An assay for cocaethylene and other cocaine metabolites in liver using high-performance liquid chromatography.
An assay for cocaethylene and other cocaine metabolites in liver using high-performance liquid chromatography.
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使用高效液相色谱法测定肝脏中的可卡乙烯和其他可卡因代谢物。
DOI：
10.1016/0003-2697(92)90103-e
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发表时间：
1992
影响因子：
2.9
通讯作者：
Harbison,RD
中科院分区：
文献类型：
--
作者：
Roberts,SM;Munson,JW;James,RC;Harbison,RD
可卡因乙烯（苯甲酰芽子碱乙酯或乙基可卡因）是可卡因和乙醇的酯交换产物，在联合使用这些药物的个体的尿液中观察到。有证据表明，可卡因乙烯具有抑制活性，其在体内的形成可能导致可卡因的毒性。本文提出了一种新的方法，该方法能够定量可卡因和可卡因，以及可卡因代谢产物苯甲酰芽子碱和去甲可卡因在肝组织中。该方法采用高效液相色谱法和紫外检测器（235 nm），可卡因的丙酯用作内标。首先用0.1 N磷酸氢二钾（pH 9.1）缓冲肝匀浆，然后用二氯甲烷：异丙醇（9：1）提取。目标化合物的提取效率约为75-85%。可卡因浓度重复测定（N = 10）的变异系数为5.75%，可卡因、去甲可卡因和苯甲酰芽子碱的值相当。基于比背景噪声大三倍的峰高，古柯乙烯的检测限约为1.7 ng注射化合物。使用这种方法，它表明，可卡因和乙醇管理后，在小鼠肝脏中存在的可卡因，具有明显的快速形成和消除。
Cocaethylene (benzoylecgonine ethyl ester or ethyl cocaine) is a transesterification product of cocaine and ethanol that has been observed in the urine of individuals using these drugs in combination. There is evidence that cocaethylene is pharmacologically active, and its formation in vivo may contribute to the toxicity of cocaine. A new method is presented here which enables the quantification of cocaethylene and cocaine, as well as the cocaine metabolites benzoylecgonine and norcocaine in liver tissue. This method utilizes high-performance liquid chromatography with uv detection (235 nm), and the propyl ester of cocaine is used as an internal standard. Liver homogenates are first buffered with 0.1 n dibasic potassium phosphate (pH 9.1) and then extracted with methylene chloride:isopropanol (9:1). Extraction efficiencies were approximately 75–85% for the compounds of interest. The coefficient of variation for replicate determinations (N = 10) of cocaethylene concentration was 5.75%, with comparable values obtained for cocaine, norcocaine, and benzoylecgonine. The detection limit for cocaethylene, based on a peak height threefold greater than background noise, was approximately 1.7 ng of injected compound. Using this method, it was demonstrated that cocaethylene is present in mouse liver following cocaine and ethanol administration, with an apparent rapid rate of formation and elimination.