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Taylor & Francis

Xenobiotica. 1981 Mar;11(3):189-96. doi: 10.3109/00498258109045291.

Biliary excretion, metabolism and enterohepatic circulation of buprenorphine.

Xenobiotica; the fate of foreign compounds in biological systems

D Brewster, M J Humphrey, M A McLeavy

PMID: 7293215 DOI: 10.3109/00498258109045291

Abstract

1. After intramuscular administration of [3H]buprenorphine to rats, dogs, rhesus monkeys and one human volunteer, most of the dosed radioactivity was excreted in the faeces, indicating biliary excretion and a possible enterohepatic circulation of the drug in these species. 2. After intravenous administration of [3H]buprenorphine (100 microgram/kg) to bile-duct cannulated rats, over 90% of the administered radioactivity was excreted in bile within 48 h after dosing. 3. The major drug-related component in rat bile was buprenorphine glucuronide. N-Dealkylated buprenorphine (again conjugated) was also present and a sex difference in the extent of N-dealkylation was apparent. 4. Intraduodenal infusion of rats with bile from rats dosed with [3H]buprenorphine produced a slow, although extensive, excretion of drug-related material in the bile of the recipient animals.

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