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类叶升麻苷在大鼠体内的药代动力学研究 被引量:9

Pharmacokinetic study on acetoside in rats
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摘要 目的:建立类叶升麻苷血药浓度的高效液相色谱测定方法,并探讨其在大鼠体内的药代动力学特点。方法:SD大鼠6只,灌胃类叶升麻苷150 mg·kg-1后,于不同时间点采血,采用反相高效液相色谱法测定其血药浓度变化,并用DAS2.0软件拟合并计算药动学参数。结果:类叶升麻苷血药浓度的回归方程为Y=3.509 8X-0.096 8,r=0.996 8,在0.125~2.5mg·L-1线性关系良好。方法回收率均大于85%,日间及日内精密度的RSD均小于15%,符合生物样品分析要求。大鼠灌胃给药150 mg·kg-1的类叶升麻苷后,血浆中的类叶升麻苷的药时曲线呈二室开放模型,主要药动学参数Tmax,Cmax,t1/2α,t1/2β,AUC0-t,AUC0-∞,CL/F,V/F,Ka分别为0.361 h,1.126 mg·L-1,0.759,4.842 h,3.134,3.766 mg·h·L-1,87.089 L·h-1·kg-1,207.704 L·kg-1,6.345 h-1。结论:建立了类叶升麻苷血药浓度方法,该方法专属性强,灵敏度高,可用于该药的体内定量分析。 Objective: To establish a HPLC method for determining acetoside in rat plasma and to investigate the pharmacokinetic characteristics of acetoside in rats. Method: Six rats were orally administered with 150 mg · kg^- 1 acetoside and their blood samples were collected at different time points. The plasma concentration of acetoside was determined by reserved HPLC, and the pharma- cokinetic parameters were calculated by DAS 2. 0 software. Result: The regression equation of acetoside in rats plasma was Y = 3. 509 8X-0. 096 8 (r =0. 996 8), which showed a good linear relation at 0. 125-2.5 mg · L^-1. The method showed a recovery of more than 85 % , and both inter-day and intra-day RSDs were less than 15 %. After the oral administration of 150 mg · kg^- 1 acetoside, the concentration-time curves of acetoside were expressed in a open two-compartment model. The main pharmacokinetics parameters of T, C t1/2α, tl/2β, AUC0., , AUC0-1, CL/F, V/F and Ka were respectively 0. 36 h, 1. 126 mg · L^-1 , 0. 759, 4. 842 h, 3. 134 3. 766 mg ·h · L^-1, 87.089 L · h ^-1· kg ^-1, 207. 704 L · kg^-1 and 6. 345 h^-1 respectively. Conclusion: It is first time to establish such a HPLC method to determine the concentration of acetoside in plasma. The method is so highly specified and sensitive that it can be used in quantitative analysis in vivo on acetoside.
出处 《中国中药杂志》 CAS CSCD 北大核心 2012年第21期3312-3315,共4页 China Journal of Chinese Materia Medica
基金 新疆维吾尔自治区高技术研究发展计划项目(201110104)
关键词 类叶升麻苷 HPLC 药代动力学 大鼠 acetoside HPLC pharmacokinetics rat
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