Dell H D, Fielder J, Kamp R, Gau W, Kurz J, Weber B, Wuensche C
Drug Metab Dispos. 1982 Jan-Feb;10(1):55-60.
Etofenamate [2-(2-hydroxyethoxy)ethyl-N-(alpha, alpha, alpha-trifluoro-m-tolyl)-anthranilate] was administered to dogs by the oral route. Minor amounts of etofenamate (Eto) and its glucuronide were found in urine and feces. The main portion of metabolites was eliminated as flufenamic acid (Flu) and hydroxy derivatives of Eto and Flu. Furthermore, a highly lipophilic fraction was isolated (extraction and TLC) and further separated into several compounds (HPLC, GLC). These metabolites were identified as Eto oleate, palmitate, linoleate, stearate, palmitoleate, myristate, and laurate by NMR and MS. The structures were confirmed by comparison with authentic material. The conjugation of etofenamate with fatty acids is an example of a new route of drug metabolism.
依托芬那酯[2-(2-羟基乙氧基)乙基-N-(α,α,α-三氟间甲苯基)-邻氨基苯甲酸酯]经口服途径给予犬。在尿液和粪便中发现了少量的依托芬那酯（Eto）及其葡糖醛酸苷。代谢物的主要部分以氟芬那酸（Flu）以及依托芬那酯和氟芬那酸的羟基衍生物形式被消除。此外，分离出了一个高亲脂性部分（萃取和薄层色谱法），并进一步分离成几种化合物（高效液相色谱法、气相色谱法）。通过核磁共振和质谱法将这些代谢物鉴定为依托芬那酯油酸酯、棕榈酸酯、亚油酸酯、硬脂酸酯、棕榈油酸酯、肉豆蔻酸酯和月桂酸酯。通过与标准物质比较确认了其结构。依托芬那酯与脂肪酸的结合是药物代谢新途径的一个例子。
