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目的测定抗癌药物伊立替康(CPT-11)及其主要活性代谢物SN-38,SN-38G的血药浓度和药代动力学指标。方法样品先经甲醇-乙腈(50∶50体积比)沉淀蛋白,并用盐酸酸化使内酯环开环。用高效液相色谱仪定量:以喜树碱作内标;Xterra RP18柱,激发波长370nm,检测波长为470nm和534nm。结果血浆CPT-11及其活性代谢物、酸性提取物在此条件下的稳定性较好。三种待测物线性范围皆为1～1000ng/ml,检测限都是1ng/ml。相对标准差为3.1%～11.7%的血浆。测定回收率为93.2%～109.8%。中位提取回收率为91%。结论所建立的方法可用于测定CPT-11,SN38和SN38-G在人血浆中的药物浓度,可满足临床进行CPT-11人体药代动力学研究。
Objective To determine the plasma concentrations and pharmacokinetic parameters of the anticancer drug irinotecan (CPT-11) and its major active metabolites SN-38 and SN-38G. Methods Samples were first precipitated with methanol-acetonitrile (50:50 by volume) and the lactone ring was opened by acidification with hydrochloric acid. Quantitative HPLC: Camptothecin as internal standard; Xterra RP18 column, excitation wavelength 370nm, detection wavelength of 470nm and 534nm. Results Plasma CPT-11 and its active metabolites, acidic extracts under this condition, the stability is better. The linear range of the three analytes are 1 ~ 1000ng / ml, the detection limit is 1ng / ml. Relative standard deviation of 3.1% to 11.7% of the plasma. The recovery rate was 93.2% ~ 109.8%. The median extraction recovery was 91%. Conclusion The established method can be used to determine the drug concentration of CPT-11, SN38 and SN38-G in human plasma, which can meet the clinical pharmacokinetics of CPT-11.