1984 Volume 32 Issue Supplement9 Pages 137-144
AC-1370, a new parenteral cephalosporin derivative, was administered to experimental animals, such as mice, rats, rabbits, dogs and monkeys at a single dose of 50mg/kg.
The plasma concentrations of AC-1370 after single intravenous administration were highest in monkeys, followed by rabbits, dogs, rats and mice, in this order, and the plasma half-lives of AC-1370 were 95.0, 67.2, 47.0, 23.3 and 17.0 minutes, respectively. Those of AC-1370 in mice, rats and dogs were almost comparable to those of cefazolin and longer than cefoperazone, cefotaxime and cefmetazole.
AC-1370 was rapidly distributed into various tissues of mice after intravenous administration and the concentrations were high in the order of those in kidney, plasma, lung, myocardium, spleen and liver. The AC-1370 concentration in kidney was three times higher than that of cefazolin, however, its concentration in liver was about one tenth of that of cefazolin.
Urinary recoveries of AC-1370 in dogs, rabbits and monkeys over a 8 hour period were ranged from 68.3% to 75.9% of the administration dose and biliary recoveries over a 6 hour period were 0.15% in dogs and 0.17% in rabbits. Probenecid had no influence on plasma concentration or urinary recovery of AC-1370, indicating AC-1370 was mainly excreted by glomerular filtration.
The extent of serum protein binding of AC-1370 measured by centrifugal ultrafiltration method were 14.3% in humans, 5.7% in dogs, 8.6% in rabbits and 7.1% in rats. These values weresmaller than those of cefazolin or cefoperazone.
