Mätzsch T, Bergqvist D, Hedner U, Ostergaard P
Thromb Haemost. 1987 Feb 3;57(1):97-101.
A low molecular weight heparin (LMW-heparin) with a mean molecular weight of 4900 dalton was prepared by controlled enzymatic depolymerization of conventional porcine mucosal heparin. The effects of 2,500, 5,000 and 10,000 U (XaI; 29, 58 and 116 mg) on factor Xa inhibition (XaI), factor IIa inhibition (IIaI), APTT, AT III and platelet count were compared to those of 5,000 U (XaI; 26 mg) of conventional heparin given s.c. to 6 healthy volunteers. 5,000 U (XaI; 58 mg) of LMW-heparin was given i.v. A dose related response with regard to the XaI and the IIa-inhibitory activities with peak values at 4 hours after the s.c. injections was obtained. An increase of the XaI/IIaI ratio over the time after injection was seen only after i.v. administration of the LMW-heparin. The APTT was only slightly prolonged and remained within normal range after s.c. injection. AT III and platelet counts were unaffected. The biological half life of the LMW-heparin was 111 minutes if assayed by Xa inhibition, 76 minutes if assayed by IIa inhibition and 40 minutes if assayed by APTT. A strong correlation between the XaI activities obtained and body weight was seen, indicating that LMW-heparin should be administered individually according to body weight.
通过对传统猪黏膜肝素进行可控酶解聚反应制备了平均分子量为4900道尔顿的低分子量肝素（LMW-肝素）。将2500、5000和10000单位（XaI；29、58和116毫克）的LMW-肝素对Xa因子抑制作用（XaI）、IIa因子抑制作用（IIaI）、活化部分凝血活酶时间（APTT）、抗凝血酶III（AT III）和血小板计数的影响，与皮下注射给6名健康志愿者的5000单位（XaI；26毫克）传统肝素的相应影响进行了比较。静脉注射了5000单位（XaI；58毫克）的LMW-肝素。皮下注射后，在XaI和IIa抑制活性方面获得了与剂量相关的反应，峰值出现在注射后4小时。仅在静脉注射LMW-肝素后，观察到注射后一段时间内XaI/IIaI比值增加。皮下注射后APTT仅略有延长，仍在正常范围内。AT III和血小板计数未受影响。通过Xa抑制作用测定时，LMW-肝素的生物半衰期为111分钟；通过IIa抑制作用测定时为76分钟；通过APTT测定时为40分钟。观察到所获得的XaI活性与体重之间存在强相关性，表明LMW-肝素应根据体重个体化给药。
