高等学校化学学报

高等学校化学学报 ›› 2000, Vol. 21 ›› Issue (5): 690.

• 论文 • 上一篇    下一篇

LC/MSn法鉴定二氧苯柳胺在家兔体内的主要代谢产物

顾景凯1, 钟大放2, 陈笑艳2, 周慧1, 沈家骢1, 林阳3   

  1. 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
  • 收稿日期:1999-08-30 出版日期:2000-05-24 发布日期:2000-05-24
  • 通讯作者: 顾景凯(1963年出生),男,博士,副教授,从事药物代谢与药物动力学研究.
  • 基金资助:

    国家自然科学基金(批准号:39625025)

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

GU Jing-Kai1, ZHONG Da-Fang2, CHEN Xiao-Yan2, ZHOU Hui1, SHEN Jia-Cong1, LIN Yang3   

  1. 1. College of Life Science, Key Lab. for Supramolecular Structure and Spectroscopy, Jilin University, Changchun 130023, China;
    2. Lab. of Drug Metabolism and Pharmacokinetics, Shengyang Pharmaceutical University, Shenyang 110015, China;
    3. PLA Dalian Junior College of Medicine, Dalian 116017, China
  • Received:1999-08-30 Online:2000-05-24 Published:2000-05-24

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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400mg乙氧苯柳胺,收集服药后0～10h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/MSn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。

关键词: N-4-(乙氧苯基)-2-羟基苯甲酰胺, 液相色谱/质谱法, 代谢物

Abstract: 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 SPEcolumn (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.

Key words: N-(4-Ethoxyphenyl)-2-hydroxyl-benzamide, Liquid chromatography/ion trap mass spectrometry, Metabolite

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