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Bioavailability of four ursodeoxycholic acid preparations.
C N Williams1, B Al-Knawy, W Blanchard
1Division of Gastroenterology, Department of Medicine, Dalhousie University, Halifax, Nova Scotia, Canada. gicnw@qe2-hsc.ns.ca
Alimentary Pharmacology & Therapeutics
|September 6, 2000
Summary
This study compared four ursodeoxycholic acid (UDCA) formulations, finding Canadian Ursofalk tablets demonstrated superior bioavailability. These UDCA tablets offer better absorption than capsule forms for patients.
Area of Science:
- Pharmacokinetics
- Drug formulation analysis
- Gastroenterology
Background:
- Ursodeoxycholic acid (UDCA) is a primary treatment for primary biliary cirrhosis and gallstones.
- Evaluating different UDCA formulations is crucial for optimizing patient outcomes.
Purpose of the Study:
- To compare the bioavailability of four commercially available ursodeoxycholic acid (UDCA) formulations.
- Assess pharmacokinetic differences between tablet and capsule UDCA preparations.
Main Methods:
- Twenty-four healthy subjects received four different UDCA formulations in a randomized crossover design.
- Serum UDCA levels were measured over 6 hours to determine AUC, Cmax, and Tmax.
- Dose proportionality and intra-participant variability were also assessed.
Main Results:
- Canadian Ursofalk tablets showed the highest mean AUC (59.34 micromol/1.6 h-1) and Cmax (17.85 nmol/mL).
- Capsule formulations (Ursolvan, Actigall) exhibited lower AUC and Cmax values.
- North American tablets demonstrated excellent reproducibility (AUC 0.97, 0.88) compared to capsules (0.32, 0.15).
Conclusions:
- Canadian Ursofalk tablets offer significantly better bioavailability than UDCA capsule formulations.
- The findings suggest formulation type impacts ursodeoxycholic acid absorption and efficacy.
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