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Bioavailability study of a new, sinking, enteric-coated ursodeoxycholic acid formulation
Pharmacological Research
|February 1, 1995
Summary
A novel sinking enteric-coated ursodeoxycholic acid (UDCA) formulation significantly enhances drug absorption compared to conventional or floating capsules. This improved bioavailability is linked to targeted release in the alkaline intestinal environment.
Area of Science:
- Pharmacology
- Gastroenterology
- Drug Delivery Systems
Background:
- Ursodeoxycholic acid (UDCA) is a key therapeutic agent.
- Optimizing UDCA oral bioavailability is crucial for treatment efficacy.
- Existing formulations may face challenges with gastric residence and pH-dependent release.
Purpose of the Study:
- To develop and evaluate a new enteric-coated UDCA formulation designed to sink in the stomach.
- To compare the pharmacokinetic profile of this sinking formulation against conventional and floating enteric-coated UDCA formulations.
- To elucidate the impact of gastric residence and intestinal pH on UDCA absorption.
Main Methods:
- Development of an enteric-coated UDCA tablet designed for gastric sinking.
- Pharmacokinetic study in 12 healthy subjects after a single 450 mg oral dose.
- Comparison of three UDCA formulations: sinking enteric-coated tablet, floating enteric-coated capsule, and conventional capsule.
- Serum UDCA levels measured using enzyme immunoassay, analyzing Area Under the Curve (AUC) and maximum concentration (Cmax).
Main Results:
- The sinking enteric-coated UDCA formulation demonstrated a significantly higher Area Under the Curve (AUC) (39.0 ± 8.5) compared to conventional (30.5 ± 4.9) and floating (29.3 ± 3.4) formulations.
- Maximum UDCA serum concentration (Cmax) was significantly higher with the sinking formulation.
- The time to maximum UDCA serum concentration (tmax) was delayed with the sinking formulation, suggesting later intestinal release.
Conclusions:
- The sinking enteric-coated UDCA tablet formulation enhances drug absorption due to targeted release in the alkaline intestinal environment.
- This formulation overcomes limitations of early intestinal release in acidic conditions, improving UDCA bioavailability.
- The findings support the hypothesis that optimized gastric behavior and intestinal release profiles are critical for ursodeoxycholic acid absorption.