1984 Volume 32 Issue Supplement2 Pages 119-132
In experimental animals, distribution and excretion of TA-058 to the body fluids and various tissues were compared with those of reference penicillins. TA-058 was intravenously or intramuscularly admistered to mice, rats, rabbits and dogs in single doses ranging 20 to 100mg/kg.
The serum levels of TA-058 were higher than those of carbenicillin, ampicillin and piperacillin and persisted much longer than the reference penicillins in the above experimental animals. The biological half lives of TA-058 were 0.59, 0.96 and 0.99 hr for rats (i.v.), dogs (i.v.) and dogs (d.i.), respectively, at doses of 20mg/kg. In mice, TA-058 was distributed in high concentrations to various tissues in the descending order of the liver, kidney and lung. In rats, the following order was observed; kidney>liver>lung.
TA-058 was excreted mainly in the urine of rat, rabbit and dog within 5 to 24 hrs. after the administration. The biliary excretions of TA-058 were 18.8 and 13.6% within 24 hrs for rats and rabbits, respectively. These rates were lower than those of piperacillin.
TA-058 was stable in the body fluids and tissues in a cold or in a frozen state and no active metabolite except TA-058 was observed in these biological samples.
