尼莫地平微乳注射液在小鼠体内的药动学和组织分布研究  

In vivo pharmacokinetics and distribution of nimodipine microemulsion injection in mice

作　　者：周丽娟[1,2] 陈曦[2] 刘清飞[2] 罗国安[2] 

机构地区：[1]郑州市中心医院药剂科,郑州450007 [2]清华大学生命科学与医学研究院,北京100084

出　　处：《中国新药杂志》2009年第13期1231-1236,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30500666);清华大学裕元基金(20240000529;20240000548)

摘　　要：目的:研究尼莫地平微乳注射液(NMD ME)在小鼠血中的药动学及在小鼠脑、肝、肾中的分布情况。方法:将NMD ME和尼莫地平注射液小鼠尾静脉注射给药,采用HPLC法测定NMD在小鼠血浆、脑、肝、肾中的浓度,得知NMD的体内分布情况。结果:血浆、脑、肝、肾中的AUC,Cmax,Tmax都无明显的区别。尼莫地平注射液小鼠尾静脉给药后,73%的小鼠出现死亡。结论:NMD ME与尼莫地平注射液相比,生物利用度基本等效,刺激性明显降低,安全性增强,具有较大的临床应用潜力。Objective：To study in vivo the pharmacokinetics of nimodipine mieroemulsion injection and its distribution of NMD ME in plasma, brain, liver and kidney of mice. Methods ： NMD ME and NMD injection were administrated by mouse tail vein injection. The concentrations were determined by HPLC for NMD in plasma, the brain,the liver,kidney in mice. The distribution in vivo was investigated for NMD. Results：There were no significant changes in AUC, Cmax,Tmax of plasma, brain, liver, kidney between NMD ME and NMD injention. In the animal experiments, 73 percent mice died in NMD injection group. Conclusion：Compared NMD with NMD injection, biological availability was equivalent. NMD ME could reduce stimulation significantly and enhance its security, and it presented great clinical value.

关 键 词：尼莫地平 微乳 刺激性 生物利用度 

分 类 号：R972.4[医药卫生—药品]