Document Detail


On the absorption of alendronate in rats.
MedLine Citation:
PMID:  7891304     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Alendronate is an antiosteolytic agent under investigation for the treatment of a number of bone disorders. Since the compound is a zwitterion with five pKa values and is completely ionized in the intestine at the physiological pH, absorption is poor; less than 1% of an oral dose is available systemically in rats. In the present studies, absorption was found to be predominantly in the upper part of the small intestine. Administration of buffered solutions of alendronate (pH 2-11) did not improve absorption. Whereas food markedly impaired the absorption of alendronate, EDTA enhanced absorption in a dose-dependent manner. Pretreatment of rats with ulcerogenic agents, mepirizole, acetylsalicylic acid, or indomethacin, resulted in a 3-7-fold increase in the oral absorption of alendronate. The absorption of phenol red, added as an indicator of intestinal tissue damage, was also increased in rats with experimental peptic ulcers. The enhanced absorption of alendronate observed in rats with experimental peptic ulcers was attributed to the alteration of the integrity of the intestinal membrane.
Authors:
J H Lin; I W Chen; F A deLuna
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  83     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  1994 Dec 
Date Detail:
Created Date:  1995-04-20     Completed Date:  1995-04-20     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1741-6     Citation Subset:  IM    
Affiliation:
Merck Research Laboratories, West Point, Pennsylvania 19486.
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MeSH Terms
Descriptor/Qualifier:
Administration, Oral
Alendronate
Animals
Bone and Bones / metabolism
Carbon Radioisotopes
Digestive System / metabolism
Diphosphonates / blood,  pharmacokinetics*
Edetic Acid / pharmacology
Gastrointestinal Transit / physiology
Glucose / pharmacology
Hydrogen-Ion Concentration
Injections, Intravenous
Intestinal Absorption*
Male
Peptic Ulcer / metabolism
Rats
Rats, Sprague-Dawley
Chemical
Reg. No./Substance:
0/Carbon Radioisotopes; 0/Diphosphonates; 50-99-7/Glucose; 60-00-4/Edetic Acid; 66376-36-1/Alendronate

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


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