Predicting human intestinal absorption in the presence of bile salt with micellar liquid chromatography

Understanding intestinal absorption for pharmaceutical compounds is vital to estimate the bioavailability and therefore the in vivo potential of a drug. This study considers the application of micellar liquid chromatography (MLC) to predict passive intestinal absorption with a selection of model com...

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Bibliographic Details
Published in:Biomedical chromatography 2016-10, Vol.30 (10), p.1618-1624
Main Authors: Waters, Laura J., Shokry, Dina S., Parkes, Gareth M.B.
Format: Article
Language:English
Subjects:
Bile Acids and Salts - metabolism
bile salts
chromatography
Chromatography, Liquid - methods
Humans
Intestinal Absorption
micellar
Micelles
MLC
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Summary:Understanding intestinal absorption for pharmaceutical compounds is vital to estimate the bioavailability and therefore the in vivo potential of a drug. This study considers the application of micellar liquid chromatography (MLC) to predict passive intestinal absorption with a selection of model compounds. MLC is already known to aid prediction of absorption using simple surfactant systems; however, with this study the focus was on the presence of a more complex, bile salt surfactant, as would be encountered in the in vivo environment. As a result, MLC using a specific bile salt has been confirmed as an ideal in vitro system to predict the intestinal permeability for a wide range of drugs, through the development of a quantitative partition–absorption relationship. MLC offers many benefits including environmental, economic, time‐saving and ethical advantages compared with the traditional techniques employed to obtain passive intestinal absorption values. Copyright © 2016 John Wiley & Sons, Ltd.
ISSN:0269-3879
1099-0801
DOI:10.1002/bmc.3731