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Updated: Jul 10, 2026
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In Vitro and In Vivo Approaches to Determine Intestinal Epithelial Cell Permeability
Published on: October 19, 2018
Intestinal permeability and its relevance for absorption and elimination
1Biopharmaceutics, Uppsala University, Uppsala, Sweden. hans.lennernas@farmaci.uu.se
Xenobiotica; the Fate of Foreign Compounds in Biological Systems
|October 31, 2007
Summary
Human jejunal permeability (Peff) is key for predicting oral drug absorption. Drugs with high jejunal Peff (> 1.5 x 10(-4) cm s(-1)) are fully absorbed, regardless of transport mechanism.
Area of Science:
- Pharmacokinetics and Drug Absorption
- Gastrointestinal Physiology
Background:
- Human jejunal permeability (Peff) is crucial as this region has high carrier protein expression and surface area.
- Intestinal drug absorption involves multiple parallel transport processes, making site-specific permeability essential for accurate predictions.
Purpose of the Study:
- To determine human jejunal permeability (Peff) and its correlation with oral drug absorption.
- To evaluate the predictive value of jejunal Peff for different drug transport mechanisms and physicochemical properties.
Main Methods:
- Determination of site-specific jejunal effective permeability (Peff) in humans.
- Analysis of drug absorption based on jejunal Peff values and known transport mechanisms (passive diffusion, carrier-mediated transport).
Main Results:
- Drugs with jejunal Peff > 1.5 x 10(-4) cm s(-1) demonstrate complete absorption.
- Jejunal Peff accurately predicts absorption for drugs utilizing absorptive carriers like peptide and amino acid transporters.
- The human intestinal epithelium exhibits high resistance to large, hydrophilic compounds; the paracellular route is minor for molecules > 200 Da.
Conclusions:
- Jejunal permeability is a valuable predictor of oral drug absorption fraction.
- Further in vivo studies and advanced perfusion techniques are needed for distal gastrointestinal tract analysis.
- Development of complex in vitro models and physiologically based pharmacokinetic modeling will enhance oral drug absorption predictions.
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