Document Detail

Acylated non-alpha-amino acids as novel agents for the oral delivery of heparin sodium, USP.
MedLine Citation:
PMID:  9685871     Owner:  NLM     Status:  MEDLINE    
Ten N-acylated, non-alpha-amino acids have been prepared as oral delivery agents and used to demonstrate the oral delivery of heparin in vivo in rats and primates. Following the oral administration of solutions containing a combination of heparin and a delivery agent to rats or primates, significant plasma heparin concentrations were evidenced by APTT and anti-Factor Xa assays. The estimated pharmacodynamic equivalence for an oral dosing solution containing heparin and a delivery agent is 39% in primates. In vitro experiments based on heparin affinity chromatography or heparin/methylene blue complexation were also performed to begin investigation of the mechanism by which these compounds facilitate heparin oral delivery. Results of in vitro studies suggest that absorption of the drug across the gastrointestinal membrane is the result of a non-covalent interaction between heparin and the delivery agent.
A Leone-Bay; D R Paton; B Variano; H Leipold; T Rivera; J Miura-Fraboni; R A Baughman; N Santiago
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  50     ISSN:  0168-3659     ISO Abbreviation:  J Control Release     Publication Date:  1998 Jan 
Date Detail:
Created Date:  1998-08-13     Completed Date:  1998-08-13     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  41-9     Citation Subset:  IM    
Emisphere Technologies, Inc., Hawthorne, New York 10532, USA.
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MeSH Terms
Administration, Oral
Amino Acids / administration & dosage*
Anticoagulants / administration & dosage*
Chromatography, Affinity
Drug Delivery Systems*
Heparin / administration & dosage*,  pharmacokinetics
Intestinal Absorption
Macaca fascicularis
Partial Thromboplastin Time
Rats, Sprague-Dawley
Reg. No./Substance:
0/Amino Acids; 0/Anticoagulants; 9005-49-6/Heparin

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

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