本文综述儿童灌流高剂量和口服甲氨蝶呤(MTX)的临床药代动力学。儿童肿瘤患者灌流MTX 后48h 的血浆MTX 浓度不受药物剂量影响;但灌流后6h,灌流结束时血浆MTX浓度与剂量有关。高剂量MTX 的血浆清除呈双相或三相。儿童的α相T_(1/2)为2.45±0.33h,β相T_(1/2)为8.45±3.39h;均龄为8岁的儿童γ相T_(1/2)为35.67±33.62h。MTX 的代谢产物7-羟基-MTX 的血浆浓度与MTX 呈 This article reviews the clinical pharmacokinetics of high-dose and oral methotrexate (MTX) in children. The plasma MTX concentration at 48h after perfusion of MTX in pediatric cancer patients was unaffected by the dose of the drug; however, the concentration of MTX at the end of perfusion was dose-dependent at 6h after perfusion. Plasma clearance of high-dose MTX was biphasic or three-phase. The T_ (1/2) of a phase of children was 2.45 ± 0.33h and the T_ (1/2) of β phase was 8.45 ± 3.39h. The γ_phase T_ (1/2) of children aged 8 years old was 35.67 ± 33.62h . MTX metabolites 7-hydroxy-MTX plasma concentrations and MTX was