Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter

Y. Ohkawa, M. Matsumura, Y. Kurosaki, M. Kurumi, Kenji Sasaki, T. Nakayama

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8 Citations (Scopus)


The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine, and its 4-O-sulfate (4-S) on the pharmacokinetics of antipyrine were investigated in rats. Plasma elimination of intravenously administered antipyrine was significantly decelerated under a steady-state concentration of 4-OH but not under that of 4-S. Tissue-to-plasma concentration ratio (Kp) of antipyrine under its steady-state concentration was significantly increased in the brain and heart by the concomitant use of 4-OH, while similar use of 4-S had no effect. The enhancement of the blood-brain barrier (BBB) permeability of antipyrine caused by the concomitant use of 4-OH was believed to be concerned with the increase of the Kp value of antipyrine in the brain. These results suggested that 4-OH could be used as a biodistribution promoter.

Original languageEnglish
Pages (from-to)529-534
Number of pages6
JournalBiological and Pharmaceutical Bulletin
Issue number5
Publication statusPublished - 2001


  • 4-hydroxyantipyrine
  • 4-hydroxyantipyrine O-sulfate
  • Antipyrine
  • Biodistribution promoter
  • Concomitant use
  • Drug/metabolite interaction

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science


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