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在应用1g/次—5g/m~2MTX加CF解救的52例肿瘤病人的102疗程中,用改良微生物法测定其血药浓度及药代动力学参数,表明在停止滴注后0及6小时的血清中MTX水平与所给剂量大小成正比,但在18、42、66小时期间则除用1gMTX治疗方案者水平较低外,3g/次—5g/m~2各治疗方案组的血药浓度均相接近。提出了根据获得的参数推算血清MTX浓度预测公式,并提出用药后MTX血清浓度在24小时≤1.3×10~(-6)M,在48小时≤2.4×10~(-7)M,在72小时≤9×10~(-8)M为安全阈值。其中5例用5g/m~2MTX患者同时用HPLC法及改良微生物法检测进行对比,二法所得的体内动力学均符合二室模型,各参数值间统计学上无明显差异,说明改良微生物法测定MTX原型是可靠的。HPLC法还能测出血清7-OH MTX浓度,其达峰时间为停止滴注后6小时,峰浓度为78.75±25.33μM,表观半衰期为14.83±5.88小时。
In the course of 102 courses of 52 cancer patients treated with 1g / time-5g / m ~ 2MTX plus CF rescue, their plasma concentration and pharmacokinetic parameters were measured by modified microbiological method, indicating that at 0 and 6 hours after the stop of instillation Of the serum MTX level is proportional to the size of the dose given, but 18,42,66 hours in addition to 1gMTX treatment regimen lower level, 3g / time -5g / m ~ 2 of the treatment group of blood Concentrations are close together. The prediction formula of serum MTX concentration was proposed based on the obtained parameters. The MTX serum concentration was proposed to be ≤1.3 × 10 ~ (-6) M at 24 hours, ≤2.4 × 10 ~ (-7) M at 48 hours, Hour ≤9 × 10 ~ (-8) M is safety threshold. Among them, 5 cases were treated with 5g / m ~ 2MTX by both HPLC and modified microbiological assay. The in vivo kinetics obtained by the two methods all accorded with two-compartment model. There was no significant difference among the parameters, indicating that the modified microbiological method The MTX prototype is reliable. HPLC method was also able to measure serum 7-OH MTX concentrations up to 6 hours after stopping the instillation, with a peak concentration of 78.75 ± 25.33 μM and an apparent half-life of 14.83 ± 5.88 hours.