Arbit Ehud, Goldberg Michael, Gomez-Orellana Isabel, Majuru Shingai
Emisphere Technologies Inc, 765 Old Saw Mill River Road, Tarrytown, NY 10591, USA.
Thromb J. 2006 May 10;4:6. doi: 10.1186/1477-9560-4-6.
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.
普通肝素和低分子量肝素是医院实践中最常用的抗血栓形成和血栓预防药物。院外长期治疗不方便,因为这些药物必须通过胃肠外给药。目前的研究致力于开发一种安全有效的口服抗血栓药物,以替代有效但难以使用的维生素K拮抗剂。一种有助于药物跨胃肠上皮运输的新型药物递送技术已被用于开发普通肝素的口服剂型。将普通肝素与载体分子N-(8-[2-羟基苯甲酰基]氨基)辛酸钠(SNAC)结合,可显著提高该药物的胃肠吸收。迄今为止的临床前和临床研究表明,口服肝素-SNAC可产生临床疗效;计划中的临床试验将寻求进一步证实。