川芎嗪硝酮衍生物在脑缺血模型大鼠脑中浓度  

Concentration of nitrone derivative of tetramethylpyrazine in brain tissue of cerebral ischemia model rats

作　　者：黎赛[1] 李沙[2,3] 陈海南[2] 孙业伟[1] 张高小[1] 王兴立[2] 蒋杰[1] 赵文[4] 王玉强[1] 

机构地区：[1]暨南大学药学院新药研究所,广州510632 [2]暨南大学药学院药剂学教研室,广州510632 [3]暨南大学中药药效物质基础及创新药物研究广东省高校重点实验室,广州510632 [4]暨南大学药学院实验技术中心,广州510632

出　　处：《中国临床药理学杂志》2011年第6期446-449,453,共5页The Chinese Journal of Clinical Pharmacology

基　　金：国家科技重大专项课题--"重大新药创制"基金资助项目(2009ZX09103-031);广东省科技计划基金资助项目(2010B011000006);广东省医学科研基金资助项目(B2009127);暨南大学科研培育与创新基金技术创新与应用研究基金资助项目(21609504)

摘　　要：目的考察脑缺血模型大鼠与正常大鼠脑组织中(2-N-叔丁基硝酮)-3,5,6-三甲基吡嗪(TBN)的浓度差异。方法用线栓法,建立大脑中动脉栓塞脑缺血大鼠模型,按不同剂量或在不同再灌注时间后给药,用HPLC方法测定脑组织中TBN浓度。结果以不同剂量、在不同再灌注时间后给药,TBN在模型大鼠脑中的浓度均基本高于正常大鼠。模型鼠脑中TBN浓度随剂量增加而增大,两者呈良好的线性关系。于不同再灌注时间后给药,对脑中TBN浓度影响明显。结论在脑缺血再灌注后,TBN能更有效地透过大鼠血脑屏障,产生更高的脑药浓度。Objective To investigate the difference of concentration of 2-（1,1-dimethylethyl）oxidoimino]methyl]-3,5,6-trimethylpyrazine（TBN） in brain between cerebral ischemia model rats and normal rats.Methods The suture occlusion method was used to establish the middle cerebral artery occlusion（MCAo） model in rats.The cerebral ischemia model rats were administered TBN at different dosages or after different reperfusion time.The concentration of TBN in their brain tissue was assayed by using HPLC method.Results After given the drug at different dosages or after different reperfusion time,the concentration of TBN in the brain of cerebral ischemia model rats was generally higher than that in normal rats.The TBN concentration in the brain of cerebral ischemia rats increased with the increase of dosage.There was a good linear relationship between TBN concentration and dosage.Administrating drug after different reperfusion time influenced the TBN concentration in brain tissue obviously.Conclusion After cerebral ischemia followed by reperfusion,TBN could effectively penetrate through the blood brain barrier,thus to result in a higher drug concentration in brain tissue.

关 键 词：川芎嗪硝酮衍生物 脑缺血 脑组织浓度 高效液相色谱法 

分 类 号：R972.6[医药卫生—药品] R285.5[医药卫生—药学]