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Bile salts and their importance for drug absorption
René Holm1, Anette Müllertz, Huiling Mu
1Biologics and Pharmaceutical Science, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark. rhol@lundbeck.com
International Journal of Pharmaceutics
|April 20, 2013
Summary
Bile salts in the gastro-intestinal tract generally enhance drug bioavailability across various formulations. This review covers bile salt properties, species variations, and their impact on drug performance.
Area of Science:
- Pharmacology
- Biochemistry
- Drug Delivery
Background:
- Bile salts are endogenous compounds crucial for digestion and are present in humans and animals used in pharmaceutical development.
- Understanding bile salt properties is essential for optimizing drug absorption and formulation strategies.
Purpose of the Study:
- To review the physicochemical properties of bile salts.
- To describe bile concentration and composition across different animal species.
- To summarize the literature on bile salt influence on in vivo drug performance and formulation efficacy.
Main Methods:
- Literature review of scientific publications.
- Analysis of physicochemical properties of bile salts.
- Comparative assessment of bile composition in various animal models.
- Synthesis of data on drug bioavailability with and without bile salt influence.
Main Results:
- Bile salts exhibit diverse physicochemical properties influencing drug interactions.
- Significant variations in bile concentration and composition exist among different animal species.
- The presence of bile in the gastro-intestinal tract generally improves drug bioavailability.
- This positive effect is observed across various drug formulation types, including suspensions, solutions, cyclodextrin complexes, and lipid-based formulations.
Conclusions:
- Bile salts play a significant role in enhancing drug bioavailability in vivo.
- Formulation strategies should consider the presence and properties of bile salts for improved drug delivery.
- While generally beneficial, specific exceptions to enhanced bioavailability warrant further investigation.
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