Home
Resources
Publications
Application of 4-hydroxyantipyrine and Acetaminophen O-sulfate as Biodistribution Promoter

Application of 4-hydroxyantipyrine and Acetaminophen O-sulfate as Biodistribution Promoter

Y Ohkawa, Y Kiyohara, T Asoh, H Maeda, M Kurumi, K Sasaki, Y Kurosaki, M Matsumura, T Nakayama

Biol Pharm Bull. 2001 Dec;24(12):1404-10.

PMID: 11767111

Abstract:

The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine and its sulfate, 4-hydroxyantipyrine O-sulfate (4-S), on the pharmacokinetics of citicoline and thiopental sodium were investigated in rats. The concomitant use of 4-OH increased significantly the tissue-to-plasma concentration ratio (Kp) of citicoline in the brain and liver and that of thiopental sodium in the brain, liver, and heart, while 4-S did not affect them. The permeability clearance of blood-brain barrier (BBB) (Kin) and the total distribution volume (Vdbr) of citicoline were not affected by either 4-OH or 4-S. However, those of thiopental sodium were significantly increased by not only 4-OH but also by 4-S. On the other hand, the plasma concentration of antipyrine was significantly decreased by the intravenous bolus coadministration of N-acetyl-p-aminophenyl O-sulfate (APAPS) at steady-state plasma concentration of antipyrine. A similar reduction was not observed with the intravenous coadministration of acetaminophen (APAP). The Kp value of antipyrine was significantly increased in the brain by the coadministration of APAPS, but was not affected by APAP. The increment in the drug distribution to the brain with the concomitant use of 4-OH (or APAPS) observed in this study is useful information for the application of drug combinations as biodistribution promoters.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1672635	4-Hydroxyantipyrine		1672-63-5	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: