摘要
目的:研究吗替麦考酚酯分散片在中国健康男性志愿者体内的药动学和生物等效性。方法:采用双周期交叉试验设计,20名健康男性受试者随机交叉单剂量口服吗替麦考酚酯分散片(试验制剂)和吗替麦考酚酯胶囊(参比制剂)1g,以高效液相色谱法测定给药后不同时间麦考酚酸的血药浓度,用DASVer2.0软件计算药动学参数,评价两种制剂的生物等效性。结果:吗替麦考酚酯试验制剂和参比制剂的主要药动学参数Cmax分别为(19.88±3.55)μg/ml和(20.16±3.47)μg/ml;tmax分别为(0.74±0.19)h和(0.80±0.17)h;t1/2分别为(8.86±2.73)h和(8.77±3.00)h;AUC0-t分别为(48.63±16.53)μg/(h·ml)和(49.96±18.01)μg/(h·ml),AUC0-∞分别为(54.34±16.63)μg/(h·ml)和(55.38±18.68)μg/(h·ml);试验制剂的AUC0-t、AUC0-∞、Cmax的90%置信区间分别为参比制剂相应参数的91.03%～104.53%、92.91%～105.26%和94.92%～102.17%。以AUC0-t计算试验制剂中吗替麦考酚酯对参比制剂的相对生物利用度F为(99.25±17.02)%。结论:经方差分析及双单侧t检验结果显示,试验制剂和参比制剂具有生物等效性。
Objective： To study the pharmacokinetics and bioequivalence of Mycophenolate Mofetil Dispersible Tablets in Chinese healthy male volunteers. Methods： 20 healthy male volunteers were orally administered with single dose of 1 g Mycophenolate Mofetil Dispersible Tablets （test preparation） and Mycophenolate Mofetil Capsules （reference preparation） by randomized crossover way, then the plasma concentrations of myeophenolic acid were determined by HPLC methods. The pharmacokinetic parameters and the relative bioequivalenee of the two preparations of Myeophenolate Mofetil was calculated by DAS Ver 2.0 software. Results： The main pharmacokinetic parameters of test and reference preparations were as follows： Cmax were （19.88±3.55） μg/ml and （20.16±3.47） μg/ml respectively; tmax were （0.74±0.19） h and （0.80±0.17） h respectively; t1/2 were （8.86±2.73） h and （8.77±3.00） h respectively; A UC0-t were （48.63±16.53） μg/（h ·ml） and （49.96±18.01） μg/（h ·ml） respectively; A UC0-∞ were （54.34±16.63） μg/（h ·ml） and （55.38±18.68） μg/（h ·ml） respectively. The 90% confidential interval of AUC0-t, A UC0-∞ and Cmax, of the test preparation were 91.03%-104.53%, 92.91%-105.26% and 94.92%-102.17% respectively. The relative bioavailability of Mycophenolate Mofetil was （99.25±17.02）%. Conclusion： The results of the statistic analysis of variance and two one side t test showed that the test and reference preparations of Mycophenolate Mofetil were bioequivalent.
出处
《中国医药导报》
CAS
2009年第13期24-27,共4页
China Medical Herald
