黄芪甲苷在大鼠体内的药代动力学和组织分布研究  

Pharmacokinetics and tissue distribution of astragaloside Ⅳ in rats

作　　者：陈宁[1] 张琪[1] 杜宇[1] 陈国广[1] 朱玲玲[1] 

机构地区：[1]南京工业大学制药与生命科学学院,南京210009

出　　处：《生物加工过程》2006年第3期67-72,共6页Chinese Journal of Bioprocess Engineering

摘　　要：建立了固相萃取-HPLC-MS测定大鼠血浆中黄芪甲苷含量的方法,并对其在大鼠体内的药代动力学和组织分布进行了研究。分别以1,2,4 mg/kg的剂量对大鼠静脉给药,给药后2,10,20,30,60 min和1.5,2,3,4,6,8 h采集血样,同时以2 mg/kg的剂量对大鼠静脉给药,给药后20,60,240 min采集各组织,测定血浆样品和组织样品中的黄芪甲苷浓度。血药浓度-时间曲线按二室模型拟合最佳,t1/2(α)分别为12.36,7.05,15.98 min,t1/2(β)分别为69.14,73.28,95.24 min,AUC分别为277.36,415.36,623.15μg.min/mL,AUC与剂量的线性方程为y=113.64x+173.47(r=0.997),表明黄芪甲苷在大鼠体内呈线性消除。组织分布研究表明黄芪甲苷在体内分布较广。The method of solid extraction and HPLC-MS for quantitative analysis Astragaloside Ⅳ in rat plasma was developed, and the pharmacokinetics and tissue distribution of Astragaloside Ⅳ in rats was studied. The rats blood was collected in 2,10,20,30,60 rain and 1.5,2,3,4,6,8 h after iv 1,2 and 4 mg/kg Astragaloside Ⅳ, and tissue samples were collected at 20,60,240 min after iv 2 mg/kg of Astragaloside Ⅳ. The concentration of Astragaloside Ⅳ in plasma and tissues were determined by HPLC-MS. The rat plasma concentration- time curves were fitted to 2-compartments model. The t1/2（α） were 12.36,7.05,15.98 min, respectively. The t1/2（β） were 69.14,73.28,95.24 min respectively and the AUC were 277.36,415.36,623.15μg· min/mL, respectively. The linear equation for AUC and dosage was y = 113.64x ＋ 173.47 （r = 0.997）. It indicated that Astragaloside Ⅳ was eliminated linearly in rats. The Astragaloside Ⅳ distribution in tissue showed that Astragaloside Ⅳ was widely distributed in vivo.

关 键 词：黄芪甲苷 固相萃取 液相色谱-质谱联用 药代动力学 组织分布 

分 类 号：R969.1[医药卫生—药理学] R286[医药卫生—药学]