吗替麦考酚酯分散片的相对生物利用度及生物等效性

Study on pharmacokinetics and bioavailability of mycophenolate mofetil dispersible tablets

目的:研究吗替麦考酚酯分散片和吗替麦考酚酯胶囊在健康志愿者中的药动学及生物等效性。方法:根据交叉试验方案口服单剂量(1 000mg)两种吗替麦考酚酯制剂,采用高效液相色谱法测定血浆中霉酚酸的浓度。结果:吗替麦考酚酯分散片和吗替麦考酚酯胶囊(对照药)的tmax分别为(0.51±0.29)h和(0.54±0.26)h;Cmax分别为(53.6±22.2)mg.L-1和(52.4±18.3)mg.L-1;AUC0→48分别为(133.7±43.6)mg.h.L-1和(142.8±46.2)mg.h.L-1;分散片相对于胶囊的生物利用度为(96.1±19.7)%。经配对检验,结果表明,两种制剂的主要药动学参数Cmax、AUC0→48的差异无显著性(P>0.05)。结论:吗替麦考酚酯分散片和吗替麦考酚酯胶囊为生物等效制剂。

OBJECTIVE To study the pharmacokinetics and relative bioavailability mycophenolate mofetil dispesible tablets. METHODS Healthy volunteers were orally given 1 000 mg of two different preparations of mycophenolate mofetil in an open randomized cross-over test. The mycophenolate mofetil concentration in plasma was determined by HPLC method, RESULTS The peak time （tmax） of mycophenolate mofetil dispesible tablets and mycophenolate mofetil capsules were （0. 51 ± 0. 29）h and （0. 54 ±0. 26） h, the pesk plassmal levels （Cmax ） were （53. 6 ±22. 2） mg · L^- 1 and （52. 4 ±18. 3） mg · L^- 1, and AUG0→48 were （ 133. 7 ±43. 6 ） mg ·h ·L^- -1和 （ 142. 8 ± 46. 2） mg· h · L^- 1. The relative bioavailability of mycophenolate mofetil dispesible tableis to mycophenolate mofetil capsules was （96. 1 ±19. 7）%. There were no significant differences in parameters Cmax AUG0→48 between two products （P〉0.05）. CONCLUSION Mycophenolate mofetil dispesible tablets and mycophenolate mofetil capsules are bioequivalent.