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    LC-MS/MS测定Hu7691在大鼠血浆中的含量及其药动学研究

    Content of Hu7691 in Rat Plasma determined by LC-MS/MS and Its Pharmacokinetic Study

      摘要
    • 摘要:
      目的 建立一种液相色谱-串联质谱(liquid chromatography-tandem mass spectrometry，LC-MS/MS)法快速、灵敏测定大鼠血浆中Hu7691的浓度。
      方法 大鼠血浆样本以乙腈沉淀蛋白后，选用三键键合烷基色谱柱，以0.1%甲酸水-乙腈作为流动相进行梯度洗脱，选用多重反应监测扫描方式进行监测。将经验证的方法应用于Hu7691在SD大鼠体内的药动学研究。
      结果 大鼠口服5、10和20 mg·kg−1 Hu7691以及静脉注射5 mg·kg−1的Hu7691后，大鼠血浆中Hu7691的AUC和Cmax随剂量的增大而增加，生物利用度分别为50.2%、62.0%、75.7%。
      结论 表明Hu7691在大鼠体内具有较高的胃肠吸收率和稳定的药动学特性。

       

      Abstract:
      OBJECTIVE To establish a liquid chromatography-tandem mass spectrometry(LC-MS/MS) method for the rapid and sensitive determination of Hu7691 in rat plasma.
      METHODS After the plasma samples were precipitated with acetonitrile, a triple-bonded alkyl column was used for gradient elution with 0.1% formic acid water and acetonitrile as mobile phase. Multiple reaction monitoring scanning was used for monitoring. The validated method was applied to study the pharmacokinetics of Hu7691 in rats.
      RESULTS The results showed that the AUC and Cmax of Hu7691 in plasma of SD rats increased with the increase of dose after oral administration of 5, 10 and 20 mg·kg−1 Hu7691 and intravenous injection of 5 mg·kg−1 Hu7691, and the bioavailability of Hu7691 were 50.2%, 62.0% and 75.7%.
      CONCLUSION Hu7691 has high gastrointestinal absorption rate and stable pharmacokinetic characteristics in rats.

       

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