1994 Volume 42 Issue Supplement4 Pages 268-276
The pharmacokinetics of biapenem (BIPM), a new parenteral antibiotic, were studied in dogs and monkeys.
Plasma concentration of radioactivity after single administration of rhiciB.Irm (10mg/kg) decreased in the biexponential pattern, of which T1/2α in dogs and monkeys were 0.6 and 0.54 hours, respectively.
Lower Cmax values following the continuous infusion were observed at the end of infusion compared with the bolus injection. No significant difference was observed in AUC and T1/2 terminal following the continuous infusion compared with the bolus injection.
Regardless of the dosing repetition, no significant difference was observed in plasma concentration of BIPM. No significant difference was shown in AUC and T1/2 terminal following the 7th injection as compared with those following the 1st one.
Over 90% of radioactivity was excreted in the urine during 48 hours post dose of [14C] BIPM in dogs and monkeys. Only trace amounts of radioactivity (0.4-0.5% of dose) were found in feces of each species.
The amount of metabolites after administration of [14C] BIPM was small, and two major metabolites were detected in dog plasma and urine.
Pharmacokinetic parameters of infant dogs were different from those of mature dogs, especially that the distribution volume of BIPM was larger in infant dogs. These results were presumed to reflect the different volume of the extracellular fluid in the whole body.
In renal dysfunction dogs, the decreasing rate of the plasma concentration of BIPM was delayed in parallel with lowering of creatinine clearance (Ccr).
