吗替麦考酚酯分散片人体药动学和生物等效性研究

 目的研究吗替麦考酚酯分散片在健康人体的药动学和相对生物利用度并求证其生物等效性。方法男性健康志愿者20名,随机交叉单剂量口服吗替麦考酚酯受试分散片和参比胶囊各1.0g,采用反相高效液相色谱法测定血浆中其活性代谢物霉酚酸浓度。应用DAS软件计算药动学参数和相对生物利用度,评价其生物等效性。结果口服受试和参比制剂后的主要药动学参数:t_1/2分别为(16.26±3.79)和(16.85±3.97)h;t_max分别为(0.67±0.22)和(0.78±0.29)h;ρ_max分别为(24.07±7.04)和(25.58±9.02)mg·L^-1;AUC_0-48分别为(56.84±12.81)和(59.06±15.96)mg·h·L^-1;AUC_0-∞分别为(62.25±12.63)和(64.58±15.28)mg·h·L^-1。受试制剂与参比制剂比较的相对生物利用度F_0-48为(97.95±13.73)%。结论两制剂具有生物等效性。

Pharmacokinetics and Bioequivalence of Mycophenolate Mofetil Dispersible Tablets in Healthy Volunteers

OBJECTIVE To study the pharmacokinetics and relative bioavailability of mycophenolate mofetil(MMF) dispersible tablets in healthy volunteers and to evaluate the bioequivalence.METHODS A single oral dose of 1.0 g MMF test dispersible tablets and reference capsules was given to 20 male healthy volunteers in a randomized,two-way crossover study.Mycophenolic acid(MPA),the active constitute of MMF was determined by RP-HPLC method.The pharmacokinetic parameters and relative bioavailability were calculated with DAS software to evaluate the bioequivalence of the two preparations.RESULTS The main pharmacokinetic parameters of test and reference preparations were as follows:t_1/2 were(16.26±3.79) and(16.85±3.97)h;t_max were(0.67±0.22) and(0.78±0.29)h;ρ_max were(24.07±7.04)and(25.58±9.02)mg·L^-1;AUC_0-48 were(56.84±12.81)and(59.06±15.96)mg·h·L^-1;AUC_0-∞ were(62.25±12.63)and(64.58±15.28)mg·h·L^-1,respectively.The differences of the major pharmacokinetic parameters between test and reference tablets were not significant.The relative bioavailability of F_0-48 was(97.95±13.73)%.CONCLUSION The statistical analysis of the results show that the two preparations are bioequivalent.