单方与复方给药后洋川芎内酯Ⅰ在大鼠体内的药动学比较研究  

Comparative study on pharmacokinetics of senkyunolide Ⅰ after administration of simple recipe and compound recipe in rats

作　　者：高文娟[1] 王雪[1] 马春靖[1] 戴荣华[1] 毕开顺[1] 陈晓辉[1] 

机构地区：[1]沈阳药科大学药学院中药质量控制技术国家地方联合工程实验室,辽宁沈阳110016

出　　处：《中国中药杂志》2013年第3期427-431,共5页China Journal of Chinese Materia Medica

摘　　要：目的:建立LC-MS法测定大鼠血浆洋川芎内酯I(senkyunolide Ⅰ,SI)的浓度,比较活络效灵丹加减方(HLXL)和川芎单味药材提取物中SI在大鼠体内的药代动力学参数有无显著性变化,评价HLXL提取物中其他成分对SI药动学的影响。方法:将12只大鼠随机分成2组,按含SI计4.53 mg.kg-1分别灌胃给予HLXL提取物和川芎提取物,不同时间点采血后进行LC-MS分析,测定血浆SI浓度,采用DAS 2.0软件对主要药动学参数进行计算,并用SPSS 16.0软件对其进行独立样本t-检验和非参数t-检验分析。结果:SI在6.750～675.0μg.L-1线性关系良好,最低检测限为6.750μg.L-1。大鼠灌胃HLXL提取物和川芎提取物的药-时曲线均符合二房室模型,测得SI的Cmax,AUC0-24 h和CL有显著性差异,其他参数均无显著性差异。结论:该实验建立的LC-MS测定法专属、准确、灵敏,适用于HLXL提取物和川芎提取物中SI的药动学研究。实验结果表明,HLXL中其他药材对SI的吸收有较大影响。Objective： To develop a LC-MS method for the determination of senkyunolide I （SI） in rat plasma, in order to ob- serve whether there is significant change in the pharmacokinetics parameters of complex prescriptions of Huoluoxiaolingdan （HLXL） and single herbal extracts from Ligusticum chuanxiong Hort. in rats, and assess the effect of other components in HLXL on the pharma- cokinetics of SI. Method： Twelve male Sprague-Dawley （SD） rats were randomly divided into two groups, and orally administered with extract from HLXL and L. chuanxiong （both equal to SI 4. 53 mg ~ kg-~ ）. Their blood was collected at different time points for LC-MS, in order to detect the plasma concentration of SI. The pharmacokinetic parameters of SI were calculated by DAS 2. 0 software. SPSS 16. 0 software was used for independent-sample T-test and Nonparametric T-test. Result： A linear relationship of SI ranged from 6. 750 to 675.0 μg L-1, and with the lowest limit of detection being 6. 750 μg L-1. Both of the plasma concentration-time curves of SI were fitted with the two-compartment model for extract of HLXL and L. chuanxiong. The detected AUC and Cmax of SI showed sig- nificant difference, with no significant difference in other parameters. Conclusion： The LC-MS determination method established in this experiment was so exclusive, accurate and sensitive that it is suitable for pharmacokinetic studies on extracts of HLXL and SI from L. chuanxion. The experiment results show that other ingredients of HLXL have noticeable effect on the absorption of SI in rat plasma.

关 键 词：HLXL 川芎 LC-MS 洋川芎内酯Ⅰ(SI) 药动学 

分 类 号：R96[医药卫生—药理学]