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互联网伪科学:检测具有篡改潜力的含阿片制剂。

Internet pseudoscience: Testing opioid containing formulations with tampering potential.

机构信息

Forensic Toxicology Division, Department of Health Sciences, University of Florence, Largo Brambilla 3, Florence, Italy.

University of Bologna, Department of Medical and Surgical Sciences, Unit of Legal Medicine, Via Irnerio 49, Bologna, Italy.

出版信息

J Pharm Biomed Anal. 2018 May 10;153:16-21. doi: 10.1016/j.jpba.2018.02.014. Epub 2018 Feb 10.

DOI:10.1016/j.jpba.2018.02.014
PMID:29455092
Abstract

Drug tampering practices, with the aim to increase availability of drug delivery and/or enhance drug effects, are accessible on Internet and are practiced by some portion of recreational drug users. Not rarely, recreational misuse may result in toxic and even fatal results. The aim of the present study was to assess the tampering risk of medicaments containing different formulations of an opioid in combination with paracetamol or dexketoprofen, following the procedures reported in dedicated forums on the web. Tablets and suppositories containing codeine, tramadol and oxycodone were extracted following the reported "Cold water extraction"; dextromethorphan was extracted from cough syrup following the procedure reported as "Acid/base extraction" and fentanyl was extracted from transdermal patches according the procedure reported in Internet. The tampered products and opportunely prepared calibrators in water were analysed by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The separation of the analytes was carried on Agilent ZORBAX Eclipse Plus C18 (RRHT 2.1 mm × 50 mm, 1.8 μm) by the gradient elution of 0.01% formic acid in water and 0.01% formic acid in methanol. Acquisition was by MRM mode considering at least two transitions for compound. Declared recoveries for these home-made extractions claimed to exceed 99% for the opioid and to complete remove paracetamol, often associated to liver toxicity and thus to obtain a "safer" preparation. In this study, the authors demonstrated that rarely the recoveries for the opioid reached 90% and that up to 60% of the paracetamol amount remained in solution. Thus, high risks for health remained both for the potential lethality of the opioid content, but also for the sub-lethal chronic use of these mixtures, which contained still uncontrolled, ignored, but often important amounts of paracetamol.

摘要

药物篡改行为旨在增加药物的可获得性和/或增强药物的效果,这些信息可在互联网上获取,并且部分娱乐性药物使用者会采用这种方式。娱乐性药物的误用通常会导致毒性,甚至致命的后果。本研究旨在评估含有不同阿片类药物制剂(与对乙酰氨基酚或右旋酮洛芬合用)的药物的篡改风险,方法是按照网络上专门论坛报道的程序进行操作。按照报道的“冷水萃取”方法从含有可待因、曲马多和羟考酮的片剂和栓剂中提取药物;按照报道的“酸碱萃取”方法从止咳糖浆中提取右美沙芬;按照互联网上报道的方法从透皮贴剂中提取芬太尼。篡改后的产品和在水中适当制备的校准器通过液相色谱-串联质谱(LC-MS/MS)进行分析。通过在 Agilent ZORBAX Eclipse Plus C18 (RRHT 2.1mm×50mm,1.8μm)上进行梯度洗脱(水中 0.01%甲酸和甲醇中 0.01%甲酸)实现对分析物的分离。采用 MRM 模式进行采集,化合物至少考虑两个转换。这些家庭自制萃取物的回收率宣称超过 99%的阿片类药物,且完全去除了常与肝毒性相关的对乙酰氨基酚,从而获得一种“更安全”的制剂。在这项研究中,作者证明了阿片类药物的回收率很少达到 90%,而且有高达 60%的对乙酰氨基酚仍留在溶液中。因此,这些混合物(仍含有未被控制、被忽视但通常是重要的对乙酰氨基酚)存在很高的健康风险,既有阿片类药物潜在致命性的风险,也有潜在的亚致死性慢性使用的风险。

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