【摘要】 目的建立测定人血浆中氟伏沙明浓度的方法 ,对国产和进口马来酸氟伏沙明片进行生物等效性研究。方法 24名健康男性志愿者按2×2交叉试验方案设计,分别口服受试制剂和参比制剂各50 mg,并在给药后96 h内动态采集血样,采用LC-MS/MS法测定血浆中氟伏沙明浓度,计算药动学参数,评价两种制剂的生物等效性。结果受试制剂和参比制剂的主要药动学参数ρ_max分别为（18.79±8.15）μg·L^-1和（19.04±7.49）μg·L^-1,t_max分别为（3.73±0.90）h和（3.81±1.02）h,AUC_0→96分别为（327.57±131.93）μg·h·L^-1和（349.36±159.63）μg·h·L^-1,AUC_0→∞分别为（346.95±134.84）μg.h·L^-1和（368.27±163.59）μg·h·L^-1,t_1/2分别为（14.55±3.14）h和（14.15±3.17）h,两制剂主要药动学参数经对数转换后进行方差分析及双单侧t检验,并计算90%置信区间,表明两种制剂生物等效,受试制剂相对于参比制剂的生物利用度为（97.08±16.70）%。结论本方法可用于氟伏沙明人体药动学及生物等效性研究,统计分析证实马来酸氟伏沙明国产与进口制剂生物等效。更多还原

【Abstract】 AIM To establish a LC-MS/MS method for determination of fluvoxamine concentration in human plasma and to study bioequivalence of fluvoxamine maleate tablets.METHODS Both 50 mg test and reference preparations were given to 24 male healthy volunteers in a randomized two-period crossover design for the pharmacokinetic and relative bioavailability study.Plasma fluvoxamine concentration was determined by LC-MS/MS.RESULTS The main pharmacokinetic parameters of the two preparations were as follows:ρ_max（18.79±8.15）μg·L^-1 and（19.04±7.49）μg·L^-1, t_max（3.73±0.90） h and（3.81±1.02）h,AUC_0→96h（327.57±131.93）μg·h·L^-1 and（349.36±159.63）μg·h L^-1,AUC_0→∞（346.95±134.84）μg·h·L^-1 and（368.27±163.59）μg·h·L^-1,t_1/2（14.55±3.14）h and（14.15±3.17）h,respectively.The mean relative bioavailability of test preparation vs reference preparation was（97.08±16.70）%.CONCLUSION The method can be applied to study the pharmacokinetics and bioavailability of fluvoxamine in humans,and statistical analysis confirms the two preparations are bioequivalent.更多还原