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作 者:沈舒[1,2] 申昕[1] 荆晶[1] 苏晨灿 强乐[1] 冯萌[1] 魏来[1] 刘利月[1] 车金[1] 王冰[1] 史小莲[1]
机构地区:[1]西安交通大学医学部,西安710061 [2]中国食品药品检定研究院,北京100050
出 处:《西北药学杂志》2014年第5期480-483,共4页Northwest Pharmaceutical Journal
基 金:陕西省自然科学基础研究计划项目(编号:2013JQ4042);西安交通大学本科生科研训练和实践创新基金(编号:xjj2013056)
摘 要:目的研究国产血小板糖蛋白Ⅱb/Ⅲa受体拮抗剂依替巴肽抗血栓形成作用。方法 30只杂种犬随机分为空白对照组、阳性对照替罗非班组,依替巴肽高、中、低剂量组(n=6)。模拟临床采取负荷量静脉给药与维持量连续给药的方式,负荷量各组为300,100和30μg·kg-1,维持量各组为5,5和2.5μg·kg-1·min-1,持续1h。建立FeCl3诱导的犬动脉血栓模型、犬股动静脉旁路血栓模型,观察依替巴肽体内抗血栓形成作用,并采用出血时间测定器测定出血时间。结果依替巴肽大、中、小剂量组动静脉血栓湿质量分别为153.4±47.7,187.5±42.9和243.3±51.9mg,动静脉血栓形成抑制率分别为50.1%,39.0%和20.8%,与空白组相比(307.2±74.1mg)大、中剂量组差异有统计学意义;各组动脉血栓湿质量分别为6.5±1.4,8.9±2.3和16.2±3.9mg,对动脉血栓湿质量的抑制率分别为69.1%,58.0%和23.2%,与空白组相比(21.1±4.8mg),大、中剂量组差异有统计学意义;给药过程中出血时间不同程度延长。结论国产依替巴肽可抑制犬动脉血栓、动静脉血栓的形成,延长出血时间。Objective To observe the antithrombotic effect of homemade eptifibatide in canine .Methods Eptifibatide was infused as a bolus of 300 ,100 and 30 μg · kg -1 ,immediately followed by progressively infusions at a rate of 5 ,5 and 2.5μg · kg -1 · min-1 respectively for 1 h .Two models ,FeCl3 induced artery thrombosis (AT ) and femoral arteriovenous-shunt thrombosis (AVST ) were established in canine .Template bleeding time (TBT) was used to measure the bleeding time .Results Eptifibatide could alle-viate the weight of thrombus in both AT and AVST models .Compared with the normal saline treated group (307.2 ± 74 .1 mg) , the inhibition rate of AVST formation were 50 .1% ,39 .0% and 20 .8% in eptifibatide treated groups with thrombus wet weight at 153 .4 ± 47 .7 ,187 .5 ± 42 .9 and 243 .3 ± 51 .9 mg accordingly .Compared with normal saline treated group (21 .1 ± 4 .8 mg ) ,the inhibition rate of AT formation were 69 .1% ,58 .0% and 23 .2% in eptifibatide treated groups with wet weight at 6 .5 ± 1 .4 , 8 .9 ± 2 .3 and 16 .2 ± 3 .9 mg accordingly .There was significant difference between the high ,middle dose of eptifibatide treated groups and normal saline treated group in the two models of thrombosis (P〈0 .05) .Eeptifibatide also prolonged the bleeding time dose-dependently .Conclusion Homemade eptifibatide has a strong antithrombotic effect in canine .
关 键 词:血小板糖蛋白Ⅱb/Ⅲa受体拮抗剂 依替巴肽 血栓形成 出血时间
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