1994 Volume 42 Issue Supplement2 Pages 198-205
The metabolism of tazobactam/piperacillin (TAZ/PIPC) in some animals was studied using in vitro and in vitro examinations.
The following results were obtained.
1. After intravenous administration of 14C-TAZ/PIPC or TAZ/14C-PIPC to rats, metabolites were investigated in plasma, urine and bile. M-1 was identified as a metabolite of TAZ having a structure of the β-lactam ring-opening product. In the urine, about 70% of unchanged TAZ, about 17% of M-1, and about 25% of unchanged PIPC were excreted for 24h, and in the bile about 60% of unchanged PIPC was excreted for 24h.
2. Plasma and urinary bioactive metabolites in rats, dogs and monkeys were examined by TLC-bioautography. No bioactive metabolites were detected in any specimens.
3. In vitro, stability of TAZ in mice plasma and tissue homogenate was examined. The metabolite M-1 was produced in plasma, kidney and small intestine homogenates.
