RP-HPLC法测定人血浆奥氮平浓度及其在健康志愿者的药代动力学研究

目的建立测定人血浆中奥氮平浓度的高效液相色谱法并进行药代动力学研究。方法10名男性健康志愿者单剂量口服奥氮平片20mg,血浆样品经液-液提取,用高效液相色谱法检测奥氮平的浓度,并用3P97程序进行数据处理。结果此方法适用于人血浆中奥氮平浓度的检测。单剂量口服奥氮平后,其血浆药-时曲线符合二室模型;主要药代动力学参数Cmax、Tmax、t1/2、AUC0-144、AUC0-inf分别为(113.7±33.1)μg·L-1、(5.07±0.65)h、(35.44±4.21)h、(2235±257)μg·h·L-1和(2516±301)μg·h·L-1。结论该方法灵敏、准确,能快速检测人血浆中奥氮平浓度。

Reversed phase high-performance liquid chromatography for determination of plasma olanzapine and pharmacokinetics of olanzapine in healthy Chinese volunteers

OBJECTIVE: To establish a reversed phase high-performance liquid chromatography (HPLC) system for determining plasma concentration of olanzapine and analyze the pharmacokinetics of olanzapine in healthy Chinese volunteers. METHODS: Ten healthy male subjects received a single oral dose of 20 mg olanzapine tablets. The plasma concentrations of olanzapine were determined by HPLC, and the data were analyzed using 3P97 program. RESULTS: The plasma concentration curve of olanzapine following a single oral dose conformed to the two compartment open model. The main pharmacokinetics parameters of olanzapine were as follow: C(max) was 113.7-/+33.1 microg/L, T(max) 5.07-/+0.65 h, t(1/2) 35.44-/+4.21 h, AUC(0-144) 2,235-/+257 microg.h.L(-1), and AUC(0-inf) 2,516-/+301 microg.h.L(-1). CONCLUSION: The system established in this study allows for highly sensitive, selective and accurate determination of plasma concentration of olanzapine, and provides valuable information for clinical trials.