In Vitro Screening Models to Assess Intestinal Drug Absorption and Metabolism

Author(s):  
Sven Deferme ◽  
Pieter Annaert ◽  
Patrick Augustijns
ChemInform ◽  
2010 ◽  
Vol 26 (31) ◽  
pp. no-no
Author(s):  
K. M. HILLGREN ◽  
A. KATO ◽  
R. T. BORCHARDT

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 405 ◽  
Author(s):  
Yunhai Cui ◽  
Stephanie Claus ◽  
David Schnell ◽  
Frank Runge ◽  
Caroline MacLean

The Caco-2 model is a well-accepted in vitro model for the estimation of fraction absorbed in human intestine. Due to the lack of cytochrome P450 3A4 (CYP3A4) activities, Caco-2 model is not suitable for the investigation of intestinal first-pass metabolism. The purpose of this study is to evaluate a new human intestine model, EpiIntestinal microtissues, as a tool for the prediction of oral absorption and metabolism of drugs in human intestine. The activities of relevant drug transporters and drug metabolizing enzymes, including MDR1 P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), CYP3A4, CYP2J2, UDP-glucuronosyltransferases (UGT), carboxylesterases (CES), etc., were detected in functional assays with selective substrates and inhibitors. Compared to Caco-2, EpiIntestinal microtissues proved to be a more holistic model for the investigation of drug absorption and metabolism in human gastrointestinal tract.


2002 ◽  
Vol 17 (5) ◽  
pp. 408-415 ◽  
Author(s):  
Shinji Yamashita ◽  
Emiko Hattori ◽  
Aiko Shimada ◽  
Yoriko Endoh ◽  
Yukako Yamazaki ◽  
...  

1995 ◽  
Vol 15 (2) ◽  
pp. 83-109 ◽  
Author(s):  
Kathleen M. Hillgren ◽  
Akira Kato ◽  
Ronald T. Borchardt

2020 ◽  
Vol 56 ◽  
pp. 101275 ◽  
Author(s):  
Bart Hens ◽  
Makoto Kataoka ◽  
Keisuke Ueda ◽  
Ping Gao ◽  
Yasuhiro Tsume ◽  
...  

1991 ◽  
Vol 42 (12) ◽  
pp. 2259-2264 ◽  
Author(s):  
Caroline J. Alcorn ◽  
Robert J. Simpson ◽  
David Leahy ◽  
Timothy J. Peters

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