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低剂量γ-丁内酯单次摄入后γ-羟基丁酸的药代动力学及血清和尿液中的检测窗口期——一项针对两名志愿者的实验

Pharmacokinetics of GHB and detection window in serum and urine after single uptake of a low dose of GBL - an experiment with two volunteers.

作者信息

Schröck Alexandra, Hari Yvonne, König Stefan, Auwärter Volker, Schürch Stefan, Weinmann Wolfgang

机构信息

Institute of Forensic Medicine, Forensic Toxicology and Chemistry, University of Bern, Switzerland.

出版信息

Drug Test Anal. 2014 Apr;6(4):363-6. doi: 10.1002/dta.1498. Epub 2013 Jun 4.

Abstract

During the last few years γ-hydroxybutyric acid (GHB) and γ-butyrolactone (GBL) have attracted much interest as recreational drugs and knock-out drops in drug-facilitated sexual assaults. This experiment aims at getting an insight into the pharmacokinetics of GHB after intake of GBL. Therefore Two volunteers took a single dose of 1.5 ml GBL, which had been spiked to a soft drink. Assuming that GBL was completely metabolized to GHB, the corresponding amount of GHB was 2.1 g. Blood and urine samples were collected 5 h and 24 h after ingestion, respectively. Additionally, hair samples (head hair and beard hair) were taken within four to five weeks after intake of GBL. Samples were analyzed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) after protein precipitation with acetonitrile. The following observations were made: spiked to a soft drink, GBL, which tastes very bitter, formed a liquid layer at the bottom of the glass, only disappearing when stirring. Both volunteers reported weak central effects after approximately 15 min, which disappeared completely half an hour later. Maximum concentrations of GHB in serum were measured after 20 min (95 µg/ml and 106 µg/ml). Already after 4-5 h the GHB concentrations in serum decreased below 1 µg/ml. In urine maximum GHB concentrations (140 µg/ml and 120 µg/ml) were measured after 1-2 h, and decreased to less than 1 µg/ml within 8-10 h. The ratio of GHB in serum versus blood was 1.2 and 1.6.

摘要

在过去几年中,γ-羟基丁酸(GHB)和γ-丁内酯(GBL)作为娱乐性药物以及在药物辅助性性侵犯罪中使用的迷奸药引起了广泛关注。本实验旨在深入了解摄入GBL后GHB的药代动力学。因此,两名志愿者服用了单剂量1.5毫升添加到软饮料中的GBL。假设GBL完全代谢为GHB,相应的GHB量为2.1克。分别在摄入后5小时和24小时采集血液和尿液样本。此外,在摄入GBL后的四到五周内采集头发样本(头发和胡须)。用乙腈进行蛋白质沉淀后,通过液相色谱-串联质谱法(LC-MS/MS)对样本进行分析。观察结果如下:添加到软饮料中的GBL味道非常苦,在玻璃杯底部形成一层液体,只有搅拌时才会消失。两名志愿者均在大约15分钟后报告出现轻微的中枢效应,半小时后完全消失。血清中GHB的最大浓度在20分钟后测得(分别为95微克/毫升和106微克/毫升)。在4 - 5小时后,血清中GHB浓度已降至1微克/毫升以下。尿液中GHB的最大浓度(分别为140微克/毫升和120微克/毫升)在1 - 2小时后测得,并在8 - 10小时内降至1微克/毫升以下。血清中GHB与血液中GHB的比值分别为1.2和1.6。

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