【2017年整理】药物制剂工程 lili.docVIP

药物制剂工程 ——溶栓剂的研发现状及展望‘ 生技082 邵丽 2008054028 溶栓剂的研发现状及展望 摘要：由血栓引起的血栓性疾病是一种常见的心脑血管疾病。溶栓剂是预防与治疗心脑血管疾病的主要抗血栓药物。本文总结性地概述了目前国内外各种新型溶栓剂的溶栓机理、临床应用效果及其副作用等。其中，第三代溶栓剂组织型纤溶酶原激活剂变异体、导向溶栓剂、嵌合体溶栓剂。以及部分天然溶栓剂包括蝙蝠唾液纤溶酶原激活剂、蛇毒纤溶酶原激活剂、水蛭素及其变异体等均通过将纤溶酶原激活为纤溶酶溶解血栓。临床实验结果表明它们在延长体内半寿期、增强对血纤维蛋白选择性和溶栓效率等方面有较大的改进，但溶栓治疗后的冠状动脉再栓塞，颅内出血等问题仍是目前未解决的难题；而纳豆激酶及豆豉纤溶酶由于溶栓原理的不同，引起内出血的几率较低。溶栓剂未来的发展方向为如何综合不同药物的优点，使其更加安全与廉价。 关键词：溶栓剂；现状；展望；血栓；纳豆激酶 Thrombolytic agent status and prospects of development Abstract: Thrombosis caused by the thrombosis is a common cardiovascular disease. Thrombolytic agents is the prevention and treatment of cardiovascular and cerebrovascular diseases, the main anti-thrombosis drugs. This summary overview of the current home and abroad, new thrombolytic agent thrombolytic mechanisms, clinical effects and side effects. Among them, the third-generation thrombolytic agent tissue plasminogen activator variant, oriented thrombolytic agents, thrombolytic agents chimera. And some natural thrombolytic agents, including bat saliva plasminogen activator, venom plasminogen activator, hirudin and its variants etc by plasminogen activator plasmin dissolves clots. Clinical results show that they extend in vivo half-life, enhancement of fibrin selectivity and efficiency of thrombolytic therapy have a greater improvement, but after thrombolytic therapy of coronary artery embolism, intracranial hemorrhage and other problems are still not currently solve problems; and nattokinase and tempeh plasminogen thrombolytic principle because different lower risk of causing internal bleeding. The future development of thrombolytic agents for the how to integrate the advantages of different drugs, to make it more safe and cheap. Keywords: thrombolytic agent; the status quo; outlook; thrombosis; nattokinase 由血栓引起的血栓性疾病是一种常见的心脑血管病，常表现为心肌梗死、缺血性脑梗死、静脉血栓栓塞，是中老年人易发的疾病之一，而且目前青年病人的数量也在上升。据世界卫生组织(WHO)估计。全世界每年死于心脑血管病的人数超过l 200万人。其中在美国，男性急性心肌梗死的死亡率达27％，女性为44％o LH在我国，每年需要