目的建立高效液相色谱测定人血浆中利奈唑胺(唑烷酮类抗菌药)浓度的方法。方法用Zorbax SB-C18色谱柱,内标为头孢拉宗,流动相为乙腈-水(含0.1%甲酸)(20∶80,v/v),流速为1.0 mL.min-1。结果利奈唑胺的线性范围为0.2～25.0μg.mL-1,定量下限为0.2μg.mL-1,日内、日间精密度均≤3.8%,提取回收率为82.2%～101.4%。结论本方法灵敏、准确、快速,可用于人血浆中利奈唑胺浓度的测定和药代动力学研究。 Objective To establish a method for the determination of linezolid (human oxazolidinone antibacterials) in human plasma by high performance liquid chromatography. Methods A Zorbax SB-C18 column was used with cefradizime as internal standard. The mobile phase was acetonitrile-water (containing 0.1% formic acid) (20:80, v / v) and the flow rate was 1.0 mL.min-1. The linear range of linezolid was 0.2 ~ 25.0μg.mL-1, the lower limit of quantification was 0.2μg.mL-1. The intra-day and inter-day precision were both ≤3.8% and the extraction recoveries were 82.2% -101.4%. Conclusion The method is sensitive, accurate and rapid and can be used for the determination of linezolid in human plasma and pharmacokinetic study.