Objective To investigate the level of mycophenolate acid ( MPA) exposure in renal allograft recipients receiving mycophenolate mofetil ( MMF) as maintenance immunosuppressive therapy. Methods Sixty renal allograft recipients were treated with cyclosporine A (CsA), MMF and prednisone (Pred), peripheral vein blood samples were obtained 0. 5 h, 2 h and 4 h after administration of MMF, the plasma concentrations of MPA were measured by enzyme-multiplied immunoassay technique. The values of area under the curve ( AUC) of plasma MPA concentration ( MPA AUC) of the renal allograft recipients were calculated by the simplified formula of limited sampling strategy. All recipients were divided into low dose MMF group ( MMF < 1.5 g/d, n = 18), recommendation dose group ( MMF = 1.5 g/d, n = 29) and high dose MMF group ( MMF > 1.5 g/d, n = 13) according to doses of oral administration of MMF. Besides, all recipients were divided into low exposure to MPA group (MPA AUC <30 mg·h·'L-1), target exposure to MPA group ( MPA AUC = 30 -60 mg-h-L-1) and high exposure to MPA group (MPA AUC > 60 mg·h·L-1) according to values of MPA AUC. Results The mean MPA AUC of 60 renal transplant recipients was (59. 83 ± 19.42) mg·h·L-1. There were 3 cases (5.0%) in low exposure to MPA group, 31 cases (51.7%) in target exposure to MPA group and 26 cases (43. 3%) in high exposure to MPA group. The mean doses of CsA in low exposure to MPA group, target exposure to MPA group and high exposure to MPA group were (166.67 ±14.43) mg/d, (137. 10 ±41.27) mg/d and (128. 85 ±37. 88) mg/d respectively, exhibiting a decreasing tendency, while there was no significant difference among groups (P >0. 05). Conclusion Under the condition of MMF dose adjustment based on clinical events without MPA AUC monitoring, MPA tends to be highly exposed in renal allograft recipients. There are significant inter-individual variations in MPA pharmacokinetics, and it is necessary to perform MMF monitoring in treatment for renal allograft recipients.%目的 观察服用霉酚酸酯(MMF)的肾移植受者在免疫抑制维持治疗期霉酚酸(MPA)的暴露水平.方法 60例肾移植受者均采用环孢素A(CsA)、MMF和强的松(Pred)三联免疫抑制方案,于服用MMF后0.5、2、4h采集外周静脉血,通过酶增强免疫分析技术测定血浆MPA浓度,以有限采样法的简化公式计算肾移植受者MPA血药浓度—时间曲线下面积(AUC).根据口服MMF剂量,将患者分为3组:MMF低剂量组(MMF＜1.5 g/d,n=18)、MMF推荐剂量组(MMF=1.5 g/d,n =29)、MMF高剂量组(MMF＞1.5 g/d,n=13).根据MPA AUC值,将患者分为MPA低暴露组(MPA AUC＜30 mg·h·L-1).MPA目标暴露组(MPAAUC =30～60 mg·h·L-1)、MPA高暴露组(MPA AUC＞60 mg.h·L-1).结果 60例肾移植受者MPA AUC平均值为(59.83±19.42)mg·h·L-1；其中,MPA低暴露组3例(5.0％),MPA目标暴露组31例(51.7％),MPA高暴露组26例(43.3％)；三组CsA平均用量分别为(166.67±14.43) mg/d、( 137.10 ±41.27) mg/d和(128.85±37.88) mg/d,呈递减趋势,但组间差异无统计学意义(P＞0.05).结论 在未监测MPA AUC水平而仅根据临床事件调整MMF用量的情况下,肾移植受者平均MPA暴露水平偏高；MPA药代动力学在不同个体间存在较大的差异,进行MMF的治疗药物监测可能是必要的.
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