【摘要】 目的:研究外消旋化布芬洛辛(RBAC)缓释片在正常人体内的药动学特点,评价其与布洛芬(BAC)缓释片的生物等效性。方法:18名健康志愿者采用随机交叉、自身对照给药方案,多剂量口服RBAC或BAC,以反相高效液相色谱法测定RBAC和BAC的血药浓度,计算药动学参数,并进行方差分析和双单侧t检验。结果:RBAC与BAC的t1/2分别为(8.14±1.95)h、(8.81±2.27)h,tmax分别为(3.44±0.62)h、(3.44±0.70)h,Cssmax分别为(3.69±0.50)、(3.68±0.76)mg/L,AUC0～τ分别为(23.49±2.53)、(22.48±2.59)(mg·h)/L;DF分别为(138.21±23.10)%、(134.53±28.14)%,Css分别为(1.96±0.21)、(1.85±0.22)mg/L;RBAC相对于BAC的生物利用度为(102.45±8.07)%。结论:2种制剂具有生物等效性。更多还原

【Abstract】 OBJECTIVES:To study the pharmacokinetics of racemic benzeneacetic acid of chirality(RBAC)sustained re-lease tablet in human body of healthy volunteers,and to evaluate the bioequiavailability of RBAC and benzeneacetic acid of chirality(BAC)sustained release tablet.METHODS:18healthy volunteers studies were administered with multidoses of RBAC or BAC by randomized crossover and own control,the plasma concentrations of RBAC and BAC were determined by RP-HPLC,the pharmacokinetic parameters were calculated and ANOVA and two&one side t tests were carried out as well.RESULTS:The pharmacokinetic parameters of RBAC and BAC were respectively as follows:t 1/2 were(8.14±1.95)h and(8.81±2.27)h;t max were(3.44±0.62)h and(3.44±0.70)h;C ss max were(3.69±0.50)mg/L and(3.68±0.76)mg/L,AUC 0～t were(23.49±2.53)(mg·h)/L and(22.48±2.59)(mg·h)/L;DF were(138.21%±23.10)%and(134.53%±28.14)%;C ss were(1.96±0.21)mg/L and(1.85±0.22)mg/L;The relative bioavailability of RBAC to BAC was(102.45±8.07)%.CON-CLUSION:RBAC and BAC were bioequivalent.更多还原