Studies on the Biliary Excretion Mechanisms of Drugs. III. Active Transport of Glucuronides into Bile in Rats

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Abstract
Thiamphenicol glucuronide (TPG), chloramphenicol glucuronide (CPG) and phenolphthalein glucuronide (PPG), administered intravenously to rats with ligated renal pedicles, rapidly appear in the bile in high concentrations as the unchanged compounds. Between 4 and 30 min after administration, the bile-to-blood concentration ratios of the glucuronides are 33-122 for TPG, 35-142 for CPG and 6-101 for PPG. Furthermore, the transport process of the glucuronides is saturable and the excretion is depressed by probenecid. The results indicate that TPG, CPG and PPG are excreted into the rat bile by an active transport process.

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