大剂量甲氨蝶呤化疗的脑脊液药代动力学研究  

Study of pharmacokinetics in cerebrospinal fluid during high dose methotrexate chemotherapy

作　　者：赵帆[1] 赵永新[2] 肖拥军[3] 孙延亮[3] 

机构地区：[1]南京医科大学附属无锡第二医院肿瘤科,江苏无锡214002 [2]南华大学附属怀化医院药剂科,湖南怀化418000 [3]南华大学附属怀化医院肿瘤科,湖南怀化418000

出　　处：《肿瘤防治杂志》2004年第12期1247-1249,共3页China Journal of Cancer Prevention and Treatment

基　　金：湖南省卫生厅科研基金资助项目 ( 0 0 115 )

摘　　要：目的 :研究大剂量甲氨蝶呤(methotrexate ,MTX)化疗的脑脊液药代动力学。方法 :采用反相高效液相色谱法对 2 7例肿瘤患者静脉滴入MTX( 1 0～ 3 0g/次 )后的脑脊液和血浆中MTX浓度进行连续测定。结果 :滴入MTX后 0、6、12、2 4和 3 6h的脑脊液浓度分别为 ( 1 65± 1 5 2 )×10 -6、( 4 3± 3 3 4)× 10 -7、( 1 46± 1 10 )×10 -7和 ( 3 19± 4 3 8)× 10 -8mol/L ,3 6h时已测不出MTX浓度 ,它的药 -时曲线与血浆相类似。直线回归方程 :Y∧ =0 0 5 797+0 0 10 82X(r =0 83 5 7)。结论 :脑脊液中MTX代谢呈二室模型 。OBJECTIVE:To study the pharmacokinetics in cerebrospinal fluid (CSF) during high dose methotrexate (HD-MTX)chemotherapy.METHODS: The MTX concentrations in CSF and plasma were measured by Reversed Phase High Performance Liquid Chromatography (RP-HPLC) in 27 patients with tumour administered with MTX (1.0-3.0 g).RESULTS: The MTX concentrations in CSF were (1.65±1.52)×10 -6mol/L(0 h),(4.3±3.34)×10 -7mol/L(6 h),(1.46±1.10)×10 -7mol/L(12 h) and (3.19±4.38)×10 -8mol/L (24 h), and could not be detected (36 h).Its drug-time curve was similar to that of plasma. The linear regression equation: Y∧=0.057 97+0.010 82X(r=0.835 7).CONCLUSIONS: Pharmacokinetics model of MTX in CSF is two-compartment model. There is a positive correlation between the MTX concentrations in CSF and plasma.

关 键 词：甲氨蝶呤 色谱法 高效液相/方法 输注 静脉内 

分 类 号：R96[医药卫生—药理学]