-max)分别分别是974.886 +/- 293.898亩克L(-1)和0.25小时,半衰期为0.353 +/- 0.026小时。这项研究将是对药理学,临床药学和eupatorin的药物作用机理的研究具有重要意义。

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  • 来源
    《RSC Advances》 |2020年第53期|共7页
  • 作者单位

    Hebei Med Univ Hosp 4 Dept Pharm Shijiazhuang 050011 Hebei Peoples R China;

    Hebei Med Univ Sch Pharm Dept Pharmaceut Anal Shijiazhuang 050017 Hebei Peoples R China;

    Hebei Med Univ Hosp 2 Shijiazhuang 050000 Hebei Peoples R China;

    Hebei Med Univ Hosp 2 Shijiazhuang 050000 Hebei Peoples R China;

    Hebei Med Univ Sch Pharm Dept Pharmaceut Anal Shijiazhuang 050017 Hebei Peoples R China;

    Hebei Med Univ Sch Pharm Dept Pharmaceut Anal Shijiazhuang 050017 Hebei Peoples R China;

    Hebei Med Univ Sch Pharm Dept Pharmaceut Anal Shijiazhuang 050017 Hebei Peoples R China;

    Hebei Med Univ Hosp 2 Shijiazhuang 050000 Hebei Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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