芒柄花素磺酸钠在脑缺血再灌注大鼠脑组织的药动学研究  

Pharmacokinetic study of sodium formononetin-3'-sulphonate in brain of cerebral ischemia-reperfusion rat

作　　者：孙瑜[1] 罗西[2] 王健[3] 庄朋伟[1] 宋丽丽[1] 陈磊[1] 乔夕[1] SUN Yu;LUO Xi;WANG Jian;ZHUANG Peng-wei;SONG Li-li;CHEN Lei;QIAO Xi(Tianjin University of Traditional Chinese Medcine,Tianjin 300193,China;Tianjin Chest Hospital,Tianjin 300051,China;Tianjin Children＇s Hospital,Tianjin 300074,China)

机构地区：[1]天津中医药大学,天津300193 [2]天津市胸科医院,天津300051 [3]天津市儿童医院,天津300074

出　　处：《现代药物与临床》2018年第8期1870-1874,共5页Drugs & Clinic

基　　金：天津市卫生和计划生育委员会中医中西医结合科研课题(2017104)

摘　　要：目的建立脑组织样品中芒柄花素磺酸钠的高效液相色谱分析方法,确定芒柄花素磺酸钠在脑缺血再灌注大鼠脑内的量–时关系,明确芒柄花素磺酸钠在模型大鼠脑组织中的吸收分布情况。方法制备大鼠脑缺血再灌注模型,随机分为10组,每组各5只。于脑缺血1 h及再灌注3.5 h ip芒柄花素磺酸钠注射液20 mg/kg,并于给药后15、30、45、60、90、120、150、180、240、300 min实施心脏灌流后取脑组织匀浆。样品处理后,采用HPLC法检测各时间点脑组织中芒柄花素磺酸钠的质量浓度。采用药动学软件Win Non Lin 6.3对数据进行分析,计算药动学参数。结果模型大鼠缺血1 h再灌注4 h时给药,脑组织中芒柄花素磺酸钠含量最高。芒柄花素磺酸钠在模型大鼠脑组织内药动学参数t1/2、Cmax、AUC0-t分别为(261.18±49.33)min、(1.56±0.37)μg/m L、(93.60±7.13)min·μg/m L。结论芒柄花素磺酸钠可以进入脑缺血再灌注大鼠脑组织,滞留时间长。Objective To establish an HPLC analysis method for sodium formononetin-3＇-sulphonate（Sul-F） brain tissue samples, and determine the amount-time relationship of Sul-F in cerebral ischemia-reperfusion rats, so as to define the clear absorption and distribution of Sul-F in brain tissue in rats model. Methods MCAO rats models were established. Animal models were randomly divided into 10 groups, and each group had 5 rats. At the point of 3.5 h reperfusion after 1 h of cerebral ischemia, rats were ip administered with Sul-F at the dose of 20 mg/kg. At different time points of 15, 30, 45, 60, 90, 120, 150, 180, 240, and 300 min after treatment of heart perfusion, brain tissue homogenate was taken. Samples were treated, then HPLC method was used to detect Sul-F content in brain tissue at different time points. Pharmacokinetic data were analyzed by Win Non Lin 6.3 pharmacokinetic software, and pharmacokinetic parameters were calculated. Results When rats in the model group were received 1 h ischemia and 4 h reperfusion, Sul-F had highest content in brain tissue. The pharmacokinetic parameters of Sul-F in MCAO rat model brain tissue were as following： t1/2 was（261.18 ± 49.33） min, Cmax was（1.56 ± 0.37） μg/m L, and AUC0-t was（93.60 ± 7.13） min·μg/m L. Conclusion Sul-F can enter the brain tissue of cerebral ischemia-reperfusion rats, and the residence time is long.

关 键 词：芒柄花素磺酸钠 脑缺血再灌注 脑药动学 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学]