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以标准肝素(SH)为原料经亚硝酸裂解制备的低分子量肝素(LMWH),给予同等抗Xa单位剂量时,对凝血系统的影响较SH小,在治疗量下(100anti-XaIU/kg)不增加出血倾向;体外实验表明,LMWH能有效地抑制chandler模型的血栓形成;体内实验表明,LMWH在100~200antiXaIU/kg范围内能有效地抑制大鼠动-静脉旁路、大鼠颈动脉电流损伤(iv,sc)和家兔颈静脉血栓模型的血栓形成,与参照品Fragmin及SH的作用相似,LMWH在上述模型中的ED50分别为:159,185(iv),193(sc),91anti-XaIU/kg;研究还发现,scLMWH吸收完全,给药后3h的抗血栓作用与iv后10min相似,而SH的作用弱。提示LMWH保留了SH的抗血栓作用,降低了SH的出血副作用。
Low molecular weight heparin (LMWH) prepared by nitrous acid cleavage using standard heparin (SH) as a raw material had a lower impact on the coagulation system when administered with the same anti-Xa unit dosage than the SH at the dose of 100anti-XaIU / kg Increase the tendency of bleeding; In vitro experiments show that, LMWH can effectively inhibit the thrombosis of chandler model; In vivo experiments showed that LMWH in 100 ~ 200antiXaIU / kg range can effectively inhibit rat venous bypass, rat carotid artery current injury (Iv, sc) and rabbit jugular vein thrombosis model, similar to the reference Fragmin and SH, LMWH ED50 in the above model were: 159,185 (iv), 193 (sc), 91anti- XaIU / kg; study also found that, scLMWH absorbed completely, 3h after administration of anti-thrombotic effect similar to iv after 10min, while the role of SH weak. Tip LMWH retains the SH anti-thrombotic effect, reducing the bleeding side effects of SH.