Current methodologies used for evaluation of intestinal permeability and absorption.
This review article will focus on the various techniques that are currently employed by drug discovery scientists in evaluating permeability/absorption of drug candidates during the drug candidate selection process. Various preclinical methodologies are available; each having advantages and disadvantages, but it is the judicious use of these techniques that can help identify drug candidates that will be well absorbed in humans. It is well recognized that the human intestinal permeability cannot be accurately predicted based on a single methodology (in vitro: tissue/cell culture, in situ, or in vivo).
Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb-Pharmaceutical Research Institute, P.O. Box 4000, F.13-04, Princeton, NJ 08543, USA.
P V
PV
Balimane
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S
Chong
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Morrison
D000818:Animals; D002460:Cell Line; D002845:Chromatography; D006801:Humans; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000033:anatomy & histology / Q000378:metabolism; D010539:Permeability; D021281:Quantitative Structure-Activity Relationship; D012995:Solubility