中文摘要：

目的：建立测定人尿液中他唑巴坦钠浓度的方法,并进行尿药排泄动力学研究。方法：尿液样品经10%高氯酸沉淀后,采用高效液相色谱-串联质谱（LC-MS/MS）法测定尿液中他唑巴坦钠的浓度。色谱柱为Hypersil GOLD C18,流动相为甲醇-水（30∶70,V/V）,流速为0.2 ml/min,柱温为30℃,进样量为5μl;采用电喷雾离子源,以多反应监测方式进行正离子扫描,用于定量分析的离子对为m/z 301→168。入组8名健康受试者,静脉滴注注射用头孢噻肟钠他唑巴坦钠（6∶1,m/m）2.34 g,收集其给药前和给药后0-2、2-5、5-8、8-12和12-16 h的尿液研究其尿液排泄动力学。结果：他唑巴坦钠尿药浓度在0.25-500μg/ml范围内线性关系良好（r=0.999 9）,定量下限为0.25μg/ml,批内、批间RSD〈10%,方法回收率为93.8%-111.8%,提取回收率为93.9%-99.7%,介质效应为87.6%-107.2%。受试者用药16 h后,他唑巴坦钠的尿累积排泄量为（209.70±39.24）mg,累积排泄率为（61.7±11.5）%。结论：LC-MS/MS法用于人尿液中他唑巴坦钠浓度的测定和排泄动力学的研究简便、快捷、灵敏度高;他唑巴坦钠主要经肾脏排泻。

英文摘要：

OBJECTIVE： To establish a method for the concentration determination of tazobactam sodium in human urine, and to study urinary excretion pharmacokinetics. METHODS： The urine samples were extracted by 10% perchloric acid, and then deter- mined by LC-MS/MS. The separation was performed on a Hypersil GOLD C18 column with mobile phase consisted of ethanol-water （30：70, V/V） at flow rate of 0.2 ml/min; the column temperature was set at 30℃, and sample size was 5 μl. ESI was used, and positive ion scanning was conducted in MRM mode; ion pair for quantitative analysis was m/z 301→168. 8 healthy volunteers were given Cefotaxime sodium and tazobactam sodium for injection （6 ： 1, m/m） 2.34 g intravenously, and then urine samples were collected before medication, 0-2, 2-5, 5-8, 8-12 and 12-16 h after medication. RESULTS： The linear range of tazobactam sodium was 0.25-500 μg/ml （r=0.999 9）. The limit of quantitation was 0.25 μg/ml; RSDs of inter-batch and intra-batch were all lower than 10% ; method recoveries were 93.8%-111.8% ; extraction recoveries were 93.9%-99.7% ; medium effect ranged 87.6%-107.2%. 16 h after medication, accumulative excretion amount of tazobactam sodium in urine was （209.70 ± 39.24） mg and accumulative excretion rate was （61.7 ± 11.5）%. CONCLUSIONS： LC-MS/MS method can be used for the concentration determination of tazobactam sodium in human urine and excretion kinetics study. It is simple, rapid and sensitivity; tazobactam sodium mainly excrete viareral tissue.