人血浆中非索非那定的LC-MSMS法测定及药动学.pdfVIP

中国医药工业杂志 Chinese Journal of Pharmaceuticals 2010, 41(10) · 759 · 人血浆中非索非那定的 LC-MS/MS 法测定及药动学 黄凤英1，刘善军2*，凌婧怡2，刘 熙2 (1. 湖南省娄底卫校附属医院，湖南娄底 417000；2. 中国药科大学，江苏南京 210009) 摘要：建立了 LC-MS/MS 法测定人血浆中的非索非那定浓度。以格列美脲为内标，采用 C18 柱，流动相为甲醇 - 水 ( 含 15 mmol/L 乙酸铵和 0.05％甲酸 )(68 ︰ 32)，电喷雾离子化源，选择性正离子反应监测，检测离子为 m/z 502.1 → 466.2( 非索非那定 )，m/z 491.2 → 352.0( 格列美脲 )，并用于人体药动学研究。20 名健康志愿者单剂量口服非索伪麻 缓释胶囊 ( 非索非那定 60、120 mg) 后非索非那定的主要药动学参数为：t1/2β(11.34±4.59) 和 (11.09±3.27) h，tmax(4.20± 0.98) 和 (3.72±1.21) h，cmax(159.28±76.81) 和 (368.89±165.21) ng/ml，AUC0-48h(997.87±421.12) 和 (2 386.3± -1 867.5)ng?h?ml ；多剂量口服非索伪麻缓释胶囊 (60 mg，bid) 后非索非那定的主要药动学参数为：cmin(35.45± -1 21.56) ng/ml，cav(97.88±57.12) ng/ml，DF(1.78±0.32)，AUCss(1 196.26±665.06) ng?h?ml 。 关键词：非索非那定；伪麻黄碱；药动学；液相色谱-串联质谱；测定 中图分类号：R969；O657.7 文献标志码：A 文章编号：1001-8255(2010)10-0759-05 Determination of Fexofenadine in Human Plasma by LC-MS/MS and Its Pharmacokinetics HUANG Fengying1, LIU Shanjun2*, LING Jingyi2, LIU Xi2 (1. Affiliated Hospital of Loudi Health School in Hunan Province, Loudi 417000; 2. China Pharmaceutical University, Nanjing 210009) ABSTRACT: A LC-MS/MS method was established for the determination of fexofenadine in human plasma. Glimepiride was used as internal standard. A C18 column was used, with the mobile phase of methanol-water (containing 15 mmol/L ammonium acetate and 0.05% formic acid)(68︰32). ESI was applied and operated in positive ion selective reaction monitoring mode. The detected ions were m/z 502.1→466.2(fexofenadine)，m/z 491.2→352.0(glimepiride). The pharmacokinetics of single oral dose and multiple oral dose