Coutts R T, Torok-Both G A, Chu L V, Tam Y K, Pasutto F M
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.
J Chromatogr. 1987 Oct 30;421(2):267-80.
The metabolism of a large dose (40 mg/kg intraperitoneally) of lidocaine (LIDO) in mature male Sprague-Dawley rats is described. Pentafluorobenzoyl chloride was used to derivatize the hydrolyzed urinary metabolites prior to extraction and analysis as pentafluorobenzoyl-derivatives by combined gas chromatography-mass spectrometry. Total ion and selected ion current (m/z 195; C6F5CO+) traces were recorded and metabolites of LIDO were readily identified. Only one major metabolite, 3-hydroxy-N-(N-ethylglycyl)-2,6-xylidine, was excreted in urine. A new metabolite, 3-hydroxy-N-glycyl-2,6-xylidine was also present in significant amounts, as well as minor quantities of four oxygenated metabolites of N-(N-ethylglycyl)-2,6-xylidine. Other known metabolites of LIDO, including 3-hydroxylidocaine, were excreted in trace quantities. The results suggest that metabolism of LIDO in rats may be age- and/or dose-dependent.
描述了大剂量（40mg/kg腹腔注射）利多卡因（LIDO）在成年雄性Sprague-Dawley大鼠体内的代谢情况。在通过气相色谱-质谱联用仪将水解后的尿液代谢物提取并分析为五氟苯甲酰衍生物之前，使用五氟苯甲酰氯对其进行衍生化。记录了总离子流和选择离子流（m/z 195；C6F5CO+）的图谱，利多卡因的代谢物很容易被识别。尿液中仅排出一种主要代谢物，即3-羟基-N-（N-乙基甘氨酰基）-2,6-二甲基苯胺。一种新的代谢物，3-羟基-N-甘氨酰基-2,6-二甲基苯胺也大量存在，同时还含有少量N-（N-乙基甘氨酰基）-2,6-二甲基苯胺的四种氧化代谢物。利多卡因的其他已知代谢物，包括3-羟基利多卡因，仅以痕量排出。结果表明，利多卡因在大鼠体内的代谢可能与年龄和/或剂量有关。
