吗替麦考酚酯分散片在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of mycophenolate mofetil dispersible tablets in healthy volunteers

目的研究国产吗替麦考酚酯(MMF)分散片(免疫抑制剂)和其进口胶囊在健康人体的生物等效性。方法用随机自身对照双周期交叉试验设计,18名男性健康志愿者口服MMF分散片或胶囊各1.0g,用高效液相色谱法测定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的药代动力学参数。结果MMF分散片与胶囊的药代动力学参数如下:tmax分别为(0.68±0.21),(0.81±0.18)h;Cmax分别为(25.58±4.79),(26.47±3.67)mg·L-1;AUC(0-48)分别为(59.19±9.23),(58.32±9.28)mg.h.L-1;t1/2分别为(15.12±3.17),(16.14±4.22)h。国产吗替麦考酚酯分散片中麦考酚酸相对于胶囊的相对生物利用度为(101.5±10.3)%。结论2制剂在人体内生物等效。

Objective To evaluate the bioequivalence of mycophenolate mofetil（ MMF ） dispersible tablets and capsules in healthy volunteers. Methods In a randomized two period crossover study, 18 healthy volunteers received a single oral dose of 1.0 g MMF dispersible tablets and capsule. The plasma concentration of mycophenolic acid （ MPA）, which is the active metabolite of MMF,were determined by HPLC. The pharmacokinetics of MPA were estimated by the non - compartment model. Results The main pharmacokinetic parameters of MMF dispersible tablets and capsules were as the following： tmax Were （0.68 ±0.21 ）, （0.81 ±0. 18） h ; Cmax were （ 25.58 ± 4.79 ）, （ 26.47 ± 3.67 ） mg·L^- 1 ; AUC（0-48） were （59.19±9.23）, （58.32 ±9.28） mg·h· L^-1; t（1/2） were（15. 12 ± 3.17）, （ 16.14 ± 4.22 ） h, respectively. The relative bioavailability was （ 101.5 ± 10.3 ） %. Conclusion The two formulations are bioequivalent in human.