麦考酚酸酯分散片在健康志愿者体内的生物等效性评价  

Assessment of bioavailability of mycophenolate mofetil dispersible tablets in healthy volunteers

作　　者：仲珑瑾[1] 焦正[1] 沈杰[1] 李中东[1] 施孝金[1] 钟明康[1] 

机构地区：[1]复旦大学附属华山医院临床药学研究室,上海200040

出　　处：《中国医院药学杂志》2006年第1期34-37,共4页Chinese Journal of Hospital Pharmacy

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。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,AUC0-48 （35.8 ±7.4）and （33.3 ±10.2）mg·L^-1 ·h,Cmax （17.0 ±4.5）and （15.8 ±4.8） mg·L^-1 ,tmax（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 significandy statistic difference （P 〉0.05）. CONCLUSION The MMF dispersible tablets and capsules are bioequivalent.

关 键 词：酚酸酯 麦考酚酸 药动学 生物等效性 高效液相色谱法 

分 类 号：R969[医药卫生—药理学]