In vivo pharmacokinetics of pyribenzoxim in rats.

Abstract

Pyribenzoxim, benzophenone O-[2,6-bis(4,6-dimethoxypyrimidin-2-yloxy)benzoyl]oxime, is a new post-emergence herbicide providing broad-spectrum weed control in rice fields. [14C]Pyribenzoxim was used to study the pharmacokinetics of the compound after oral administration of a dose of 1000 mg kg-1 to male Sprague-Dawley rats. The material balance ranged from 97.3 to 99.7% of the administered dose and urinary and fecal recovery accounted for 97.1%, with the majority of radioactivity recovered in feces (88.6%) by 168 h after treatment. Elimination as volatile products or as carbon dioxide was negligible. The following values were obtained for the compound in the blood: AUC0-168 h, 28,400 micrograms equiv hg-1; Tmax, 12 h; Cmax, 372 micrograms equiv g-1; half-life, 53 h. Radioactivity in tissue decreased from 96.1% of applied radiocarbon at 6 h to 0.4% at 168 h and the highest concentration of radioactivity among the tissues was observed in liver while the lowest residues were found in brain. The elimination half-lives of radioactivity from tissues was in the range of 7 to 77 h and Tmax values of 12, 24 and 12 h were observed for blood, liver and kidney, respectively. Except for that in the digestive tract, the tissue-to-blood ratio (TBR) was highest in the liver.