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女性口服补充剂后海松子碱的尿排泄特征 - 兴奋剂使用场景。

Urinary excretion profile of higenamine in females after oral administration of supplements - Doping scenario.

机构信息

Seibersdorf Labor GmbH, Seibersdorf, Austria; Singidunum University, Belgrade, Serbia.

Antidoping Agency, Belgrade, Serbia.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Mar 1;1235:124047. doi: 10.1016/j.jchromb.2024.124047. Epub 2024 Feb 15.

DOI:10.1016/j.jchromb.2024.124047
PMID:38387341
Abstract

In 2017, higenamine was added to the World Antidoping Agency's (WADA) Prohibited list under group S3: beta-2 agonists and it is banned for athletes both in - and out of competition. Aim of this study was to characterize the urinary excretion profile of higenamine and its metabolite coclaurine after oral administration of multiple doses of higenamine capsules. For this purpose, an administration study including female basketball players was performed. For the detection of higenamine and cocalurine in the collected urine samples, a new, fast, and highly sensitive quantitative on-line SPE LC HRMS method was developed and validated. The method was applied for the quantification of higenamine and cocalurine in urine and their excretion pattern was defined. Results obtained show substantial inter-individual differences in the excretion profile of higenamine and coclaurine. For higenamine, half-lives were estimated to be between 4 and 27 h, and for coclaurine between 5 and 25 h. Furthermore, the data indicate that the elimination of coclaurine is rate-limited by its formation. Higenamine could be detected at a urine concentration above 10 ng/mL for at least 20 h after the last application for all study participants.

摘要

2017 年,盐酸育亨宾被世界反兴奋剂机构(WADA)列入 S3 组禁用清单:β-2 激动剂,无论是在比赛中还是在比赛外,运动员都被禁止使用。本研究的目的是描述口服盐酸育亨宾胶囊多次给药后盐酸育亨宾及其代谢物可可碱的尿排泄特征。为此,进行了一项包括女性篮球运动员的管理研究。为了检测收集的尿液样本中的盐酸育亨宾和可可碱,开发并验证了一种新的、快速且高度敏感的在线 SPE LC HRMS 定量方法。该方法用于定量检测尿液中的盐酸育亨宾和可可碱,并定义其排泄模式。结果表明,盐酸育亨宾和可可碱的排泄模式存在显著的个体间差异。盐酸育亨宾的半衰期估计在 4 至 27 小时之间,可可碱的半衰期在 5 至 25 小时之间。此外,数据表明可可碱的消除受其形成的限制。所有研究参与者在最后一次给药后至少 20 小时,尿液中盐酸育亨宾的浓度仍可检测到 10ng/ml 以上。

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