Analysis of Amineptine and its Metabolites in Human Urine by Gas Chromatography/Mass Spectrometry

Gas Chromatography/Mass Spectrometry를 이용한 뇨중 Amineptine과 그 대사체 분석방법에 관한 연구

  • Lee, Jeong Ae (Bioanalysis and Biotransformation Research Center, Korea Institute of Science and Technology) ;
  • Kim, Younglim (Department of Natural Medicines Evaluation, Natural Medicine Products Division, Korea Food and Drug Administration) ;
  • Lho, Dong-Seok (Bioanalysis and Biotransformation Research Center, Korea Institute of Science and Technology)
  • 이정애 (한국과학기술연구원 생체대사연구센터) ;
  • 김영림 (식품의약품안전청 생약평가부 생약제제과) ;
  • 노동석 (한국과학기술연구원 생체대사연구센터)
  • Received : 2000.02.09
  • Published : 2000.06.25

Abstract

A gas chromatography-mass spectrometric (GC/MS) procedure for the determination of amineptine (dihydro-10, 11-dibenzo[a, d] cycloheptenyl-5-amino-7-heptanoic acid) and its main metabolites in human urine was described. Amineptine has been known to be extensively metabolized by the ${\beta}$-oxidation of the heptanoic side chain with formation of pentanoic side chain metabolite ($C_5$-metabolite), and lactamizarion by internal dehydration of (${\beta}$-oxidized metabolite (${\delta}$-lactam). The detection of these compounds was based on acid hydrolysis, liquid-liquid extraction and trimethylsilylated derivatization of the carboxylic acid group. For the determination of amineptine and its metabolites in biological fluids, selected ions at the m/ 192, molecular ion and one of the characteristic ions were monitored by GC/MS. On the excretion study of amineptine in human urine, 70-90% of amineptine, ${\delta}$-lactam, and $C_5$-metabolite were found to be excreted within 4 hours and their excretion completed within 20 hours.

Keywords

amineptine;lactamization;metabolite;excretion

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