Document Detail

Determination of the stereoselectivity of chiral drug transport across Caco-2 cell monolayers.
MedLine Citation:
PMID:  16287047     Owner:  NLM     Status:  MEDLINE    
This study aimed to determine the transport characteristics of chiral drug enantiomers across Caco-2 cell monolayers as a model of human intestinal epithelial membrane. Esmolol was chosen as a model drug, and the study focused on the transepithelial transport of esmolol enantiomers in this in vitro model system. Separation and quantitation of (S)- and (R)-esmolol were performed by RP-HPLC with the use of GITC as a precolumn derivatizing agent. Bidirectional transport studies of 5.0-400.0 micromol/l esmolol demonstrated that the two enantiomers were transported mainly by a passive, transcellular mechanism. At concentrations of 5.0-100.0 micromol/l, enantioselective permeability of esmolol was observed. In the absorptive transport, Papp of (S)-esmolol was smaller than (R)-esmolol and vice versa for secretory transport. The enantioselectivity disappeared when the drug concentration was increased to 200.0 micromol/l. In conclusion, the transport characteristics of (S)- and (R)-esmolol were distinctly different. An enantioselective carrier-mediated mechanism in addition to passive diffusion was involved in the transport process of esmolol across Caco-2 cell monolayers.
Ying He; Su Zeng
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Chirality     Volume:  18     ISSN:  0899-0042     ISO Abbreviation:  Chirality     Publication Date:  2006 Jan 
Date Detail:
Created Date:  2005-12-06     Completed Date:  2006-02-09     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8914261     Medline TA:  Chirality     Country:  United States    
Other Details:
Languages:  eng     Pagination:  64-9     Citation Subset:  IM    
Copyright Information:
Copyright (c) 2005 Wiley-Liss, Inc.
College of Pharmaceutical Sciences, Department of Pharmaceutical Analysis and Drug Metabolism, Zhejiang University, Hangzhou, P.R. China.
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MeSH Terms
Adrenergic beta-Antagonists / pharmacokinetics
Biological Transport, Active
Caco-2 Cells
Cell Membrane Permeability*
Pharmaceutical Preparations / metabolism*
Propanolamines / isolation & purification,  pharmacokinetics
Reg. No./Substance:
0/Adrenergic beta-Antagonists; 0/Pharmaceutical Preparations; 0/Propanolamines; 84057-94-3/esmolol

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

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