吗替麦考酚酯胶囊在健康受试者人体内相对生物利用度和生物等效性研究

目的研究吗替麦考酚酯胶囊在健康人体内的药动学和相对生物利用度，进行生物等效性评价．方法18名男性健康志愿者双周期随机交叉单次口服吗替麦考酚酯胶囊1g，服药间隔为l周，采用高效液相色谱法测定血浆中麦考酚酸浓度．结果两种制剂主要药动学参数无显著性差异，参比和受试的c～分别为37．91±10．38和37．70±7．75mg／L；tmax分别为0．52±0．38h和0．50±0．25h；t1/2分别为16．37±9．90h和13．85±8．83h；AUC0→24分别为每升62．00±10．12mg／h和每升60．10±10．21mg/h．吗替麦考酚酯胶囊的相对生物利用度为97．59±12．24％．结论2种制剂具有生物等效性．图4，表4，参5

Research on the Relative Bioavailability and Bioequivalence of Mycophenolate Mofetil Capsules in Healthy Volunteers

Objective To investigate the pharmacokinetics and relative bioavailability of mycophenolate mofetil capsules in healthy volunteers, and to evaluate its bioequivalence. Methods A single oral dose of 1 g of two kinds of mycophenolate mofetil capsules was administered by randomized crossover way in 18 male healthy vol- unteers, and the plasma concentrations of mycophenolic acid were determined by high performance liquid chromatography （HPLC）. Result The main pharmacokinetic parameters have no significant differences of be- tween two kinds of preparations. The pharmacokinetic parameters of reference preparation and tested prepara- tions were as follows ：Cmax,= （ 37.91 ± 10.38 ）, （ 37.70 ±7.75 ）mg/L; tmax（0.52 ±0.38）h , （0.50 ±0.25） h ;t1/2 （ 16.37± 9.90） h, （ 13.85 ± 8.83 ） h; AUC0→24 （62.00 ± 10.12） mg/h · L, （60.10 ± 10.21 ） mg/h · L. The relative bioavailability of the tested preparation was （97.59 ± 12.24） %. Conclusion The reference preparation and the tested preparation were bioequivalent. 4figs. , 4tabs. , 5refs.