Document Detail


Apricot extract inhibits the P-gp-mediated efflux of talinolol.
MedLine Citation:
PMID:  12434397     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Within the framework of developing strategies to enhance the intestinal absorption of P-glycoprotein (P-gp) substrates, the modulatory effect of a standardized apricot extract on P-gp-related efflux carriers was investigated in the Caco-2 system, Ussing chambers and the rat in situ perfusion model using talinolol as a model substrate. Using the Caco-2 system, polarity in transport of talinolol could be observed, the absorptive transport being much lower than the secretory transport (P(app-abs) = 1.08 +/- 0.29 x 10(-6) cm/s and P(app-secr) = 11.74 +/- 0.80 x 10(-6) cm/s). Inclusion of apricot extract (1%) in the apical medium resulted in a statistically significantly diminished polarity (P(app-abs) = 4.88 +/- 0.96 x 10(-6) cm/s and P(app-secr) = 9.39 +/- 0.58 x 10(-6) cm/s, p < 0.05). In addition, the inhibitory effect of apricot extract on P-gp related efflux mechanisms was shown to be concentration (0% approximately 0.1% < 0.3% < 1%) and pH dependent. Experiments performed with the Ussing chambers resulted in similar observations. In the rat in situ perfusion model, inclusion of apricot extract (1%) in the perfusion medium resulted in a threefold increase of the amount of talinolol appearing in the collected blood compared to the reference condition (23.6 +/- 5.53 pmol/cm. min and 7.13 +/- 1.08 pmol/cm. min, respectively; p < 0.05). Coadministration of this standardized apricot extract might be a safe and useful strategy to enhance the intestinal absorption of P-gp substrates. The nature and structure of the compound(s) responsible for this inhibiting effect on P-gp-related efflux carriers remain to be elucidated, as well as the exact mechanism by which apricot extract exerts its inhibitory function.
Authors:
Sven Deferme; Raf Mols; Willy Van Driessche; Patrick Augustijns
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  91     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  2002 Dec 
Date Detail:
Created Date:  2002-11-15     Completed Date:  2003-05-19     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2539-48     Citation Subset:  IM    
Copyright Information:
Copyright 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:2539-2548, 2002
Affiliation:
Laboratory for Pharmacotechnology and Biopharmacy, Herestraat 49, Gasthuisberg, 3000 Leuven, Belgium.
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MeSH Terms
Descriptor/Qualifier:
Animals
Caco-2 Cells / drug effects,  metabolism
Humans
Intestinal Absorption / drug effects,  physiology
Male
P-Glycoprotein / antagonists & inhibitors*,  physiology*
Plant Extracts / pharmacokinetics,  pharmacology*
Propanolamines / antagonists & inhibitors,  pharmacokinetics*
Prunus*
Rats
Rats, Wistar
Chemical
Reg. No./Substance:
0/P-Glycoprotein; 0/Plant Extracts; 0/Propanolamines; 38649-73-9/talinolol

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


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