目的 研究重组水蛭素的抗凝活性,为水蛭素新药开发提供实验依据.方法 家兔iv重组水蛭素前及后心脏采血,应用血凝仪测定凝血酶时间(TT)、凝血酶原时间(PT)和活化的部分凝血活酶时间(APTT),并考察其抗凝活性的量效和时效关系.结果 重组水蛭素能明显延长TT和APTT,且呈剂量依赖性,但在所试剂量范围内对PT无明显影响;其延长TT和APTT的作用随时间而下降,作用持续时间约60 min.结论 重组水蛭素具有明显抗凝作用,明显强于现有抗凝药肝素,且其作用强度与同剂量德国产基因重组水蛭素Refludan相同.

Object To study the anticoagulant activity of recombinant hirudin (rH) made in China and to provide the experimental basis for the development of hirudin. Methods Thrombin time (TT), prothrombin time (PT) and activated partial thromboplastin time (APTT) were determined by coagulometer for rabbit blood samples collected before and after iv rH. The percent of lengthening above coagulation time parameters was calculated and used to investigate the dose and time effect relationship of rH. Results The TT and APTT were prolonged remarkably by rh, while PT not within the test range, in a dose dependent manner, and the action duration was about 60 min. Conclusion Domestic rH (N-Ile¹-Thr²-r-hirudin) has obvious anticoagulant effects. Its potency is much higher than heparin, and identical to that of Refludan (N-Leu¹-r-hirudin), which was an authorized rH product made in Germany.

国家“九五”科技攻关计划资金资助(96-C02-01-05A)