麦考酚酸酯在中国健康受试者体内的药动学

Pharmacokinetics of Mycophenolate Mofetil in Chinese Healthy Volunteers

目的研究麦考酚酸酯在中国健康人体内的药动学。方法12名健康受试者口服麦考酚酸酯1．0g后，用HPLC法测定血浆中麦考酚酸浓度；用3P97药动学程序拟合计算药动学参数。结果口服麦考酚酸酯后麦考酚酸的药-时曲线符合一级吸收二室模型，药动学参数Tmax为（0．75±0．18）h，Cmax为（30．81±10．75）mg·L^-1，t1／2β为（16．3±11．7）h，AUC0-12h和AUC0-∞分别为（41．16±10．45）、（69．42±20．62）mg·h·L^-1。结论麦考酚酸个体间药动学差异大，与国外文献报道基本一致。

Aim To study the pharmacokinetics of mycophenolate mofetil in Chinese healthy volunteers. Methods After oral administration of mycophenolate mofetil, the plasma concentrations of mycophenolic acid were measured by high performance liquid chromatography （HPLC）. The pharmacokinetic parameters of mycophenolic acid were estimated by 3P97 program. Results The plasma concentration-time profiles conformed to two compartment models with a first order absorption. The T max was （ 0.75 ± 0. 18 ） h, C max （ 30. 81 ±10. 75 ） mg·L^-1, t 1/2β （ 16.3 ± 11.7 ） h, AUC0 - 12h （41. 16±10.45 ） mg·h ·L^-1, AUC0-∞ （ 69.42± 20.62 ） mg·h ·L^ -1, respectively. Conclusion The pharmacokinetics of mycophenolate mofetil was highly variable between individuals in Chinese healthy volunteers, which basically conforms to literature overseas.