The oral delivery of heparin is the preferred therapy in the treatment of patients with a high risk of deep vein thrombosis and pulmonary embolism. New conjugates of heparin and sodium deoxycholate were synthesized in order to enhance the heparin absorption in the GI tract. After oral administration of DOC-heparin, the concentration in anti-FXa assay was increased with increasing amount of coupled DOC. The maximum concentration of DOC-heparin VIII conjugate was 3.3±0.5 IU/mL at an oral dose of 10 mg/kg, which was 3-fold higher than the base-line level. Finally, DOC coupled to heparin greatly enhanced the absorption of heparin in the GI tract, and this enhancing effect was not induced by changing the tissue structure of the GI wall.

中文翻译：

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胃肠道中脱氧胆酸钠结合肝素的口服吸收评价

肝素的口服给药是治疗深静脉血栓形成和肺栓塞高风险患者的首选治疗方法。为了增强肝素在胃肠道中的吸收，合成了新的肝素和脱氧胆酸钠结合物。口服DOC-肝素后，抗FXa分析的浓度随DOC偶联量的增加而增加。在口服剂量为10 mg / kg时，DOC-肝素VIII缀合物的最大浓度为3.3±0.5 IU / mL，比基线水平高3倍。最终，DOC与肝素的结合大大增强了肝素在胃肠道中的吸收，并且这种增强作用不是通过改变胃肠道壁的组织结构来诱导的。