Document Detail

Bioavailability of four ursodeoxycholic acid preparations.
MedLine Citation:
PMID:  10971229     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: Ursodeoxycholic acid (UDCA) is the drug of choice for treating primary biliary cirrhosis and dissolving cholesterol gallstones. OBJECTIVES: The objective of this study was to compare the bioavailability of four commercially available ursodeoxycholic acid formulations in standardized doses. METHODS: Twenty-four healthy subjects were studied in groups of four, and received each of the different UDCA preparations in random order, with a 1-week washout or more in-between. Serum UDCA levels were determined for a 6-h period. The mean area under the curve (AUC), Cmax and Tmax were determined for each drug formulation, and the results compared. Dose proportionality was determined using the Canadian Ursofalk tablet using either 250 mg, 500 mg or 750 mg dosing. The intraparticipant variability was assessed by asking each participant to repeat the last drug that they took the second time, 1 week later. RESULTS: The mean AUC was 68.99 micromol/1.6 h-1 for the USA UDCA tablet, 59.34 micromol/1.6 h-1 for the Canadian UDCA tablet, 55.55 micromol/1.6 h-1 for Ursolvan capsules, and 46.66 micromol/1.6 h-1 for Actigall capsules. The mean Cmax values were 24.29, 17.85, 16.63 and 413.32 nmol/mL, respectively. The mean Tmax was 1.82, 2.3, 2.79 and 3.39 h, respectively. Linear aggression analysis assessing the direct proportionality of AUC on the dose for the Canadian UDCA tablet gave an estimate of 0.063 + 0.0164 (standard error, P-value=0.0117), e.g. if the dose increases from 250 mg to 500 mg, the serum ursodeoxycholic acid increases by 250 x 0.063=15.75. There was excellent reproducibility for the AUC for the North American tablets (0.97, 0.88) compared to the two capsules (0.32, 0.15). CONCLUSIONS: The significantly higher AUC and Cmax and shorter Tmax for the Canadian Ursofalk tablets compared to the UDCA capsule preparations supports better bioavailability.
C N Williams; B Al-Knawy; W Blanchard
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Publication Detail:
Type:  Clinical Trial; Comparative Study; Journal Article; Randomized Controlled Trial; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Alimentary pharmacology & therapeutics     Volume:  14     ISSN:  0269-2813     ISO Abbreviation:  Aliment. Pharmacol. Ther.     Publication Date:  2000 Sep 
Date Detail:
Created Date:  2000-10-19     Completed Date:  2000-10-19     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8707234     Medline TA:  Aliment Pharmacol Ther     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1133-9     Citation Subset:  IM    
Division of Gastroenterology, Department of Medicine, Dalhousie University, Halifax, Nova Scotia, Canada.
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MeSH Terms
Administration, Oral
Biological Availability
Chemistry, Pharmaceutical
Cross-Over Studies
Linear Models
Reproducibility of Results
Therapeutic Equivalency
Ursodeoxycholic Acid / blood,  pharmacokinetics*
Reg. No./Substance:
128-13-2/Ursodeoxycholic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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