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目的 探讨口服他克莫司 (Tacrolimus ,FK5 0 6 )的药代动力学规律 ,寻求临床上准确反映早期药物浓度时间曲线下面积 (AUC)的监测方法。 方法 16例肾移植受者首剂口服 0 .0 75mg/kgFK5 0 6后 ,采用ELISA法测定服药后 0 .5、1.0、1.5、2 .0、3.0、5 .0、8.0、12 .0h时间点血药浓度 ,采用 3p87药代动力学计算程序将测得的FK5 0 6浓度自动拟合计算出AUC ,并分别将各时间点血药浓度与AUC进行相关性检验 ,计算相关系数。 结果 AUC变化范围为 4 4 .4 0～ 15 8.0 1μg·h-1·L-1,平均 ( 92 .2 3± 34.97) μg·h-1·L-1,个体间AUC可相差 4倍 ;血药谷浓度Cmin与AUC之间的相关性有显著差异 (P <0 .0 0 1,rmin=0 .6 5 0 )。 结论 首剂口服同一剂量FK5 0 6后 ,个体间药物浓度时间曲线下面积差异很大。Cmin能准确反映首剂口服FK5 0 6后的AUC ,临床上可通过监测Cmin达到FK5 0 6早期剂量的个体化
Objective To investigate the pharmacokinetics of oral administration of tacrolimus (FK506) and to find a method that can accurately reflect the area under the curve (AUC) of early drug concentration. Methods 16 cases of renal transplant recipients first oral 0 0 75mg / kgFK5 0 6, measured by ELISA after taking 0.5, 1.0, 1.5, 2.0, 3.0, 5.0, 8.0, 12.0h time Point blood concentration, using 3p87 pharmacokinetic calculation program FK5 0 6 concentration was automatically fitted to calculate the AUC, respectively, at each time point blood concentration and AUC correlation test to calculate the correlation coefficient. Results The AUC ranged from 44.0 to 15.81 μg · h-1 · L-1, with an average (92.2 ± 34.97) μg · h-1 · L-1. There was a significant difference in the correlation between plasma concentration of Cmin and AUC (P <0.01, rmin = 0.560). Conclusions After the first dose of FK5 0 6 was administered orally, the area under the curve of drug concentration between individuals differed greatly. Cmin can accurately reflect the first dose of oral FK5 0 6 AUC clinically by monitoring Cmin FK5 0 6 early dose of individualized