Studies on the pharmacokinetics and metabolism of N4-carbamoyl-1,3,4,5-dihydro-diazepam (Uxepam®) in rats, dogs and man

M. Vajda, Zs Tegyey, M. Kozma, L. Vereczkey

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The pharmacokinetics and metabolism of Uxepam®, a new minor tranquillizer, have been investigated in rats [2], dogs and man. For the experiments in rats [2] separation of metabolites of 2-14C-uxepam was achieved by thin-layer chromatography. In the experiments on dogs and man, Extrelut microcolumns were used for preseparation. Recovery was 95% ± 12.77 (S.D.) determined by radioactive tracer experiments. The compounds were separated and determined by reversed-phase HPLC with UV detection at 240 nm. The limit of detection for uxepam was 10 ng ml-1. The metabolises were identified by mass spectrometry. The main metabolites in the rat were desmethyl-uxepam, 5-hydroxy-phenyl-desmethyl-uxepam and diazepam. Desmethyl-carbamoyl-dihydro-diazepam, diazepam and desmethyl-diazepam were found in human plasma. In dogs only one metabolite, desmethyl-uxepam, was detected in plasma. Enterohepatic recycling was observed in dogs and in humans.

Original languageEnglish
Pages (from-to)497-503
Number of pages7
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume4
Issue number4
DOIs
Publication statusPublished - 1986

Keywords

  • HPLC.
  • Uxepam
  • metabolism
  • pharmacokinetics

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmaceutical Science
  • Drug Discovery
  • Spectroscopy
  • Clinical Biochemistry

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