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Effects of 4-Hydroxyantipyrine and Its 4-O-Sulfate on Antipyrine as Biodistribution Promoter.

2001; Pharmaceutical Society of Japan; Volume: 24; Issue: 5 Linguagem: Inglês

10.1248/bpb.24.529

1347-5215

Yuhsuke Ohkawa, Miki MATSUMURA, Yuhji KUROSAKI, Masateru Kurumi, Kenji Sasaki, Taiji Nakayama,

Receptor Mechanisms and Signaling

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.