Oral heparin: Status review

被引:57
作者
Arbit E. [1 ]
Goldberg M. [1 ]
Gomez-Orellana I. [1 ]
Majuru S. [1 ]
机构
[1] Emisphere Technologies Inc., Tarrytown, NY 10591
关键词
Enoxaparin; Tissue Factor Pathway Inhibitor; Solid Dosage Form; Oral Dosage Form; Oral Direct Thrombin Inhibitor;
D O I
10.1186/1477-9560-4-6
中图分类号
学科分类号
摘要
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. © 2006 Arbit et al; licensee BioMed Central Ltd.
引用
收藏
相关论文
共 72 条
[1]  
Gustafsson D., Bylund R., Antonsson T., Nilsson I., Nystrom J.E., Eriksson U., Bredberg U., Teger-Nilsson A.C., A new oral anticoagulant: The 50-year challenge, Nat Rev Drug Discov, 3, pp. 649-659, (2004)
[2]  
Kearon C., Natural history of venous thromboembolism, Circulation, 107, pp. 122-130, (2003)
[3]  
Agnelli G., Prandoni P., Santamaria M.G., Bagatella P., Iorio A., Bazzan M., Moia M., Guazzaloca G., Bertoldi A., Tomasi C., Gianluigi S., Ascani A., Villalta S., Frulla M., Mosena L., Girolami A., Vaccarino A., Alatri A., Palareti G., Marchesi M., Ambrosio G.B., Parisi R., Doria S., Steidl L., Ambrosini F., Silingardi M., Ghirarduzzi A., Iori I., Ageno W., Three Months versus One Year of Oral Anticoagulant Therapy for Idiopathic Deep Venous Thrombosis, N Engl J Med, 345, pp. 165-169, (2001)
[4]  
Brass L.M., Krumholz H.M., Scinto J.M., Radford M., Warfarin use among patients with atrial fibrillation, Stroke, 28, pp. 2382-2389, (1997)
[5]  
Buckingham T.A., Hatala R., Anticoagulants for atrial fibrillation: Why is the treatment rate so low?, Clin Cardiol, 25, pp. 447-454, (2002)
[6]  
Bungard T.J., Ackman M.L., Ho G., Tsuyuki R.T., Adequacy of anticoagulation in patients with atrial fibrillation coming to a hospital, Pharmacotherapy, 20, pp. 1060-1065, (2000)
[7]  
Bungard T.J., Ghali W.A., Teo K.K., McAlister F.A., Tsuyuki R.T., Why do patients with atrial fibrillation not receive warfarin?, Arch Intern Med, 160, pp. 41-46, (2000)
[8]  
Donnan G.A., Dewey H.M., Chambers B.R., Warfarin for atrial fibrillation: The end of an era?, Lancet Neurol, 3, pp. 305-308, (2004)
[9]  
Di Nisio M., Middeldorp S., Buller H.R., Direct Thrombin Inhibitors, N Engl J Med, 353, pp. 1028-1040, (2005)
[10]  
Leone-Bay A., Paton D.R., Variano B., Leipold H., Rivera T., Miura-Fraboni J., Baughman R.A., Santiago N., Acylated non-alpha-amino acids as novel agents for the oral delivery of heparin sodium, USP, J Control Release, 50, pp. 41-49, (1998)