国产与进口马来酸氟伏沙明片的人体生物等效性研究

目的:研究国产马来酸氟伏沙明片在人体的相对生物利用度,并与进口片比较,评价二者生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服国产马来酸氟伏沙明片(受试制剂)或进口片(参比制剂)100mg后,采用高效液相色谱法测定血药浓度,用3p97软件计算两者的药动学参数,并评价其生物等效性。结果:受试制剂与参比制剂的药-时曲线符合口服吸收一室模型。药动学参数分别为t1/2K(e14.22±9.52)、(12.06±8.94)h,tma(x4.80±2.21)、(4.90±2.45)h,Cma(x31.75±15.84)、(33.60±19.40)ng.mL-1,AUC0～9(6456.12±382.86)、(451.60±379.01)ng.h.mL-1,AUC0～∞(557.69±443.32)、(545.12±429.64)ng.h.mL-1。受试制剂相对于参比制剂的生物利用度为(101.00±14.24)%,经方差分析、双单侧t检验及1-2α置信区间法统计分析,各药动学参数差异无统计学意义(P>0.05)。结论:国产马来酸氟伏沙明片与进口片具有生物等效性。

Study on the Bioequivalence of Domestic and Imported Fluvoxamin Maleate Tablets in Healthy Volunteers

OBJECTIVE：To study the relative bioavailability of domestic fluvoxamin maleate tablets in healthy volunteers, and to evaluate the bioequivalence of domestic and imported Fluvoxamin maleate tablets. METHODS： A randomized crossover design was performed in 20 healthy male volunteers. A single oral dose of domestic tablets 100 mg （test tablets） or imported tablets 100 mg （reference tablets） were given to volunteers. Plasma concentrations of fluvoxamin maleate were measured by HPLC. The pharmacokinetic parameters were measured by 3p97 software as well as bioequivalence. RESULTS： The plasma concentration-time curves of test tablets and reference tablets conformed to one-compartment model. Main pharmacokinetic parameters of test tablets vs. reference tablets were as follows： t1/2Ke（14.22±9.52） h vs. （12.06±8.94） h; tmax（4.80±2.21） h vs. （4.90±2.45） h;Cmax（31.75±15.84） ng·mL-1 vs. （33.60±19.40） ng·mL-1; AUC0～96（456.12±382.86） ng·h·mL-1 vs. （451.60±379.01） ng·h·mL-1; AUC0～∞（557.69±443.32） ng·h·mL-1 vs. （545.12±429.64） ng·h·mL-1. The relative bioavailability of test tablets was（101.00±14.24）%. There was no significant difference between the two formulations in pharmacokinetic parameters by variance analysis,t test and 1-2α confidence interval method （P0.05）. CONCLUSION： Domestic and imported fluvoxamin maleate tablets are bioequivalent.