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  • P-ISSN 1225-0163
  • E-ISSN 2288-8985

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

Analytical Science and Technology / Analytical Science and Technology, (P)1225-0163; (E)2288-8985
2000, v.13 no.3, pp.385-393
Lee, Jeong Ae
Kim, Younglim
Lho, Dong-Seok
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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 <TEX>${\beta}$</TEX>-oxidation of the heptanoic side chain with formation of pentanoic side chain metabolite (<TEX>$C_5$</TEX>-metabolite), and lactamizarion by internal dehydration of (<TEX>${\beta}$</TEX>-oxidized metabolite (<TEX>${\delta}$</TEX>-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, <TEX>${\delta}$</TEX>-lactam, and <TEX>$C_5$</TEX>-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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