Görög P, Raake W
Arzneimittelforschung. 1987 Mar;37(3):342-5.
Antithrombotic activity of mucopolysaccharide polysulfuric acid ester (MPS) was investigated in vitro as well as in animal models of thrombosis. In vitro studies were performed by using native human blood and the haemostatometer. MPS (greater than or equal to 25 micrograms/ml) caused concentration dependent inhibition of the in vitro haemostasis (platelet reactivity). Antihaemostatic activity of epoprostenol (prostacyclin) was synergized by MPS. In vivo platelet thrombus formation was induced by laser irradiation in the microvasculature of hamster cheek pouch. The time until occlusion of the irradiated small vein and the duration of occlusion were measured. MPS administered intravenously at a dose range of 1-10 mg/kg b.w. inhibited thrombus formation and prolonged the time until occlusion of the irradiated vessel. Upon topical administration of a solution of 1, 5 or 25% MPS the occlusion time was also prolonged. Topical application of MPS as a 0.3% cream (Hirudoid) increased the occlusion time significantly. 24 h percutaneous application of 0.3% MPS cream but not the placebo on the back skin of rats resulted in a significant (p less than 0.001) inhibition of thrombus formation in the microvessels of the mesoappendix. A common finding at all modes of administration of MPS was that reperfusion of the occluded vessel occurred much earlier in MPS treated animals than in the controls.
在体外以及血栓形成的动物模型中研究了硫酸多糖酯(MPS)的抗血栓活性。体外研究使用正常人血液和止血计进行。MPS(大于或等于25微克/毫升)导致体外止血(血小板反应性)的浓度依赖性抑制。MPS增强了依前列醇(前列环素)的抗止血活性。通过激光照射仓鼠颊囊微血管诱导体内血小板血栓形成。测量照射的小静脉闭塞前的时间和闭塞持续时间。以1-10毫克/千克体重的剂量静脉注射MPS可抑制血栓形成,并延长照射血管闭塞前的时间。局部应用1%、5%或25%的MPS溶液也可延长闭塞时间。局部应用0.3%的MPS乳膏(喜疗妥)可显著延长闭塞时间。在大鼠背部皮肤经皮应用0.3%的MPS乳膏24小时而非安慰剂,可显著(p<0.001)抑制阑尾系膜微血管中的血栓形成。MPS所有给药方式的一个共同发现是,与对照组相比,接受MPS治疗的动物中闭塞血管的再灌注发生得要早得多。