麦考酚钠肠溶片在肾移植患者早期的药动学初步研究  

Pharmacokinetics Study of Enteric-Coated Mycophenolate Sodium in the Early Period after Renal Transplantation

作　　者：邱葵[1] 尹航[2] 于晓佳[1] 刘丽宏[1] 

机构地区：[1]首都医科大学附属北京朝阳医院药事部,北京100020 [2]首都医科大学附属北京朝阳医院泌尿外科,北京100020

出　　处：《中国药学杂志》2014年第18期1637-1641,共5页Chinese Pharmaceutical Journal

摘　　要：目的研究肾移植患者口服麦考酚钠肠溶片(EC-MPS)达稳态后其活性代谢产物霉酚酸(MPA)的药动学。方法选取同种异体活体肾移植患者12例(男8例,女4例)进行研究,所有患者均采用环孢素(CsA)+麦考酚钠肠溶片(EC-MPS)+泼尼松(Pred)的三联用药方案。用高效液相色谱法测定霉酚酸血药浓度,血药浓度数据用DAS2.0软件,按非房室模型拟合计算药动学参数,并分别用不同时间点的血药浓度与AUC0-12 h作相关性分析。结果霉酚酸稳态后的药动学参数Tmax为(5.67±3.68)h,ρmax为(11.78±6.21)mg·L-1,AUC0-12 h为(44.72±15.22)mg·h·L-1,MRT为(5.54±1.15)h,CLz/F为(0.35±0.15)L·h-1,Vz/F为(2.71±1.25)L,相关性分析显示ρ8 h相关性最好。结论霉酚酸个体间药动学差异大,建议将ρ8 h作为肾移植术后早期监测MPA的参考指标。OBJECTIVE To determine the steady state pharmacokinetics of mycophenolic acid （ MPA）, the active metabolite, after an oral administration of enteric-coated mycophenolate sodium （EC-MPS） in the renal transplant patients. METHODS This study was conducted in 12 Chinese renal transplant patients （8 men and 4 women） receiving living donor and treated with EC-MPS, cyelosporine, and corticosteroids. MPA concentrations were measured by high performance liquid chromatography （HPLC）. The DAS2.0 pharmaceutical kinetics software was used for the calculation of pharmacokinetic parameters. The correlation of each sampling time for MPA AUC were analyzed. RESULTS The mean time for it to reach peak （tmax ） , the mean maximum plasma concentration, the mean area under the curve （AUC） from 0 to 12 h, mean residence time （MRT） , and clearance （CL） were （5.67 ± 3.68） h, （11.78 ＋6.21） mg · L^-1, （44.72±15.22） mg · h · L^-1, （5.54±1.15） h, （ 0.35±0. 15） L · h^-1, respectively. Spearman＇s correlation coefficients for P0 h, P6 h, P8 h and Pl2 h were 0. 414 （ P = 0. 18 ）, 0. 716 （ P = 0. 009 ）, 0. 755 （ P = 0. 004 ） and 0. 148 （ P = 0. 646）. CONCLUSION The PKs of EC-MPS has a high variability among Chinese renal transplant recipients. The Ps h to look as a important concentration rather than P0 h were proposed.

关 键 词：麦考酚钠肠溶片 霉酚酸 肾移植患者 药动学 

分 类 号：R969.1[医药卫生—药理学]