毛蕊花糖苷在大鼠、比格犬体内的药代动力学比较  

Comparison of Pharmacokinetics after Administration of Acteoside in Rat and Beagle Dog

作　　者：霍仕霞 高莉 彭晓明 李建梅 陈西敬[2] 文彦丽[2] 闫明 

机构地区：[1]新疆维吾尔自治区维吾尔医药研究所新疆维吾尔医方剂学实验室,新疆乌鲁木齐830049 [2]中国药科大学药物代谢与动力学研究中心,江苏南京211198

出　　处：《中国现代中药》2016年第10期1273-1278,1304,共7页Modern Chinese Medicine

基　　金：新疆维吾尔自治区科研机构创新发展专项资金(2015007)

摘　　要：目的:采用LC-MS/MS法测定毛蕊花糖苷单次、多次给药后在大鼠和比格犬血浆中的浓度,并对其在两种动物体内的药代动力学特征进行比较。方法:SD大鼠单次、多次灌胃给予毛蕊花糖苷40 mg·kg-1和静脉注射10 mg·kg-1,比格犬单次、多次灌胃给予毛蕊花糖苷20 mg·kg-1和静脉注射5 mg·kg-1后,于不同时间点采血,用DAS 2.0软件拟合并计算药代动力学参数。结果:毛蕊花糖苷在大鼠和比格犬体内吸收符合一级动力学,比格犬的达峰时间和最大血药浓度是大鼠的两倍多,比格犬吸收的速率和清除率明显小于大鼠;表观分布容积结果表明毛蕊花糖苷在大鼠某一脏器组织有特异性分布,在比格犬体内无特异性分布;比格犬血药浓度-药时曲线下面积较大鼠的高,表明毛蕊花糖苷在比格犬体内吸收程度较高,药物滞留时间也较长。结论:毛蕊花糖苷在大鼠和比格犬体内的药代动力学特征差异较大。Objective： The plasma concentration of acteoside in rats and beagle dogs were determined by LC-MS/MS, and the pharmacokinetics in rats and beagle dogs were compared. Methods： SD rat were given 40 mg· kg-1 acteoside in single and multiple doses via ig, and given 10 mg·kg-1 acteoside via iv. Beagle dog were given 20 mg·kg-1 acteoside in single and multiple doses via ig, and given 5 mg· kg-1 acteoside via iv. Blood samples were collected at different times after administration. The pharmacokinetics were calculated by DAS 2.0 program. Results： The character of acteoside is the firstorder kinetics in rats and beagle dogs, the peak time （Tmax） and peak concentration （ Cmax ） of beagle dogs were higher than those of rats significantly, absorption rate and clearance of beagle dogs were significantly lower than rats＇; The results of apparent volume of distribution （V/F） indicated that acteoside has specific distribution in certain organs of rats＇, but not in beagle dogs. The area under concentration-time curve （AUC） of beagle dogs were higher than rats＇ , it showed that absorption extent and residence time of acteoside in beagle dogs were all higher than rats＇. Conclusion： The pharmacokinetic characteristics of acteoside were quite differences in rats and beagle dogs.

关 键 词：毛蕊花糖苷 大鼠 比格犬 单次给药、多次给药 比较 

分 类 号：R971.9[医药卫生—药品]