目的:建立替加氟静脉输注后血浆中活性代谢物5-FU浓度的HPLC-UV检测方法.方法:5名肿瘤病人静脉滴注替加氟4h后采集静脉血.以阿昔洛韦为内标,采用硝酸银沉淀蛋白,上清液吹干后用流动相复溶.采用Kromasil 100-5 C18柱(4.6 mm×250 mm)色谱柱,检测波长265 nm,柱温45℃,流速1.0 mL·min-1,流动相为三乙胺(0.5％,冰醋酸调pH至6.98)-甲醇(97∶3,V/V).结果:在线性范围62.5～750 ng·mL-1内低、中、高浓度5-FU的回收率分别为:88.3％、82.4％和91.6％；低、中、高浓度的批内RSD分别为:1.6％、1.8％和3.2％；批间样品RSD分别为:13.8％、13.8％和5.7％.最低检测限为31.25 ng·mL-1.结论:方法灵敏度高、稳定性好、特异性强、干扰少,可以为5-FU药代动力学和生物等效性研究提供方法.%Objective: To establish an HPLC-UV method for the determination of 5-FU in human plasma after intravenous infusion of tegafur. Methods: The blood samples were collected after intravenous infusion of tegafur for 4 h in 5 patients with cancer. Plasma samples were precipitated by silver nitrate after addition of the internal standard (acyclovir). After centrifugation, the supernatants were dried and redissolved with the mobile phase. The detection wavelength was 265 nm, the mobile phase consisted of triethylamine (0.5%, pH 6.98)-methanol (97:3, V/V). Results: The linear range was 62.5-750 ng·ml-1, the LLOQ was 31.25 ng·mL-1. For the low, medium and high concentrations of 5-FU, respectively, the recoveries were 88.3%, 82.4% and 91.6%, respectively; the intra-batch RSD were 1.6%, 1.8% and 3.2%, and the inter-batch RSD were 13.8%,13.8% and 5.7%. Conclusion: The method is sensitive and accurate, which can provide a new method for the studies of pharmacokinetics and bioequivalence of 5-FU.
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