非法设计药物“摇头丸”(一种改性安非他明)的高效液相色谱分析及其在稳定性、分配和血浆蛋白结合方面的应用。

Acta pharmaceutica Nordica Pub Date : 1991-01-01
E R Garrett, K Seyda, P Marroum
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引用次数: 0

摘要

建立了特异、灵敏的3,4-亚甲基二氧基苯丙胺(MDMA)和3,4-亚甲基二氧基苯丙胺(MDA)的反相高效液相色谱(HPLC)分析方法,在280 nm分光光度检测下,MDMA和MDA的分析灵敏度分别低至2.7 ng/ml和1.6 ng/ml。测定了MDMA和MDA的一些性质。两种药物在1 M盐酸水溶液和1 M氢氧化钠溶液中均稳定。在90℃、6 m3 HCl的极端条件下,MDMA的半衰期为6.6 h, MDA的半衰期为7.1 h。在25℃和39℃条件下,MDMA和MDA在血浆中高度稳定28 h,冷冻血浆47 d后药物浓度保持不变。血浆和红细胞中MDMA和MDA浓度测定的表观红细胞-血浆分配系数均为1.45。本文提出了一个方程,用于校正红细胞中被困的平衡血浆/缓冲液中的药物浓度。通过多种方法测定犬血浆蛋白的MDMA和MDA结合率,两种药物的结合率均为0.34 ~ 0.40。蛋白质的结合程度与药物浓度无关。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
High performance liquid chromatographic assays of the illicit designer drug "Ecstasy", a modified amphetamine, with applications to stability, partitioning and plasma protein binding.

Specific, sensitive, reverse-phase high-performance liquid chromatographic (HPLC) assays of 3,4-methylenedioxymethamphetamine (MDMA) and 3,4-methylenedioxyamphetamine (MDA) have been devised with analytical sensitivities as low as 2.7 ng/ml of plasma for MDMA and 1.6 ng/ml for MDA, using spectrophotometric detection at 280 nm. The assays were used to determine some properties of MDMA and MDA. Both drugs were stable in aqueous 1 M HCl, and 1 M NaOH solutions at room temperature. The half-life for MDMA was 6.6 h and for MDA was 7.1 h under the extreme conditions of 90 degrees C and 6 M HCl. MDMA and MDA were highly stable for 28 h in plasma at 25 degrees and 39 degrees C. The concentrations of the drugs were unchanged in frozen plasma after 47 days. The apparent red blood cell-plasma partition coefficient determined from assayed concentrations of the drugs in plasma and erythrocytes was 1.45 for both MDMA and MDA. An equation is presented to correct drug concentration in erythrocytes for the trapped equilibrated plasma/buffer in the packed red blood cells. The fraction of MDMA and MDA bound to dog plasma proteins was determined by several methods and it is 0.34-0.40 for both drugs. The extent of protein binding was independent of the drugs' concentration.

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