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Current methodologies used for evaluation of intestinal permeability and absorption.
P V Balimane1, S Chong, R A Morrison
1Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb-Pharmaceutical Research Institute, P.O. Box 4000, F.13-04, Princeton, NJ 08543, USA.
Journal of Pharmacological and Toxicological Methods
|March 29, 2001
Summary
Evaluating drug candidate absorption requires multiple preclinical methods. No single technique accurately predicts human intestinal permeability, necessitating a judicious combination for successful drug discovery.
Area of Science:
- Pharmacology and Drug Discovery
- Preclinical Research Methodologies
Background:
- Drug candidate selection relies heavily on predicting in vivo absorption.
- Accurate prediction of human intestinal permeability is crucial for therapeutic success.
Purpose of the Study:
- To review current techniques for evaluating drug candidate permeability and absorption.
- To highlight the importance of integrating various preclinical methodologies.
Main Methods:
- Discussion of in vitro (tissue/cell culture), in situ, and in vivo preclinical models.
- Analysis of the advantages and disadvantages of each methodology.
Main Results:
- No single preclinical method can accurately predict human intestinal permeability.
- Judicious use of diverse techniques is essential for identifying well-absorbed drug candidates.
Conclusions:
- A multifaceted approach combining various preclinical methods is necessary for reliable prediction of drug absorption.
- Integrating data from multiple techniques enhances the identification of viable drug candidates.