【摘要】 目的:评价麦考酚酸酯(MMF)分散片与其胶囊(商品名:骁悉)的生物等效性。方法:20名健康志愿者按随机双周期交叉试验方案设计,单剂量口服MMF分散片或其胶囊各500mg,采用RP-HPLC荧光检测法测定MMF的活性代谢产物麦考酚酸(MPA)的血药浓度。用非房室模型计算MPA药动学参数,用方差分析和双单侧t检验评价两者之间的生物等效性。结果:MMF分散片与其胶囊的主要药动学参数AUC0-48分别为(32.7±6.6)与(30.6±9.9)mg.L-1.h,AUC0-∞分别为(35.8±7.4)与(33.3±10.2)mg.L-1.h,Cmax分别为(17.0±4.5)与(15.8±4.8)mg.L-1,tmax分别为(0.45±0.29)与(0.6±0.3)h,t1/2β分别为(13.4±4.7)与(12.7±4.4)h。MMF分散片相对于其胶囊的生物利用度F为(111.6±24.0)%,经统计学检验,两者差异无显著性(P>0.05)。结论:MMF分散片与其胶囊具有生物等效性。更多还原

【Abstract】 OBJECTIVE To evaluate the bioequivalence of mycophenolate mofetil（MMF） dispersible tablets and capsules （Cellcept）.METHODS In a randomized two period crossover study,20 healthy volunteers received a single oral dose of 500 mg MMF dispersible tablet and capsule.The plasma concentrations of mycophenolic acid（MPA）,which is the active metabolite of MMF,were determined by RP-HPLC with fluorescence detection.The pharmacokinetic parameters of MPA and relative bioavailability were estimated by the non-compartment model with a statistic analysis of ANOVA and two one-sided t test.RESULTS The pharmacokinetic parameters of MMF dispersible tablet and capsules were as following: AUC₀-48（32.7±6.6） and（30.6±9.9）mg·L^-1·h,AUC₀-∞（35.8±7.4）and（33.3±10.2）mg·L^-1·h,C_max（17.0±4.5）and（15.8±4.8） mg·L^-1,t_max（0.45±0.29）and（0.6±0.3）h,t₁/2β（13.4±4.7）and（12.7±4.4）h,respectively.Compared with the MMF capsules,the relative bioavailability of MMF dispersible tablet was（111.6±24.0）% and there was no significantly statistic difference（P>0.05）.CONCLUSION The MMF dispersible tablets and capsules are bioequivalent.更多还原