Biliary excretion of ampicillin, metampicillin and carbenicillin

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Abstract
The biliary excretion of three β-lactam derivatives (ampicillin, metampicillin, carbenicillin) was studied: (1) in the isolated rabbit liver using an experimental perfusion system; (2) in the duodenal juice collected through duodenal tubing of normal subjects; (3) in the bile obtained by T-tube drainage in cholecystectomized patients. The three compounds are partially excreted in the bile. Biliary concentrations in isolated rabbit liver perfusions amounted to4.1 % (ampicillin), 46.5 % (metampicillin) and 1.8 % (carbenicillin) of the administered dose. In man, the duodenal tubing technique also demonstrated high bile recovery of metampicillin (5.8% of the administered dose). The assays performed in patients with T-tube drainage showed that the antibiotic activity levels in the bile after administration of these three β-lactamines exceeded the minimum inhibitory concentrations of the pathogens included in their antibacterial spectra for several hours; under these conditions, the highest biliary excretion (8.3 % of the administered dose) is also achieved with metampicillin administered intravenously.

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