不同给药途径的尿代谢:诊断性尿标志物的选择。

IF 2.7 3区 医学 Q2 BIOCHEMICAL RESEARCH METHODS
Xavier de la Torre, Cristiana Colamonici, Dayamin Martínez Brito, Rodny Montes de Oca Porto, Francesco Botrè
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引用次数: 0

摘要

通过对其主要尿液代谢物4-氯-3α-羟基雄甾-4-en-17-one (M1)的监测,证实了醋酸氯酚经皮应用的意外污染。这项工作旨在描述人类的肠道代谢,并寻找特定的代谢标志物或浓度阈值,从而区分口服和透皮给药,帮助建立适当的标准,以便在怀疑偶然污染时被反兴奋剂界采用。分别给予单次口服(n = 3,男性)、单次经皮给药(n = 1,男性)和多次经皮给药(n = 3,男性和n = 3,女性)后采集尿样。样品经酶解、液-液萃取、形成三甲基硅基衍生物后,采用气相色谱-串联质谱法和飞行时间质谱法进行分析。描述了口服和透皮应用后马桶的代谢。口服给药后(M1-M10)可检出10种代谢物,经皮给药后仅检出5种代谢物(M1-M4和M9)。由于个体间吸收、代谢和/或排泄的差异,使用任何代谢物的浓度可能是困难的。相反,M4和M1之间的比率显示了在这里描述的条件下区分两种管理的合理结果。无法评估使用一种或另一种给药途径的意向性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Clostebol Metabolism by Different Routes of Administration: Selection of Diagnostic Urinary Markers.

The accidental contamination by the use of transdermal applications of clostebol acetate has been proven by the monitoring of its main urinary metabolite 4-chloro-3α-hydroxy-androst-4-en-17-one (M1). This work is aimed at describing clostebol metabolism in humans and at searching for specific metabolic markers or concentration thresholds allowing for distinguishing between an oral and a transdermal administration, helping to set up adequate criteria to be adopted by the antidoping community when incidental contamination is suspected. Urine samples were collected after the administration of a single dose of clostebol acetate orally (n = 3, males), a single transdermal dose (n = 1, male), and multiple transdermal administrations (n = 3, males, and n = 3, females). After enzymatic hydrolysis, liquid-liquid extraction, and the formation of trimethylsilyl derivatives, the samples were analyzed by gas chromatography coupled to tandem mass spectrometry and time-of-flight mass spectrometry. The metabolism of clostebol after oral and transdermal applications was described. Ten metabolites were detected after oral administration (M1-M10), but only five (M1-M4 and M9) could be detected after transdermal applications under the assay conditions applied. The use of concentrations of any metabolite might be difficult because of the interindividual variability in absorption, metabolism, and/or excretion. Instead, the ratios between M4 and M1 showed plausible results to discriminate between both administrations under the conditions described here. The intentionality of the use of one or other route of administration cannot be assessed.

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来源期刊
Drug Testing and Analysis
Drug Testing and Analysis BIOCHEMICAL RESEARCH METHODS-CHEMISTRY, ANALYTICAL
CiteScore
5.90
自引率
24.10%
发文量
191
审稿时长
2.3 months
期刊介绍: As the incidence of drugs escalates in 21st century living, their detection and analysis have become increasingly important. Sport, the workplace, crime investigation, homeland security, the pharmaceutical industry and the environment are just some of the high profile arenas in which analytical testing has provided an important investigative tool for uncovering the presence of extraneous substances. In addition to the usual publishing fare of primary research articles, case reports and letters, Drug Testing and Analysis offers a unique combination of; ‘How to’ material such as ‘Tutorials’ and ‘Reviews’, Speculative pieces (‘Commentaries’ and ‘Perspectives'', providing a broader scientific and social context to the aspects of analytical testing), ‘Annual banned substance reviews’ (delivering a critical evaluation of the methods used in the characterization of established and newly outlawed compounds). Rather than focus on the application of a single technique, Drug Testing and Analysis employs a unique multidisciplinary approach to the field of controversial compound determination. Papers discussing chromatography, mass spectrometry, immunological approaches, 1D/2D gel electrophoresis, to name just a few select methods, are welcomed where their application is related to any of the six key topics listed below.
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