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Oral heparin: status review

BioMed Central
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Abstract ral ss BioMed CentThrombosis Journal Open AcceReview Oral heparin: status review Ehud Arbit*, Michael Goldberg, Isabel Gomez-Orellana and Shingai Majuru Address: Emisphere Technologies Inc. 765 Old Saw Mill River Road. Tarrytown, NY 10591, USA Email: Ehud Arbit* - [email protected]; Michael Goldberg - [email protected]; Isabel Gomez- Orellana - [email protected]; Shingai Majuru - [email protected] * Corresponding author Abstract Unfractionated heparin and low molecular weight heparin are the most commonly used antithrombotic and thromboprophylactic agents in hospital practice. Extended out-of-hospital treatment is inconvenient in that these agents must be administered parenterally. Current research is directed at development of a safe and effective oral antithrombotic agent as an alternative for the effective, yet difficult to use vitamin K antagonists. A novel drug delivery technology that facilitates transport of drugs across the gastrointestinal epithelium has been harnessed to develop an oral dosage form of unfractionated heparin. Combining unfractionated heparin with the carrier molecule, sodium N-(8 [2-hydroxybenzoyl]amino) caprylate, or SNAC has markedly increased the gastrointestinal absorption of this drug. Preclinical and clinical studies to-date suggests that oral heparin-SNAC can confer a clinical efficacious effect; further confirmation is sought in planned clinical trials. Introduction The current use of anticoagulants is extensive and it is esti- mated that 0.7% of the population in the Western world receive these drugs [1]. Broader indications for anticoagu- lants and their increased use in the outpatient settings as well as for long-term dosing has stimulated renewed inter- est in developing oral anticoagulant and antithrombotic agents. At present, the cornerstone of oral anticoagulants are the vitamin K antagonists, of which the coumarin derivative warfarin, (Coumadin) is the most widely used. It has been used clinically

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