Document Detail

Ursodeoxycholic acid complexation with 2-hydroxypropyl-beta-cyclodextrin increases ursodeoxycholic acid biliary excretion after single oral administration in rats.
MedLine Citation:
PMID:  11174081     Owner:  NLM     Status:  MEDLINE    
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.
P Ventura; R Panini; G Montosi; C Garuti; M Vandelli; G Brunetti; H Tauschel; A Pietrangelo; G Salvioli
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Pharmacology     Volume:  62     ISSN:  0031-7012     ISO Abbreviation:  Pharmacology     Publication Date:  2001 Feb 
Date Detail:
Created Date:  2001-02-22     Completed Date:  2001-05-31     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0152016     Medline TA:  Pharmacology     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  107-12     Citation Subset:  IM    
Copyright Information:
Copyright 2001 S. Karger AG, Basel.
Chair of Geriatrics and Gerontology, Department of Internal Medicine, University of Modena, Modena, Italy.
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MeSH Terms
Administration, Oral
Bile / metabolism*,  secretion
Biliary Fistula
Biological Availability
Chemistry, Pharmaceutical
Cyclodextrins / pharmacokinetics*
Drug Combinations
Rats, Sprague-Dawley
Ursodeoxycholic Acid / pharmacokinetics*
Reg. No./Substance:
0/Cyclodextrins; 0/Drug Combinations; 0/beta-Cyclodextrins; 128-13-2/Ursodeoxycholic Acid; 94035-02-6/2-hydroxypropyl-beta-cyclodextrin

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