Norpoth K
Cancer Treat Rep. 1976 Apr;60(4):437-43.
A method is described for the quantitative determination of cyclophosphamide, isophosphamide, and trophosphamide and their stable alkylating metabolites on thin-layer chromatography plates with the aid of 4-pyridinealdehydr-2-benzothiazolylhydrazone (PBH). The method requires only 0.01-0.02 ml of urine from patients treated with high doses of cyclophosphamide of isophosphamide, but a careful standarization is required by using reference substances. In the urine of patients treated with isophosphamide, the 4-carboxy derivative and two different dechloroethyl derivatives resulting from side-chain oxidation are the predominant metabolites determined, next to isophosphamide. Side-chain oxidation may be prevalent. Determination of isophosphamide and its stable alkylating metabolites in the urine of 25 patients shows that the ratio of unchanged isophosphamide to its metabolites varies widely. The mean value of the total amount of PBH-reactive compounds exceeded 50% of the given dose, whereas less than 1% was found to be converted to urine metabolites which release acrolein.
描述了一种借助4-吡啶醛-2-苯并噻唑腙(PBH)在薄层色谱板上定量测定环磷酰胺、异环磷酰胺、曲磷胺及其稳定烷基化代谢物的方法。该方法仅需0.01 - 0.02毫升接受高剂量环磷酰胺或异环磷酰胺治疗患者的尿液,但使用参考物质时需要仔细标准化。在用异环磷酰胺治疗的患者尿液中,4-羧基衍生物以及由侧链氧化产生的两种不同的脱氯乙基衍生物是除异环磷酰胺外测定的主要代谢物。侧链氧化可能很普遍。对25例患者尿液中异环磷酰胺及其稳定烷基化代谢物的测定表明,未改变的异环磷酰胺与其代谢物的比例差异很大。PBH反应性化合物总量的平均值超过给定剂量的50%,而发现转化为释放丙烯醛的尿液代谢物的不到1%。