比伐卢定的升降压物质检查和毒性实验  

Pressor and Depressor Substance Test and Toxicity of Bivalirudin

作　　者：刘春[1] 赵毓梅[1] 郑霞[1] 

机构地区：[1]海南省药品检验所,海口570216

出　　处：《中国药房》2014年第9期805-807,共3页China Pharmacy

摘　　要：目的：研究比伐卢定的升降压物质检查和毒性实验。方法：按照2010年版《中国药典》二部相关方法，以1～5倍（2．8～14mg／kg）临床单次用药剂量作为降压和升压物质检查剂量，采用猫血压法确定降压物质检查限值，采用SD大鼠总动脉插管监测血压确定升压物质检查限值；小鼠经尾静脉注射给药急性毒性实验测算其半数致死量（LD60），并确定异常毒性检查限值。结果：比伐卢定的降压、升压物质检查限值均为14mg／kg；小鼠静脉注射的LD50为1．60g/kg，LD50的95％可信限为1．50--1．71g／kg；异常毒性检查注射给药后观察48h，未见小鼠死亡。结论：比伐卢定符合《中国药典》要求。OBJECTIVE： To study the pressor and depressor substance test and toxicity of bivalirudin. METHODS： According to Chinese Pharmacopeia （2010 edition）, the 1-5 times of clinical single dose （2.8-14 mg/kg） were used for the determination of depressor substances and vasopressor substance. The limit of depressor substance was determined with cat blood pressure. The blood pressure of SD rats was monitored by total arterial intubation to determine the limit of vasopressor substance. Mice were given medi- cines via tail vein in acute toxicity test to detect LDs0. The limit of abnormal toxicity test was calculated. RESULTS： The limit of depressor substance test and vasopressor substance were both 14 mg/kg. The LDs0 of intravenous injection of bivalirudin in mice was 1.60 g/kg and 95% confidence limit was 1.50-1.71 g/kg. The abnormal toxicity test showed that no mice died within 48 h after medication. CONCLUSIONS： Bivalirudin is in line with the requirements of Chinese Pharmacopeia.

关 键 词：比伐卢定 降压物质检查 升压物质检查 急性毒性 异常毒性 

分 类 号：R965[医药卫生—药理学]