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为了监测大剂量甲氨喋呤（ＨＤＭＴＸ）化疗时脑脊液中药物浓度的动态变化，采用高效液相色谱法对１２例患者２０例次静脉点滴ＨＤＭＴＸ（每次１．５～３．０ｇ）后的脑脊液和血浆中ＭＴＸ浓度同时进行监测，并以２例常规ＭＴＸ用量（每次６０ｍｇ）的脑脊液监测浓度做对比。结果显示，滴注ＭＴＸ后０，６，１２，２４，３６ｈ的脑脊液ＭＴＸ平均浓度分别为３．３７×１０－６，６．８３×１０－７，１．６８×１０－７，２．９９×１０－８，０．４０×１０－８ｍｏｌ／Ｌ，血浆ＭＴＸ平均浓度分别为８．７０×１０－５，２．７９×１０－５，２．６７×１０－６，７．０７×１０－７，６．６５×１０－８ｍｏｌ／Ｌ。２例常规ＭＴＸ用量者的脑脊液ＭＴＸ浓度未测出。结果表明ＨＤＭＴＸ化疗时，脑脊液ＭＴＸ浓度是血浆ＭＴＸ浓度的（４．５７±１．６０）％，２者呈线性关系。并提示ＭＴＸ透过血脑屏障的机理可能为被动转运。
In order to monitor the dynamic changes of drug concentration in cerebrospinal fluid during high-dose methotrexate (HD-MTX) chemotherapy, 20 cases of intravenous infusion of HD-MTX were performed by high performance liquid chromatography (1.5-3.3 each time). After 0g), MTX concentrations in cerebrospinal fluid and plasma were monitored at the same time, and the concentration of cerebrospinal fluid monitored in 2 routine MTX doses (60 mg each) was compared. The results showed that the mean concentrations of MTX in cerebrospinal fluid at 0, 6, 12, 24, and 36 h after instillation of MTX were 3.37×10-6, 6.83×10-7, 1.68×10-7, 2.99, respectively. ×10-8,0.40×10-8 mol/L, mean plasma MTX concentrations were 8.70×10-5, 2.79×10-5, 2.67×10-6, and 7.07×10 respectively. -7, 6.65 x 10-8 mol/L. MTX concentrations in cerebrospinal fluid were not measured in 2 patients with conventional MTX doses. The results showed that the concentration of MTX in CSF was (4.57±1.60)% in the plasma concentration of MTX in HD-MTX chemotherapy, and there was a linear relationship between them. It suggests that the mechanism of MTX through the blood-brain barrier may be passive transport.