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Gas Chromatographic/Mass Spectrometric Characterization of Dromostanolone Metabolites in Human Urine

机译:人体尿液中单羟萘甾酮代谢物的气相色谱/质谱表征

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The metabolism of dromostanolone (2メ-methyl-5メ - androstan-17モ-ol-3-one) was studied in three adult volunteers after oral dose of 20 mg. Solvent extracts of urine obtained after enzyme hydrolysis were derivatized with MSTFA/TMCS and MSTFA/TMIS. The structures of intact drug and its metabolites were determined by gas chromatography/mass spectrometry (GC/MS) in electron impact (EI) mode. The major metabolite (2メ-methyl-5メ- androstan-3メ-ol-17-one), its 3モ -epimer, parent compound, and several hydroxylated metabolites including intact drug were detected by comparing total ion chromatograms of control urine with that of the administered sample. Two epimers of 2メ -methyl-5メ- androstan-3,17モ-diol were detected using selected ion monitoring. The maximum excretion of dromostanolone and 2メ-methyl-5メ- androstan-3メ-ol-17-one was reached in 6.2-15 hr. The half-life of intact dromostanolone was 5.3 hr. About 3.0% of the administered amount was found to be excreted within 95 hr as unchanged form.
机译:口服剂量为20 mg后,在三名成人志愿者中研究了dromostanolone(2′-甲基-5′- androstan-17mo-ol-3-one)的代谢。酶水解后获得的尿液溶剂提取物用MSTFA / TMCS和MSTFA / TMIS衍生化。完整的药物及其代谢产物的结构通过气相色谱/质谱(GC / MS)在电子碰撞(EI)模式下确定。通过比较对照尿液的总离子流图,可检测出主要代谢物(2メ-甲基-5メ-雄烷-3メ-ol-17-one),其3mo-ep基,母体化合物以及包括完整药物在内的几种羟基化代谢物。与所管理样品的使用选定的离子监测方法检测到2个-3-甲基-5--雄酮-3,17-二醇的差向异构体。 dromostanolone和2′-甲基-5′-雄烷-3′-ol-17-one的最大排泄量在6.2-15小时内达到。完整的dromostanolone的半衰期为5.3小时。发现约3.0%的施用量在95小时内以不变的形式排泄。

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