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15mmol/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/z502.1→466.2(非索非那定),m/z491.2→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、120mg)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(2386.3±867.5)ng·h·ml-1;多剂量口服非索伪麻缓释胶囊(60mg,bid)后非索非那定的主要药动学参数为:cmin(35.45±21.56)ng/ml,cav(97.88±57.12)ng/ml,DF(1.78±0.32),AUCss(1196.26±665.06)ng·h·ml-1。
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 of fexofenadine/pseudoephedrine sustained-release capsules in 20 healthy volunteers was investigated.For single dosage(60 and 120 mg fexofenadine),the main pharmacokinetic parameters of fexofenadine were as follows:t1/2β(11.34±4.59) and(11.09±3.27) h,tmax(4.20±0.98) and(3.72±1.21) h,cmax(159.28±76.81) and(368.89±165.21) ng·ml-1,AUC0-48h(997.87±421.12) and(2 386.3± 867.5) ng·h·ml-1.For multiple dosage(60 mg fexofenadine,bid),the main pharmacokinetic parameters of fexofenadine were as follows:cmin(35.45±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-1.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2010年第10期759-763,782,共6页
Chinese Journal of Pharmaceuticals