Raake W, Klauser R J, Elling H, Zeiller P
Department of Pharmacology and Chemistry, Luitpold-Werk, Munich, FRG.
Haemostasis. 1991;21 Suppl 1:127-32. doi: 10.1159/000216273.
The dose- and time-dependent antithrombotic activity of recombinant hirudin (r-hirudin) was examined in a new animal model of venous thrombosis. For the evaluation of the antithrombotic activity of r-hirudin, an occluding thrombus was produced by repeated clamping of the rat jugular vein. The number of clampings necessary to induce thrombosis served as a measure of antithrombotic activity. The gradual reduction of blood flow was registered by Doppler sonography. In order to estimate the relative antithrombotic activity of r-hirudin, its potency in this model was compared with other antithrombotic substances. r-Hirudin proved to be less potent than heparin after intravenous administration. Its half-life after subcutaneous administration was relatively short; however, the antithrombotic potency after subcutaneous administration was comparable to that of heparin.
在一种新的静脉血栓形成动物模型中,研究了重组水蛭素(r-水蛭素)的剂量和时间依赖性抗血栓活性。为评估r-水蛭素的抗血栓活性,通过反复夹闭大鼠颈静脉形成闭塞性血栓。诱导血栓形成所需的夹闭次数作为抗血栓活性的指标。用多普勒超声记录血流的逐渐减少。为估计r-水蛭素的相对抗血栓活性,将其在该模型中的效力与其他抗血栓物质进行比较。静脉给药后,r-水蛭素的效力被证明低于肝素。皮下给药后其半衰期相对较短;然而,皮下给药后的抗血栓效力与肝素相当。