Abstract
Abstract Prolonged ampicillin blood levels have been attributed to recycling through the biliary system. The present study was undertaken to make specific measurements of the role of inactivation and biliary excretion of penicillin G and ampicillin by the liver with an isolated rat liver preparation. Varying amounts of the drugs were circulated through the rat liver, antibiotic concentrations were measured, and inactivation rates were calculated. Radioactive penicillins were also administered to determine the fate of degradation products. Ampicillin was inactivated only half as rapidly as penicillin G. Small, but equal amounts of each drug were excreted in the bile. Thus, the higher and more prolonged blood levels of ampicillin appear to be due to a lower rate of inactivation by the liver rather than to recycling through the biliary system.
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