Document Detail


Transepithelial transport of bepridil in the human intestinal cell line, Caco-2, using a "dynamic model".
MedLine Citation:
PMID:  12877575     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The purpose of the study was to go further into the transepithetial transport of bepridil, an anticalcic agent, through monolayer cells Caco-2, using a "dynamic model" including a transfer of inserts with Caco-2 cells into new wells, free of drug, at regular intervals, in order to simulate the blood flux. The state of cells was evaluated by measuring the transepithelial electrical resistance and the transport of bepridil was followed using a gas chromatography/mass spectrometry determination. This study exhibits the importance of the basolateral renewal both on the transport of bepridil and the maintenance of cells in a satisfactory state. Two elimination phases from the cell compartment seem to occur, with basolateral half lives respectively of 12.2 and 25.6 hours, probably linked with two kinds of cellular binding sites. This dynamic model permits the reflection and simulation of the slowness of the in vivo absorption of bepridil in the small intestine.
Authors:
F Mathieu; M J Galmier; A Nicolay; J F Pognat; C Lartigue
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of drug metabolism and pharmacokinetics     Volume:  28     ISSN:  0378-7966     ISO Abbreviation:  Eur J Drug Metab Pharmacokinet     Publication Date:    2003 Apr-Jun
Date Detail:
Created Date:  2003-07-24     Completed Date:  2004-03-23     Revised Date:  2011-02-02    
Medline Journal Info:
Nlm Unique ID:  7608491     Medline TA:  Eur J Drug Metab Pharmacokinet     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  155-60     Citation Subset:  IM    
Affiliation:
UMR INSERM 484, Laboratoire de Chimie Analytique et Spectrométrie de Masse, Faculté de Pharmacie, Clermont-Ferrand, France.
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MeSH Terms
Descriptor/Qualifier:
Bepridil / pharmacokinetics*
Biological Transport / physiology
Caco-2 Cells
Epithelial Cells / metabolism
Humans
Intestinal Mucosa / metabolism*
Models, Biological*
Models, Chemical*
Chemical
Reg. No./Substance:
64706-54-3/Bepridil

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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