Prox A, Breyer-Pfaff U
Dr. Karl Thomae GmbH, Biberach, Department of Chemical Research, Biberach, FRG.
Drug Metab Dispos. 1987 Nov-Dec;15(6):890-6.
From the urine patients being treated with amitriptyline, drug metabolites were extracted by adsorption to polystyrene. Nonconjugated compounds and aglycones liberated by enzymic hydrolysis were purified separately by repeated TLC and characterized by physicochemical and chemical methods. Besides the known E- and Z-10-hydroxy derivatives of amitriptyline (AT), nortriptyline (NT), and their primary amine analogue, two isomeric 10,11-dihydroxy compounds could be identified in each series. Metabolites with an oxo function in position 10 occurred in minor quantities. The phenols 2-hydroxy-NT and 2,11-dihydroxy-NT, as well as the 1,2-dihydrodiol derived from NT, were regularly present, while the corresponding tertiary amines as well as 3-hydroxy-AT and -NT were detected occasionally in very small amounts.
从接受阿米替林治疗的患者尿液中，通过吸附到聚苯乙烯上提取药物代谢物。通过反复薄层层析分别纯化经酶水解释放出的非共轭化合物和苷元，并采用物理化学和化学方法对其进行表征。除了已知的阿米替林（AT）、去甲替林（NT）的E型和Z型10-羟基衍生物及其伯胺类似物外，在每个系列中还可鉴定出两种异构的10,11-二羟基化合物。在10位具有氧代功能的代谢物含量较少。酚类2-羟基-NT和2,11-二羟基-NT以及源自NT的1,2-二氢二醇经常存在，而相应的叔胺以及3-羟基-AT和-NT偶尔能检测到极少量。
