Pharmacokinetics of ursodeoxycholic acid in rat

Aldo Roda, Patrizia Hrelia, Moreno Paolini, Miller Calzolari, Brunella Grigolo, Patrizia Simoni, Rita Aldini, Giorgio Cantelli Forti

Research output: Contribution to journalArticlepeer-review

Abstract

The pharmacokinetic behaviour and metabolism of ursodeoxycholic acid (UDCA) have been studied in the rat. After oral administration of both 3H-labelled (4 μCi/kg body wt) and unlabelled (20 mg) UDCA, UDCA appeared in serum almost entirely in conjugated form (taurine conjugated); UDCA was present in bile mostly as taurine conjugated; the more relevant metabolite is 3α,6α,7β-trihydroxycholanoic acid which represents 10% of the total bile acid pool. UDCA increased bile flow and selectively decreased biliary cholesterol secretion, while phospholipid secretion was unaffected. Faecal UDCA excretion was 15-20% while the urinary extraction was 1.5% during 24 h. The data show that UDCA, when administered in high dose, is promptly secreted into bile almost entirely metabolized to tauroursodeoxycholic acid, where it (1) desaturates the cholesterol in bile, (2) exerts choleretic properties.

Original languageEnglish
Pages (from-to)327-335
Number of pages9
JournalPharmacological Research
Volume23
Issue number4
DOIs
Publication statusPublished - 1991

Keywords

  • bile acids
  • gallstone dissolution
  • ursodeoxycholic acid

ASJC Scopus subject areas

  • Pharmacology

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