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Biliary excretion, metabolism and enterohepatic circulation of buprenorphine.

Authors
  • Brewster, D
  • Humphrey, M J
  • McLeavy, M A
Type
Published Article
Journal
Xenobiotica; the fate of foreign compounds in biological systems
Publication Date
Mar 01, 1981
Volume
11
Issue
3
Pages
189–196
Identifiers
PMID: 7293215
Source
Medline
License
Unknown

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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