今日药学

2015, v.25(07) 504-506

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依达拉奉在比格犬体内的药动学研究
Pharmacokinetic Parameters of Edaravone in Beagle Dogs

汪剑锋,胡敏,李文静,杨娟
WANG Jianfeng,HU Min,LI Wenjing,YANG Juan

摘要(Abstract):

目的研究口服给药后依达拉奉在比格犬体内的药动学特征。方法经灌胃给予比格犬依达拉奉(10 mg/kg)后在不同时间点从后肢静脉取血2 m L,采用沉淀蛋白法处理血浆样品,应用LC-MS/MS法检测比格犬各时间点血浆中的依达拉奉血药浓度。并使用DAS 2.1药代动力学软件计算药动学参数。结果比格犬体内依达拉奉的t1/2为(4.127±0.356)h,Tmax为(0.375±0.177)h,Cmax为(8.124±0.86 5)mg/L,AUC0-∞为(7.970±0.149)mg·L-1·h-1。结论建立的方法简单、灵敏,可用于依达拉奉在比格犬体内的血药浓度测定,药动学结果为依达拉奉口服给药的可行性研究提供依据。
OBJECTIVE To study the oral pharmacokinetic characteristics of edaravone in beagle dogs. METHODS The 2 m L of blood samples were collected at a series of time points after oral administration of edaravone( 10 mg / kg) to beagles,and it was dealt by protein precipitation. Based on the LC-MS / MS method,the concentration of edaravone in beagle plasma was detected after oral administration. Then the pharmacokinetic parameters were calculated by DAS 2.1. RESULTS The oral pharmacokinetic parameter t1 / 2of edaravone in beagle was( 4.127 ± 0. 356) h,Tmaxwas( 0. 375 ± 0. 177) h,Cmaxwas( 8. 124 ± 0. 865) mg / L,AUC0-∞was( 7. 970 ±0. 149) mg·L-1·h-1. CONCLUSION The established medthod is simple and sensitive for the determination of the concentration of edaravone in beagle plasma. The pharmacokinetic results provide a basis for the feasibility study of oral adiministration of edaravone.

关键词(KeyWords): 依达拉奉;LC-MS/MS;比格犬;药动学
edaravone;LC-MS/MS;beagle;pharmacokinetic

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作者(Author): 汪剑锋,胡敏,李文静,杨娟
WANG Jianfeng,HU Min,LI Wenjing,YANG Juan

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