目的 建立一快速、简便的血清伊曲康唑(ITZ)药物浓度的反相高效液相色谱测定方法。方法 200 μl血清，用叔丁基甲醚一步提取后氮气吹干，复溶后直接进样分析。流动相为甲醇-0.5%醋酸铵-乙醚(365∶110∶25)；流速0.8 ml·min〈sup〉-1〈/sup〉；检测波长261 nm；Supelcosil LC〈sub〉18〈/sub〉色谱柱，柱温40℃；室温操作。结果 ITZ与内标在血清中分离良好，t〈sub〉R〈/sub〉分别为8.3和10 min；10～500 ng·ml〈sup〉-1〈/sup〉浓度范围线性良好(r=0.9997,n=5)，富集进样方法可检出浓度达2 ng·ml〈sup〉-1〈/sup〉；样品操作20 min内可完成。结论 本方法取样量小，操作快速简便，灵敏度高；适用于治疗药物监测和临床药物动力学和药效学研究。

OBJECTIVE A RP-HPLC assay was developed for the determination of itraconazole (ITZ) in human seurm. METHODS Suitable single-step extraction proceduers by using 1.0 ml tert-Butyl methyl ether were described with only 200 μl of seurm.The mobile phase was consisted of methyl alcohol-0.5% ammonium acetate-ether (365∶110∶25) with the detection wavelength at 261 nm.The column Supelcolsil LC₁₈(25 cm×4.6 mm,5 μm) was selected. RESULTS The assay allowed excellent linearity (r=0.9997) over the range of 10 to 500 ng·ml^-1,and the limit of sensitivity was 2 ng·ml^-1(50 μl inj.).The coefficients of variation for 25,150 and 400 ng·ml^-1 check asmples were 1.69% to 2.91% for inter-run (n=6),and 1.78% to 3.09% for intra-run (n=10),respectively.The average recovery for them were 95% to 104% (n=16). CONCLUSION The assay was successfully applied to the analysis of serum samples after oral administration of 200 mg ITZ in a PK/PD study.