title: Pharmacokinetics of ursodeoxycholic acid in rat.
abstract: The pharmacokinetic behaviour and metabolism of ursodeoxycholic acid (UDCA) have been studied in the rat. After oral administration of both 3H-labelled (4 muCi/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 3 alpha,6 alpha, 7 beta-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.
authors.affiliation: Istituto di Chimica Analitica, Università di Messina, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Roda
authors.forename: P
authors.initials: P
authors.lastname: Hrelia
authors.forename: M
authors.initials: M
authors.lastname: Paolini
authors.forename: M
authors.initials: M
authors.lastname: Calzolari
authors.forename: B
authors.initials: B
authors.lastname: Grigolo
authors.forename: P
authors.initials: P
authors.lastname: Simoni
authors.forename: R
authors.initials: R
authors.lastname: Aldini
authors.forename: G C
authors.initials: GC
authors.lastname: Forti
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D005243:Feces / Q000737:chemistry; D005260:Female; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D014580:Ursodeoxycholic Acid / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
chemical_list: D014580:Ursodeoxycholic Acid