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目的：建立一新的高压液相色谱法用来研究氟他胺（Ｆｌｕ）及其活性代谢产物２羟基氟他胺（ＨＦ）的药物动力学．方法：正常及肝损伤大鼠灌胃Ｆｌｕ５０ｍｇ·ｋｇ－１．采用反相高压液相色谱法，以甲基睾丸素为内标，流动相为甲醇∶乙腈∶水∶乙醚＝４０∶２０∶３５∶１（体积比），检测波长为２３４ｎｍ．结果：Ｆｌｕ的Ｋ与Ｃｌ分别由０６２±０１６ｈ－１及６０±１０Ｌ·ｋｇ－１·ｈ－１减小到０１６±００３ｈ－１及０６３±０２９Ｌ·ｋｇ－１·ｈ－１（Ｐ＜００１），ＡＵＣ与Ｃｍａｘ分别由８６±１３ｍｇ·Ｌ－１·ｈ及２４±０７ｍｇ·Ｌ－１增加到１００±４４ｍｇ·ｋｇ－１·ｈ及６７±２８ｍｇ·Ｌ－１（Ｐ＜００１）．ＨＦ的Ｋ（ｍ）由００７±００１ｈ－１减小到００５±００１ｈ－１（Ｐ＜００１）．结论：在肝损伤大鼠，Ｆｌｕ与ＨＦ消除受到显著抑制．
OBJECTIVE: To establish a new high-pressure liquid chromatography (HPLC) method to study the pharmacokinetics of flutamide and its active metabolite 2-hydroxyflutamide (HF). Methods: Normal and hepatic injury rats were given Flu50mg · kg-1. Reversed-phase high pressure liquid chromatography with methyltestosterone as internal standard, mobile phase methanol: acetonitrile: water: ether = 40:20:35:1 (volume ratio), detection wavelength of 234nm. Results: K and Cl of Flu decreased from 062 ± 016h-1 and 60 ± 10L · kg-1 · h-1 to 016 ± 003h-1 and 063, respectively ± 0.29L · kg-1 · h-1 (P <001), and the AUC and Cmax were respectively 86 ± 13 mg · L-1 · h and 24 ± 07 mg · L-1 Increased to 100 ± 44 mg · kg-1 · h and 67 ± 28 mg · L-1 (P <001). The K (m) of HF decreased from 00 ± 001h-1 to 005 ± 001h-1 (P <001). Conclusion: In rats with liver injury, the elimination of Flu and HF was significantly inhibited.