Money S R, York J W
Department of Surgery, Division of Vascular Surgery, Alton Ochsner Medical Foundation, Ochsner Clinic, 1514 Jefferson Highway 8N, New Orleans, LA 70121, USA.
Cardiovasc Surg. 2001 Jun;9(3):211-8. doi: 10.1016/s0967-2109(00)00144-7.
To review the current research and published literature regarding the development of oral heparin therapy for the prophylaxis and treatment of deep venous thrombosis.
Currently, the accepted practice of prophylaxis and/or treatment of acute deep venous thrombosis (DVT) is intravenous or subcutaneous (SQ) heparin followed by oral warfarin or SC low molecular weight heparin (LMWH) therapy followed by warfarin. Both of which are less than ideal. More recently, advances have been made towards an effective oral heparin preparation that would resolve many of the drawbacks to the current therapies.
A review of the current and relevant English literature identified via a search of the Medline database from January 1990 to present.
Initial oral heparin therapy for DVT was unsuccessful due to presumed inadequate intestinal absorption as a result of heparin's molecular and structural characteristics. The development of oral heparin therapy, based on combining heparin with the carrier molecule Sodium N-(8[2-hydroxybenzoyl]amino) caprylate (SNAC) to enhance its intestinal absorption and bioavailability for the prophylaxis and treatment of DVT has been demonstrated to be effective in animal models. More recent efforts have been aimed at human trials.
Recent advances in prophylaxis and treatment of DVT have stimulated great interest among researchers to develop an effective, convenient, and well tolerated oral therapy. An effective oral heparin therapy may represent an ideal method of prophylaxis and treatment of DVT.
回顾目前关于口服肝素疗法用于预防和治疗深静脉血栓形成的研究及已发表文献。
目前,急性深静脉血栓形成(DVT)预防和/或治疗的公认做法是静脉注射或皮下注射肝素,随后口服华法林,或皮下注射低分子肝素(LMWH),随后口服华法林。这两种方法都不尽如人意。最近,在开发一种有效的口服肝素制剂方面取得了进展,该制剂将解决当前疗法的许多缺点。
通过检索1990年1月至今的Medline数据库,对当前及相关英文文献进行综述。
由于肝素的分子和结构特征导致肠道吸收不足,最初用于DVT的口服肝素疗法未获成功。基于将肝素与载体分子N-(8-[2-羟基苯甲酰基]氨基)辛酸钠(SNAC)结合以增强其肠道吸收和生物利用度来预防和治疗DVT的口服肝素疗法,已在动物模型中证明是有效的。最近的努力旨在进行人体试验。
DVT预防和治疗的最新进展激发了研究人员对开发一种有效、方便且耐受性良好的口服疗法的极大兴趣。有效的口服肝素疗法可能代表预防和治疗DVT的理想方法。