Zolpidem and zolpidem phenyl-4-carboxylic acid pharmacokinetics in oral fluid after a single dose
Zolpidem and zolpidem phenyl-4-carboxylic acid pharmacokinetics in oral fluid after a single dose
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DOI：
10.1002/dta.2594
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发表时间：
2019-07-01
影响因子：
2.9
通讯作者：
Shen, Min
中科院分区：
文献类型：
--
作者：
Feng, Xueyi;Chen, Hang;Shen, Min
背景在毒品促成犯罪和路边药物测试的背景下，口服液唑吡坦的检测表明最近服用了唑吡坦。已经描述了唑吡坦在血液和尿液等经典生物基质中的药代动力学；然而，基于口服液的此类数据的报道有限。目的研究口服液中唑吡坦及其主要代谢物唑吡坦苯基-4-羧酸(ZPCA)的药代动力学。方法14名受试者口服10 mg酒石酸唑吡坦片，于不同时间采集口服液样品，柱后加入试剂，采用LC-MS/MS联用技术进行分析。结果唑吡坦和ZPCA在口服1h后均能被检测到，并迅速消除，半衰期分别为2.77±0.71h和5.11±0.67h。唑吡坦最大浓度(36.73+/-10.89 ng/mL)出现在2+/-0.52h，ZPCA最大浓度(0.28+/-0.16 ng/mL)出现在2+/-0.37h。在服用唑吡坦后，唑吡坦/ZPCA比率降低，这一观察结果可能有助于确定药物使用时间。结论口服液中唑吡坦浓度的测定可用于毒品犯罪和路边毒品检测环境中唑吡坦的非侵入性监测。
Background Oral fluid zolpidem detection in the settings of drug-facilitated crime and roadside drug testing indicates recent zolpidem intake. Zolpidem pharmacokinetics in classical biological matrices such as blood and urine have been described; however, reports of such data based on oral fluids are limited. Objective The aim of this study is to describe the pharmacokinetics of zolpidem and its major metabolite zolpidem phenyl-4-carboxylic acid (ZPCA) in oral fluids after intake. Methods Ten milligrams of zolpidem tartrate tablets were orally administered to 14 volunteers, and oral fluid samples were collected at various times up to 72 hours and analyzed via liquid chromatography-tandem mass spectrometry (LC-MS/MS) with post-column reagent addition. Results Both zolpidem and ZPCA could be detected in oral fluid after 1 hour and were rapidly eliminated, with half-lives of 2.77 +/- 0.71 hours and 5.11 +/- 0.67 hours, respectively. Maximum zolpidem concentrations (36.73 +/- 10.89 ng/mL) occurred at 2 +/- 0.52 hours, and maximum ZPCA concentrations (0.28 +/- 0.16 ng/mL) occurred at 2 +/- 0.37 hours. Zolpidem/ZPCA ratios decreased after zolpidem intake, an observation that might be helpful for determining the time of drug use. Conclusion The results showed that the measurement of zolpidem in oral fluid can be used for the non-invasive monitoring of zolpidem consumption and misuse in drug-facilitated crime and roadside drug testing settings.