Budde Klemens, Tedesco-Silva Helio, Pestana Jose Medina, Glander Petra, Neumayer Hans-H, Felipe Claudia Rosso, Machado Paula Pinheiro, Sechaud Romain, Schmouder Robert
Department of Nephrology, University Hospital Charité, Berlin, Germany.
Ther Drug Monit. 2007 Jun;29(3):381-4. doi: 10.1097/FTD.0b013e318068619d.
The delayed release of mycophenolic acid (MPA) from enteric-coated mycophenolate sodium (EC-MPS) may lead to different MPA predose (C0) levels compared with mycophenolate mofetil (MMF). A post hoc analysis was performed on MPA morning predose values assessed in 88 maintenance renal transplant patients from three studies converted from MMF (1000 mg twice a day) to equimolar EC-MPS (720 mg twice a day) or vice versa, both in combination with cyclosporine. The median MPA predose level was approximately 30% higher when patients received EC-MPS (2.40 microg/mL; range, 0.49-39.30 microg/mL) compared with MMF (1.83 microg/mL; range, <0.1-12.80 microg/mL). Rare cases (3.0%) of high MPA C0 levels 15 microg/mL or greater were observed with EC-MPS consistent with a very prolonged release of MPA from this formulation. Both EC-MPS and MMF exhibited a poor correlation between MPA C0 levels and exposure as assessed by MPA area under the curve. Physicians targeting a certain MPA predose level have to be aware of the higher morning C0 levels with EC-MPS, whereas the overall MPA exposure is not different to MMF.
与霉酚酸酯（MMF）相比，肠溶衣霉酚酸钠（EC-MPS）中霉酚酸（MPA）的延迟释放可能导致不同的MPA给药前（C0）水平。对三项研究中88例维持性肾移植患者的MPA晨起给药前值进行了事后分析，这些患者从MMF（每日两次，每次1000 mg）转换为等摩尔的EC-MPS（每日两次，每次720 mg），或反之亦然，两者均与环孢素联合使用。与MMF（1.83μg/mL；范围，<0.1-12.80μg/mL）相比，患者接受EC-MPS时（2.40μg/mL；范围，0.49-39.30μg/mL），MPA给药前水平中位数高约30%。观察到罕见病例（3.0%）的MPA C0水平≥15μg/mL，这与该制剂中MPA的非常缓慢释放一致。通过MPA曲线下面积评估，EC-MPS和MMF的MPA C0水平与暴露之间均显示出较差的相关性。针对特定MPA给药前水平的医生必须意识到EC-MPS晨起C0水平较高，而MPA的总体暴露与MMF并无差异。
