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异环磷酰胺(NSC - 109724)在人体中的代谢研究。

Studies on the metabolism of isopnosphamide (NSC-109724) in man.

作者信息

Norpoth K

出版信息

Cancer Treat Rep. 1976 Apr;60(4):437-43.

PMID:1277219
Abstract

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.

摘要

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%。

相似文献

1
Studies on the metabolism of isopnosphamide (NSC-109724) in man.异环磷酰胺(NSC - 109724)在人体中的代谢研究。
Cancer Treat Rep. 1976 Apr;60(4):437-43.
2
[Quantitative determination of cyclophosphamide, ifosfamide, and trofosfamide and their stable metabolites on TLC-plates with the aid of 4-pyridine-aldehyde-2-benzothiazolyl-hydrazone (PBH) (author's transl)].
Arzneimittelforschung. 1975 Sep;25(9):1331-6.
3
Studies on the human pharmacokinetics of isophosphamide (NSC-109724).异环磷酰胺(NSC-109724)的人体药代动力学研究。
Cancer Treat Rep. 1976 Apr;60(4):451-8.
4
Side chain oxidation of ifosfamide in man.异环磷酰胺在人体内的侧链氧化。
Klin Wochenschr. 1975 Nov 15;53(22):1075-6. doi: 10.1007/BF01614384.
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[Isolation and characterisation of two main metabolites of ifosfamide from human urine (author's transl)].人尿中异环磷酰胺两种主要代谢物的分离与鉴定(作者译)
Arzneimittelforschung. 1976;26(7):1376-7.
6
Excretion kinetics of ifosfamide side-chain metabolites in children on continuous and short-term infusion.异环磷酰胺侧链代谢产物在持续和短期输注儿童中的排泄动力学
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7
Quantification by gas chromatography of N,N'-di-(2-chloroethyl)-phosphorodiamidic acid in the plasma of patients receiving isophosphamide.
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X-ray crystallographic studies of cyclophosphamide (NSC-26271) derivatives.
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Biologic activity of two derivatives and six possible metabolites of cyclophosphamide (NSC-26271).环磷酰胺(NSC - 26271)的两种衍生物及六种可能代谢物的生物活性
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Cancer Chemother Pharmacol. 1990;26(2):105-11. doi: 10.1007/BF02897254.

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