Document Detail


Inhibition of intestinal absorption of cholesterol by surface-modified nanostructured aluminosilicate compounds.
MedLine Citation:
PMID:  19090562     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The aim of this work was to assess the ability of aqueous suspensions of surface-modified nanostructured aluminosilicate (NSAS) compounds to reduce the intestinal absorption of cholesterol in a rat model. The rats were divided into 10 treatment groups which included several NSAS compounds at various doses, ezetimibe at 10 mg/kg, stigmastanol at 50 mg/kg, and normal saline. All compounds and controls were independently administered by oral gavage and then a mixture of [(3)H]cholesterol and cold cholesterol in 10% Intralipid(R) was immediately administered orally to the animals. Systemic blood was sampled and the concentration of cholesterol in plasma was determined by means of radioactivity. Protonation of NSAS using an ion-exchange column resulted in significant inhibition of cholesterol absorption relative to the control group (31.5% and 38.6% reduction in absorption of cholesterol for 50 and 100 mg/kg doses, respectively). Other surface-ion modifications of NSAS compounds did not show significant effect on intestinal cholesterol absorption. The inhibition of cholesterol absorption by ezetimibe was superior and by stigmastanol was equal to the effect of protonated NSAS in the doses investigated in this study. In conclusion, protonated NSAS material seems to inhibit significantly the intestinal absorption of dietary cholesterol in a rat model.
Authors:
Pavel Gershkovich; Jerry Darlington; Olena Sivak; Panayiotis P Constantinides; Kishor M Wasan
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  98     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-02     Completed Date:  2009-08-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2390-400     Citation Subset:  IM    
Affiliation:
Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, British Columbia, Canada. pgershko@interchange.ubc.ca
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MeSH Terms
Descriptor/Qualifier:
Aluminum Silicates / chemistry*,  pharmacology*
Animals
Anticholesteremic Agents / pharmacology
Azetidines / pharmacology
Cholesterol / blood,  metabolism*
Intestinal Absorption / drug effects*
Male
Nanostructures / chemistry
Particle Size
Protons
Rats
Rats, Sprague-Dawley
Sitosterols / pharmacology
Surface Properties
Viscosity
Chemical
Reg. No./Substance:
0/Aluminum Silicates; 0/Anticholesteremic Agents; 0/Azetidines; 0/Protons; 0/Sitosterols; 163222-33-1/ezetimibe; 57-88-5/Cholesterol; 83-45-4/stigmastanol

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


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