吗替麦考酚酯软胶囊的药动学及生物等效性研究

目的:研究吗替麦考酚酯软胶囊与吗替麦考酚酯胶囊在健康人体内的相对生物利用度及药动学,评价2种制剂的生物等效性。方法:采用双周期随机交叉设计,20名男性健康志愿者单剂量口服试验软胶囊或参比胶囊4粒(每粒0.25g),以高效液相色谱法测定血浆中霉酚酸(MPA)浓度。运用DAS2.0软件处理血药浓度数据和计算药动学参数,对2种制剂做出生物等效性评价。结果:受试者口服1.0g吗替麦考酚酯软胶囊试验药或参比胶囊,其AUC0→t分别为(69.95±14.13)、(66.95±19.05)μg·h·mL-1,AUC0→∞分别为(85.18±20.51)、(77.39±23.78)μg·h·mL-1,Cmax分别为(31.26±13.09)、(31.90±14.45)μg·mL-1,tmax分别为(0.875±0.358)、(0.775±0.291)h,t1/2分别为(20.342±12.546)、(18.837±11.579)h。20名健康志愿者单剂量口服吗替麦考酚酯软胶囊试验药的相对生物利用度为(109.6±26.9)%。结论:试验软胶囊与参比胶囊具有生物等效性。

Study on the Pharmacokinetics and Bioequivalence of Mycophenolate Mofetil Soft Capsules

OBJECTIVE：To study the relative bioavailability and pharmacokinetics of Mycophenolate mofetil capsules vs.Mycophenolate mofetil soft capsules in healthy volunteers.METHODS：In double period randomized crossover study,20 healthy volunteers were given a single oral dose of trial capsule and reference capsule 4 pills（0.25 g per pill）.The concentration of mycophenolate（MPA） was determined by HPLC.Pharmacokinetic parameters were calculated using DAs 2.0 software and the bioequivalence of 2 formulations were evaluated.RESULTS：Main pharmacokinetic parameters of trial capsule vs.reference capsule were as follows：AUC0→t：（69.95±14.13）μg·h·mL-1 vs.（66.95±19.05）μg·h·mL-1;AUC0→∞：（85.18±20.51）μg·h·mL-1 vs.（77.39±23.78） μg·h·mL-1;Cmax：（31.26±13.09）μg·mL-1 vs.（31.90±14.45）μg·mL-1;tmax：（0.875±0.358）h vs.（0.775±0.291）h.The relative bioavailability of Mycophenolate mofetil soft capsules in 20 healthy volunteers was（109.6±26.9）%.CONCLUSION：Results of study indicated the 2 formulations are bioequivalent.