LC/MS^n法鉴定二氧苯柳胺在家兔体内的主要代谢产物  

Identification of Major Metabolites of Etofesalamide in Rabbits by Liquid Chromatography/Ion Trap Mass Spectrometry

作　　者：顾景凯[1] 钟大放[2] 陈笑艳[2] 周慧[1] 沈家骢[1] 林阳[3] 

机构地区：[1]吉林大学生命科学学院超分子结构与谱学开放实验室,长春130023 [2]沈阳药科大学药物代谢与药物动力学实验室,沈阳110015 [3]中国人民解放军大连医学高等专科学校,大连116017

出　　处：《高等学校化学学报》2000年第5期690-693,共4页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金!(批准号:39625025)

摘　　要：报道了治疗痤疮新药乙氧苯柳胺［Ｎ－４－（乙氧苯基）－２－羟基苯甲酸胺］在家兔尿中的主要代谢产物．选择 ４只健康家兔，单剂量口服 ４００ ｍｇ乙氧苯柳胺，收集服药后 ０～１０ ｈ的尿样．将未经或经过β－Ｄ－葡萄糖苷酸酶／硫酸酯酶水解的尿样以固相萃取柱纯化后，采用 ＬＣ／ＭＳ~ｎ方法对尿中推测的代谢物和标准品分别进行选择离子监测（ＳＩＭ）和多级全扫描质谱（ＭＳ~ｎ）分析．结果在尿中发现了 ５个代谢物，分别为利胆酚［Ｎ－（对－羟基苯基）－水杨酰胺］以及利胆酚和乙氧苯柳胺与硫酸或葡糖醛酸的结合物．The major metabolites of etofesalamide [N-(4-ethoxyphenyl)-2-hydroxyl-benzamide],a novel drug for acne therapy, in rabbits were described. Urine samples from 0 to 10 h were collected after single oral administration of 400 mg etofesalamide to four rabbits. The samples with or without hydrolysis by β-D-glucuronidase/sulphatase were purified by SPE column (Sep--Pah C18) and then were analyzed with LC/MSn for potential metabolites. Etofesalamide and its five metabolites were identified in rabbit urine based on the reference substances and mass spectra. These included oxaphenamide [N-(p-hydrox- yphenylsalicyl)] and the conjugates of glucuronide and sulfate for etofesalamide and oxaphenamide, respectively.

关 键 词：液相色谱/质谱法 代谢物 乙氧苯柳胺 药物代谢 

分 类 号：R986[医药卫生—药品] R969.1[医药卫生—药学]