黄芪总皂苷提取物在大鼠体内的药代动力学和组织分布研究

Astragalosides Extract on Pharmacokinetics and Tissue Distribution in Rats

目的:建立测定大鼠血浆中黄芪甲苷的HPLC-UV法,并对其在大鼠体内的药代动力学和组织分布进行了研究。方法:分别按黄芪药材提取物0. 0022 g·kg^(-1)大鼠体质量灌胃给予黄芪总皂苷提取物,分别于0. 25、0. 5、0. 75、1、2、3、4、6、8、10、12、24 h采集血样;按黄芪药材提取物0. 0022 g·kg^(-1)大鼠体质量灌胃给予黄芪总皂苷提取物,在给药前(0 h)和给药后0. 5、1、2 h取血后处死,立即解剖采集心、肝、脾、胃、肾、肺、大肠、小肠、等组织,测定血浆样品和组织样品中的黄芪甲苷浓度。结果:药代动力学结果表明黄芪总皂苷提取物中黄芪甲苷在血浆中代谢;组织分布结果黄芪总皂苷提取物1h时组织内黄芪甲苷含量从高到低顺序是:肝>小肠>肺>心>胃>大肠>脾>肾。结论:黄芪总皂苷提取物具有一定的强心作用,与中药黄芪具有补气固表作用相吻合,符合黄芪药物作用;黄芪总皂苷提取物1 h时组织内黄芪甲苷含量从高到低顺序可知,在肺中含量较高,符合黄芪药材归经。

Objective:To establish methods for determining AstragalosideⅣin rats plasm by HPLC-UV and study the pharmacokinetics and tissue distribution of AstragalosideⅣin rats.Methods:The rats blood was collected in 0.25,0.5,0.75,1,2,3,4,6,8,10,12,24 h after garaged 0.0022 g·kg-1 Astragalosides extract.Each rat had been garaged 3.5 m L.The rats were executed after collecting blood and tissue samples were collected before garaged(0 h),0.5,1,2 h after garaged 0.0022 g·kg-1 Astragalosides extract which included heart,liver,spleen,stomach,kidney,lung,large intestine,small intestine and other groups.The concentrations of AstragalosideⅣin plasma and tissues were determined by HPLC.Results:AstragalosideⅣof Astragalosides extract metabolism in plasma was found to be active during pharmacokinetic study.Medication had longer survival time than blank rats in process of blood collection.AstragalosideⅣassay of Astragalosides extract metabolism in tissues after 1 h from high to low were:liver>small intestine>lung>heart>stomach>large intestine>spleen>kidney.Conclusion:Astragalosides extract has active cardiotonic effect,being consistent with radix astragali effect of invigorating Qi for consolidating superficies.AstragalosideⅣof Astragalosides extract metabolism in tissues after 1 h from high to low shows higher levels in the lung,which is accorded with radix astragali tropism.