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合成代谢类固醇的研究。II——人尿中氧雄龙代谢物的气相色谱/质谱表征。

Studies on anabolic steroids. II--Gas chromatographic/mass spectrometric characterization of oxandrolone urinary metabolites in man.

作者信息

Massé R, Bi H G, Ayotte C, Dugal R

机构信息

Institut National de la Recherche Scientifique (INRS-Santé), Université du Québec, Pointe-Claire, Canada.

出版信息

Biomed Environ Mass Spectrom. 1989 Jun;18(6):429-38. doi: 10.1002/bms.1200180612.

Abstract

The metabolism of 17 alpha-methyl-17 beta-hydroxy-2-oxa-5 alpha-androstan-3-one (oxandrolone) in man has been investigated by gas chromatography/mass spectrometry. After oral administration of a 10 mg dose to man, five metabolites were detected in the free fraction of the urinary samples. Oxandrolone, the major compound excreted in urine, was detected within 72 h after administration. During this period 35.8 and 8.4% of the administered dose was excreted as unchanged oxandrolone and 17-epioxandrolone, respectively. In addition, minute amounts of 16 alpha- and 16 beta-hydroxyoxandrolone and a delta-hydroxy acid resulting from the hydrolysis of the lactone group of oxandrolone were detected in the urine samples 8-60 h after administration. Furthermore, the susceptibility of oxandrolone to hydrolysis was investigated under several pH conditions. Extraction and fractionation of steroidal metabolites was achieved by using C18 and silica Sep Pak chromatography. The mass spectra of the metabolites are presented and major fragmentation pathways discussed.

摘要

通过气相色谱/质谱法对17α-甲基-17β-羟基-2-氧杂-5α-雄甾烷-3-酮(氧雄龙)在人体内的代谢情况进行了研究。给人体口服10毫克剂量后,在尿液样本的游离部分检测到了五种代谢物。氧雄龙是尿液中排出的主要化合物,在给药后72小时内被检测到。在此期间,分别有35.8%和8.4%的给药剂量以未变化的氧雄龙和17-表氧雄龙形式排出。此外,在给药后8 - 60小时的尿液样本中检测到了微量的16α-和16β-羟基氧雄龙以及由氧雄龙内酯基团水解产生的δ-羟基酸。此外,还研究了在几种pH条件下氧雄龙的水解敏感性。通过使用C18和硅胶Sep Pak色谱法实现了甾体代谢物的提取和分馏。给出了代谢物的质谱图并讨论了主要的裂解途径。

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