| Determination of the stereoselectivity of chiral drug transport across Caco-2 cell monolayers. | |
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MedLine Citation:
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PMID: 16287047 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Ying He; Su Zeng |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Chirality Volume: 18 ISSN: 0899-0042 ISO Abbreviation: Chirality Publication Date: 2006 Jan |
Date Detail:
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Created Date: 2005-12-06 Completed Date: 2006-02-09 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8914261 Medline TA: Chirality Country: United States |
Other Details:
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Languages: eng Pagination: 64-9 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2005 Wiley-Liss, Inc. |
Affiliation:
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College of Pharmaceutical Sciences, Department of Pharmaceutical Analysis and Drug Metabolism, Zhejiang University, Hangzhou, P.R. China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic beta-Antagonists
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pharmacokinetics Biological Transport, Active Caco-2 Cells Cell Membrane Permeability* Humans Pharmaceutical Preparations / metabolism* Propanolamines / isolation & purification, pharmacokinetics Stereoisomerism |
| Chemical | |
Reg. No./Substance:
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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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