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在5例儿童身上研究甲氨蝶呤(MTX)的药代动力学。5名接受MOP方案进行维持治疗的急性淋巴性白血病儿童,口服单剂(3.97—11.90mg/m~2)MTX后,采用微生物法测定MTX血浓度。 结果表明:消除半衰期(t 1/2)及达峰时间(Tp)分别为113.8±21.2min及103.6±5.9min,个体差异不大。而峰面积(Cmax)及浓度曲线下的面积(AUC)分别为0.0612—0.2960μg/ml及18.65—95.10μg.min/ml,个体差异较大,且不呈剂量依赖性。 在大鼠的实验表明长春新碱及强的松不会干扰MTX的测定,也不会影响MTX的药代动力学过程。
Methotrexate (MTX) pharmacokinetics were studied in 5 children. Five children with acute lymphoblastic leukemia treated with MOP regimen were treated with a single oral dose of MTX (3.97-11.90 mg / m ~ 2). MTX blood concentration was determined by the microbiological method. The results showed that the elimination half-life (t1 / 2) and peak time (Tp) were 113.8 ± 21.2 min and 103.6 ± 5.9 min, respectively. While the peak area (Cmax) and the area under the concentration curve (AUC) were 0.0612-0.2960μg / ml and 18.65-95.10μg.min / ml respectively, with significant individual differences and no dose-dependent. Experiments in rats showed that vincristine and prednisone did not interfere with the MTX assay and did not affect the pharmacokinetics of MTX.