注射用塞克硝唑小鼠及犬急性毒性试验  

Acute Toxicity of Secnidazole for Injection in Mice and Dogs

作　　者：张同辉[1] 郏自明[1] 周一平[1] 游窑生[1] 陈四艳[1] 余启枝[1] 何映[1] 

机构地区：[1]湖北省医药工业研究院有限公司湖北省药物安全性评价中心,武汉430061

出　　处：《医药导报》2009年第5期582-585,共4页Herald of Medicine

摘　　要：目的观察动物单次注射塞克硝唑(SI)的急性毒性。方法将40只昆明种小鼠分为给药组和对照组,最大给药量法进行静脉注射毒性实验;3只Beagle犬以近似致死剂量法进行静脉滴注毒性试验。给药后均观察14d。结果小鼠静脉注射给予塞克硝唑500mg·kg-1后无死亡,但活动减少、反应迟钝和呆滞,1h内恢复正常。犬2000mg·kg-1静脉注射塞克硝唑后24h死亡;静脉注射塞克硝唑1330mg·kg-1后活动减少,反应迟钝;静脉注射给予塞克硝唑890mg·kg-1后未见明显不良反应。结论小鼠静脉注射塞克硝唑的最大给药量>500mg·kg-1,犬静脉滴注塞克硝唑的安全剂量为890mg·kg-1,近似致死量为1330～2000mg·kg-1,主要毒性反应为可逆性神经系统毒性症状。Objective To investigate the acute toxicity of secnidazole [ 1-（2-methyl-5-nitroimidazole-1-yl） propan-2- ol] for injection （SI） at a single dose in mice and dogs. Methods The maximal administration dose（MAD）and the approximate lethal dose（ALD） were studied in 40 mice and three Beagle dogs by intravenous injection and through intravenous drip, respectively. Both animals were kept on observing for 14 days. Results All mice were alive after injection and the nerve toxicity symptoms such as reduced activity, languishment and twitch were found during one hour after administration. The dog died at 2 000 mg·kg^-1 of SI, activity was decreased at 1 330 mg·kg^-1 , and remained normal at 890 mg·kg^-1. Conclusion The MAD of SI is above 500 mg·kg^-1 in mice. The ALD is 1 330 - 2 000mg·kg^-1 and the no observed adverse effect level （NOAEL） is 890 mg·kg^-1 in dog by intravenous drip. The main toxicity is appeared in nerve system in both animals.

关 键 词：塞克硝唑 毒性试验 小鼠 犬 

分 类 号：R965.3[医药卫生—药理学]