title: Ursodeoxycholic acid complexation with 2-hydroxypropyl-beta-cyclodextrin increases ursodeoxycholic acid biliary excretion after single oral administration in rats.
abstract: Complexation of ursodeoxycholic acid (UDCA) with 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) improves the water solubility and the dissolution rate of UDCA and may therefore increase its bioavailability. We compared the amount and the rate of biliary excretion of UDCA and biliary lipid secretion after a single oral administration of UDCA in 3 different pharmaceutical formulations [UDCA-HPbetaCD ('urso-beta-cyclodextrin'), UDCA suspension and UDCA capsule] at 3 different dosages each, in 11 groups (2 control groups) of bile fistula rats. UDCA excretion increased with an increase in dose, biliary UDCA recovery and peak secretion were significantly higher after administration of UDCA-HPbetaCD than after UDCA in suspension or capsule. This enhancement of biliary excretion may achieve greater UDCA enrichment in the bile acid pool than conventional pharmaceutical UDCA formulations, this giving to UDCA-HPbetaCD a considerable therapeutical potential.
authors.affiliation: Chair of Geriatrics and Gerontology, Department of Internal Medicine, University of Modena, Modena, Italy. paaloven@unimo.it
authors.forename: P
authors.initials: P
authors.lastname: Ventura
authors.forename: R
authors.initials: R
authors.lastname: Panini
authors.forename: G
authors.initials: G
authors.lastname: Montosi
authors.forename: C
authors.initials: C
authors.lastname: Garuti
authors.forename: M
authors.initials: M
authors.lastname: Vandelli
authors.forename: G
authors.initials: G
authors.lastname: Brunetti
authors.forename: H
authors.initials: H
authors.lastname: Tauschel
authors.forename: A
authors.initials: A
authors.lastname: Pietrangelo
authors.forename: G
authors.initials: G
authors.lastname: Salvioli
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism*; D001658:Biliary Fistula; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000493:pharmacokinetics*; D004338:Drug Combinations; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D014580:Ursodeoxycholic Acid / Q000493:pharmacokinetics*; D047392:beta-Cyclodextrins
chemical_list: D003505:Cyclodextrins; D004338:Drug Combinations; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D014580:Ursodeoxycholic Acid