Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin

Journal of Medicinal Chemistry
A Leone-BayR A Baughman

Abstract

A family of novel compounds (delivery agents) that promote the gastrointestinal absorption of USP heparin in rats and primates has been discovered. The delivery agents in combination with heparin were administered either orally or intracolonically in an aqueous propylene glycol solution and caused dramatic increases in both plasma heparin concentrations (anti-Factor Xa) and clotting times (APTT). Using one of the most effective delivery agents in this series, an estimated relative bioavailability of 8% can be achieved following oral administration to cynomolgus monkeys. To establish a correlation between the in vivo data and an in vitro parameter, immobilized artificial membrane (IAM) chromatography was performed. Log relative k' values were correlated to the efficiency of oral heparin delivery.

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Citations

Mar 21, 2000·Medicinal Research Reviews·A Leone-BayJ J Weidner
Feb 14, 2002·Biopolymers·Ruel Z B DesameroJohn E Smart
Feb 14, 2002·Biopolymers·Ruel Z B DesameroJohn E Smart
Mar 12, 2002·Archives of Pharmacal Research·So Yean ChoYeong Shik Kim
Jan 16, 2004·Archives of Pharmacal Research·So Yean ChoYeong Shik Kim
Sep 12, 2007·Pharmaceutical Research·Adam W G Alani, Joseph R Robinson
Nov 26, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·A Bernkop-SchnürchD Guggi
Nov 24, 2001·Advanced Drug Delivery Reviews·M ThanouH E Junginger
Mar 7, 2002·International Journal of Pharmaceutics·Libo YangJoseph A Fix
Dec 16, 2000·Pharmaceutical Science & Technology Today·T Geetha, S Singh
Jul 22, 2004·Journal of Biomaterials Science. Polymer Edition·Liang DongPat Wong
Mar 29, 2005·Journal of Pharmaceutical Sciences·Thierry SchmitzAndreas Bernkop-Schnürch
Feb 3, 2011·Medicinal Research Reviews·Rishi PaliwalSuresh P Vyas
Sep 5, 2006·International Journal of Pharmaceutics·V Grabovac, A Bernkop-Schnürch
Jun 21, 2016·Advanced Drug Delivery Reviews·Sam MaherDavid J Brayden
Mar 29, 2000·Journal of Pharmaceutical Sciences·B J Aungst
Mar 17, 2006·Journal of Medicinal Chemistry·Katri H RaitioTapio Nevalainen
Sep 23, 2000·Journal of Medicinal Chemistry·A Leone-BayR A Baughman

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