Kimura T, Sternson L A, Higuchi T
Clin Chem. 1976 Oct;22(10):1639-43.
We describe a gas chromatographic method for measuring submicrogram quantities of dianhydrogalactitol, a promising antineoplastic agent (currently undergoing clinical trials in humans), in plasma. The drug is first extracted from blood plasma by saturating the aqueous phase with solid potassium carbonate and extracting with isopropanol/chloroform (9/1 by vol). It is then converted to the corresponding n-butaneboronic ester by reaction at room temperature with butaneboronic acid and chromatographed on an SE-30 (3%) column, with flame ionization detection. Practicality of the method for monitoring drug distribution was demonstrated by administering dianhydrogalactitol in therapeutic doses to a dog and monitoring its concentrations in blood for the next 2 h.
我们描述了一种气相色谱法，用于测定血浆中亚微克量的双脱水半乳糖醇（一种有前景的抗肿瘤药物，目前正在进行人体临床试验）。首先通过用固体碳酸钾使水相饱和并用异丙醇/氯仿（体积比9/1）萃取，从血浆中提取该药物。然后在室温下使其与丁硼酸反应转化为相应的正丁硼酸酯，并在配备火焰离子化检测器的SE - 30（3%）柱上进行色谱分析。通过给一只狗施用治疗剂量的双脱水半乳糖醇并在接下来的2小时内监测其血液浓度，证明了该方法在监测药物分布方面的实用性。
