【摘要】 目的建立测定人血浆中克拉霉素的LC-MS/MS法,研究市售克拉霉素胶囊在人体的药动学特点。方法以罗红霉素为内标,取血浆样品0.3 mL经蛋白沉淀后,以甲醇-水(1%甲酸溶液)-乙腈=(80∶10∶10)为流动相,用C18柱分离,采用电喷雾离子源,正离子方式检测,扫描方式为多反应检测(MRM)。结果克拉霉素线性范围为10~2 500μg.L-1,日内、日间RSD均<3.5%。应用此法研究18名健康受试者单剂量口服250 mg克拉霉素市售胶囊的药动学参数tmax、ρmax、t12、AUC0→t和AUC0→∞,其值分别为(1.95±0.71)h(、949±399)μg.L-1、(4.79±0.84)h(、5 600±1 753)μg.h.L-1(、5 766±1 776)μg.h.L-1。结论该法用于人体药动学的研究具有专属、快速、灵敏等特点。更多还原

【Abstract】 AIM To develop a LC-MS/MS method to determine clarithromycin in human plasma.METHODS The tested drug and internal standard clarithromycin were extracted from plasma samples and chromatographed on a C18 column.The mobile phase consisted of methanol-water(1%formic acid)-acetonitrile(80∶10∶10,V/V/V).Detection was performed on a triple quadrupole tandem mass spectrometer via electrospray ionization source in the positive mode.RESULTS The linear calibration curves were obtained in the concentration range of 10-2 500 μg·L-1.The intra-and inter-run precisions were lower than 3.5% in terms of relative standard deviation.tmax,ρmax,t12,AUC0→t and AUC0→∞ values were found to be(1.95±0.71) h,(949±399) μg·L-1,(4.79±0.84) h,(5 600±1 753) μg·h·L-1,(5 766±1 776) μg·h·L-1,respectively after a single oral dose of 250 mg clarithromycin capsule to 18 volunteers.CONCLUSION This method is successful in the evaluation of pharmacokinetic profiles of clarithromycin capsule in huaman plasma.更多还原