HPLC—MS／MS测定人血浆中文拉法辛的浓度及人体生物等效性

目的研究2种盐酸文拉法辛胶囊的人体生物等效性。方法 24名男性健康志愿者采用随机双交叉试验方案设计,分别口服受试制剂或参比制剂（博乐欣）50 mg,采集36 h内动态血标本;HPLC-MS/MS法测定血浆中文拉法辛的浓度,DAS程序对试验数据进行处理,计算药动学参数和相对生物利用度,判定2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Cm ax分别为（59.32±17.21）、（60.58±17.42）μg·L^-1,Tm ax分别为（2.08±0.46）、（2.25±0.55）h,T1/2分别为（6.69±1.67）、（6.35±1.69）h,AUC0-36分别为（524.65±227.01）、（528.22±226.57）μg·L^-1.h,AUC0-∞分别为（544.81±246.05）、（546.85±244.62）μg·L^-1.h,2种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2种制剂生物等效,受试制剂的人体相对生物利用度为（100.37±10.41）%。结论 2种盐酸文拉法辛胶囊生物等效。

Determination of venlafaxine in human plasma and bioequivalence with HPLC-MS/MS

Objective To investigate the bioequivalence of venlafaxine hydrochloride capsules in Chinese healthy volunteers.Methods 50 mg test preparation and reference preparation were given to 24 male healthy volunteers in randomized two-way crossover design and blood samples in 36 h were collected.HPLC-MS/MS was used to determine plasma concentrations of venlafaxine.The pharmacokinetics and relative bioavailability were calculated by DAS to evaluate bioequivalence.Results The main pharmacokinetic parameters of the two preparation were as follows： Cmax were（59.32±17.21） and（60.58±17.42） μg·L^-1,Tmax were（2.08±0.46） and（2.25±0.55） h,T1/2 were（6.69±1.67） and（6.35±1.69） h,AUC0-36 were（524.65±227.01） and（528.22±226.57） μg·L^-1·h,AUC0-∞were（544.81±246.05） and（546.85±244.62） μg·L^-1·h,respectively.The mean relative bioavailability of test preparation and reference preparation were（100.37±10.41）%.Conclusion The statistical analysis shows the two preparations are bioequivalent.