Bergqvist D, Hedner U, Sjörin E, Holmer E
Thromb Res. 1983 Nov 15;32(4):381-91. doi: 10.1016/0049-3848(83)90091-9.
Two types of LMW heparin were prepared by gel filtration of standard heparin (LMW fraction) and by degradation of heparin by nitrous acid (LMW fragment), respectively. The effects on factor Xa inhibition (XaI), APTT, platelet aggregation and AT III level of these preparations were studied after subcutaneous administration to humans and compared with those of standard heparin. At a dose of 5000 IU (XaI) the LMW fraction and LMW fragment induced peak plasma XaI activity of 0.32 IU/ml and 0.41 IU/ml respectively, compared to 0.07 IU/ml for heparin. Still 11.5 h after administration both LMW preparations gave higher activities than heparin ever induced. Following administration of 10,000 IU (XaI) of the LMW fragment the plasma peak XaI activity was 0.81 IU/ml. This prolonged the APTT from 36 sec to 46 sec only. The half-lives of the XaI activity in plasma were between 3 and 4 hours. No effect on platelet aggregation or AT-III level was demonstrated.
分别通过对标准肝素进行凝胶过滤(低分子量级分)和用亚硝酸降解肝素(低分子量片段)制备了两种低分子量肝素。将这些制剂皮下注射给人体后,研究了它们对因子Xa抑制作用(XaI)、活化部分凝血活酶时间(APTT)、血小板聚集和抗凝血酶III(AT III)水平的影响,并与标准肝素进行了比较。在5000国际单位(XaI)的剂量下,低分子量级分和低分子量片段诱导的血浆XaI活性峰值分别为0.32国际单位/毫升和0.41国际单位/毫升,而肝素为0.07国际单位/毫升。给药后11.5小时,两种低分子量制剂的活性仍高于肝素所诱导的活性。给予10000国际单位(XaI)的低分子量片段后,血浆XaI活性峰值为0.81国际单位/毫升。这仅使APTT从36秒延长至46秒。血浆中XaI活性的半衰期在3至4小时之间。未显示对血小板聚集或AT-III水平有影响。