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目的:建立灵敏、快速、准确的人尿液中西他沙星浓度的HPLC-MS/MS检测方法,并将其用于测定健康受试者口服西他沙星颗粒剂后的尿药排泄。方法:尿液经甲醇处理后,取上清液进行HPLC-MS/MS法分析。10例受试者,每例空腹和餐后(随机交叉)单次口服西他沙星颗粒剂50 mg,经5天的清洗期后将两式受试者对调,两周期分别收集给药前(0 h)及给药后0~3、3~6、6~12、12~24、24~36、36~48、48~60 h各时间段的所有尿液并分析,计算西他沙星在尿液中的累计排泄量和累积排泄率。结果:西他沙星尿液的线性范围为0.250~200μg·m L-1,定量限为0.250μg·m L-1。健康受试者口服西他沙星颗粒剂后3 h即能检测到原型药物,36小时内经尿液排泄基本完全,累积排泄量约为35 mg,累积排泄率约为70%。结论:所建立的方法简便、可靠,可用于人口服西他沙星颗粒剂后药物尿液浓度的测定及其尿药排泄研究。
OBJECTIVE: To establish a sensitive, rapid and accurate HPLC-MS / MS method for the determination of citalofloxacin in human urine and to determine its urinary excretion after oral administration of citalotaxine granules in healthy subjects. Methods: After the urine was treated with methanol, the supernatant was taken for HPLC-MS / MS analysis. Ten subjects were given a single 50 mg oral dose of sitaxatine for fasting and postprandial (randomized crossover). Two subjects were matched after a 5-day washout period, (0 h) and 0 ~ 3, 3 ~ 6, 6 ~ 12, 12 ~ 24, 24 ~ 36, 36 ~ 48 and 48 ~ 60 h after administration, The cumulative excretion and cumulative excretion rate of star in urine. Results: The linear range of sitatacin urine was 0.250 ~ 200μg · m L-1, and the limit of quantification was 0.250μg · m L-1. In healthy subjects, the prototype drug was detected 3 h after oral administration of Xishaxacin Granules. Urine excretion was almost complete within 36 hours. The cumulative excretion was about 35 mg, and the cumulative excretion rate was about 70%. Conclusion: The established method is simple and reliable, which can be used to determine the urinary excretion of drug and the excretion of urinary excretion after oral administration of Xishaxacin Granules.