左乙拉西坦注射液血管刺激性研究  

Vascular irritation of levetiracetam injection

作　　者：李权宁 卜艳红 李辽辽 李东波 冯柯臻 赵正杭 LI Quan-ning;BU Yan-hong;LI Liao-liao;LI Dong-bo;FENG Ke-zhen;ZHAO Zheng-hang(Department of Pharmacology,School of Xi’an Jiaotong University Health Science Center,Xi’an 710061;Xi’an Grand Deten Pharmaceutical Co.,Ltd.,Xi’an 710119;Department of Public Health,School of Xi’an Jiaotong University Health Science Center,Xi’an 710061;Department of Pharmacy,School of Xi’an Jiaotong University Health Science Center,Xi’an 710061)

机构地区：[1]西安交通大学医学部基础医学院,西安710061 [2]西安远大德天药业股份有限公司,西安710119 [3]西安交通大学公共卫生学院,西安710061 [4]西安交通大学药学院,西安710061

出　　处：《中南药学》2022年第3期593-596,共4页Central South Pharmacy

摘　　要：目的评估仿制药左乙拉西坦注射液对家兔血管的刺激性,为该药物上市申请及临床安全用药提供参考。方法新西兰兔应用微量注射泵左耳缘静脉注射质量浓度为13 mg·m^(L-1)的左乙拉西坦注射液,右耳缘静脉注射0.9%氯化钠注射液,给药容量为5.8 mL·kg^(-1),速率1 mL·min^(-1),2次·d^(-1),连续3 d。肉眼观察每次给药后、末次给药后17 d给药部位及周边组织的刺激性反应,并分别于末次给药后的第3日及第17日处理4只和2只动物进行组织病理检查。结果在给药期,左乙拉西坦注射液对兔的耳缘静脉具有轻微刺激性,而恢复期未见明显刺激性症状。结论仿制药左乙拉西坦注射液对兔耳血管无明显刺激性作用,符合我国《化学药物刺激性、过敏性和溶血性研究技术指导原则》中注射剂对血管刺激性的要求,可用于上市注册申请。Objective To evaluate the vascular irritation of the levetiracetam injection in rabbits and provide reference for safe drug usage in clinical practice and evidence for its marketing application.Methods Levetiracetam injection was injected into the marginal vein of the left ear of New Zealand rabbits by a microinjection pump.The dosing mass concentration,volume and speed were 13 mg·m^(L-1),5.8 mL·kg^(-1) and 1 mL·min^(-1),respectively,twice daily for three consecutive days,and equivoluminal sodium chloride injection(0.9%)was injected into right at the same volume and speed.The irritation of the site and peripheral tissues was observed after each administration and 17 days after the last injection;Histopathological examination was performed on 4 or 2 rabbits on the 3rd and 17th day after the last administration.Results Levetiracetam injection presented a slight irritation on the ear veins of rabbits during the administration,but no obviously irritating symptoms were seen after the recovery.Conclusion Levetiracetam injection has no obvious irritation on the ear veins of rabbits,which accords with the criteria of“Guidance for Chemical Drug Development on Irritation,Anaphylaxis and Hemolysis Test”,and could be used for registration.

关 键 词：左乙拉西坦注射液 血管刺激性 兔 

分 类 号：R965[医药卫生—药理学]