Little information on the human metabolism and urinary elimination of hydrafinil (9-fluorenol) exists. In order to support preventive anti-doping activities concerning compounds such as hydrafinil, a pilot elimination study was conducted with three healthy male volunteers receiving a single oral dose of 50 mg of hydrafinil. Urine samples were collected prior to and up to 72-h post-administration and were subjected to both gas chromatography–mass spectrometry and liquid chromatography–mass spectrometry, which allowed for the identification of the intact drug as well as Phase I and Phase II metabolites, primarily hydroxylated and/or glucuronidated or sulfo-conjugated hydrafinil. The identity of these metabolites was corroborated by high-resolution/high-accuracy tandem mass spectrometry, and the applicability of routine doping control workflows for the detection of hydrafinil and its main metabolites was assessed. Therefore, two findings of hydrafinil and its metabolites were recorded, which concerned out-of-competition doping control samples and, hence, were not pursued with confirmatory analyses. Yet, the initial testing procedure results indicate that hydrafinil might require consideration in sports drug testing programs to ensure its detection, if classified as prohibited by the World Anti-Doping Agency (WADA).

中文翻译：

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用于常规兴奋剂控制目的的尿 hydrafinil 代谢物的质谱表征

很少有关于 hydrafinil (9-芴醇) 的人体代谢和尿液消除的信息。为了支持预防性反兴奋剂活动，例如 hydrafinil，对三名健康男性志愿者进行了一项初步消除研究，他们接受了 50 mg hydrafinil 的单次口服剂量。在给药前和给药后 72 小时内收集尿液样本，并进行气相色谱-质谱法和液相色谱-质谱法，以便鉴定完整的药物以及 I 期和 II 期代谢物，主要是羟基化和/或葡萄糖醛酸化或磺基共轭的hydrafinil。高分辨率/高精度串联质谱证实了这些代谢物的身份，并评估了常规兴奋剂控制工作流程对检测 hydrafinil 及其主要代谢物的适用性。因此，记录了 hydrafinil 及其代谢物的两项发现，这些发现涉及赛外兴奋剂对照样品，因此未进行验证性分析。然而，最初的测试程序结果表明，如果世界反兴奋剂机构 (WADA) 将其归类为禁止，则可能需要在运动药物测试项目中考虑 hydrafinil 以确保其检测到。