中国中药杂志

2012, v.37(16) 2461-2464

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醒脑静口服给药栀子苷在Beagle犬体内的药代动力学研究
Pharmacokinetics and bioavailabilities of geniposide in Beagle dogs after oral administration Xingnaojing

田秀峰;李鹏跃;王宏洁;边宝林;杜守颖;杨健;
TIAN Xiufeng1,3,LI Pengyue2,WANG Hongjie2,BIAN Baolin2,DU Shouying1,YANG Jian2(1.Beijing University of Chinese Medicine,Beijing 100102,China; 2.Institute of Chinese Materia Madica,China Academy of Chinese Medical Sciences,Beijing 100700,China; 3.Yanhuang Dongfang(Beijing) Healthcare Technology Co.,Ltd.,Beijing 100024,China)

摘要(Abstract):

目的:建立Beagle犬血浆中栀子苷的高效液相色谱分析方法,研究醒脑静口服给药后栀子苷的药代动力学特征及生物利用度。方法:Beagle犬分别口服、注射给予醒脑静,采用HPLC测定Beagle犬血浆中栀子苷浓度,以Kinetica软件拟合,计算相关药动学参数。结果:Beagle犬血浆中栀子苷在1.24~158.88 mg.L-1线性关系良好,口服给药的主要药动学参数为Cmax(11.8±0.6)mg.L-1,Tmax(52.0±4.5)min,AUC(1 280.8±172.0)mg.min.L-1,MRT(118.7±25.4)min。注射给药的药动学参数为Cmax(107.4±6.3)mg.L-1,AUC(7 930.1±670.0)mg.min.L-1,MRT(92.4±5.1)min。生物利用度为(6.46±0.87)%。结论:该实验建立的Beagle犬血浆中栀子苷的HPLC分析方法,适用性良好,提取、方法回收率和日内、日间精密度均符合要求,室温及冻融条件下稳定性良好。醒脑静口服给药栀子苷的生物利用度较低。
Objective: To establish a method for determination of geniposide in Beagle dogs plasma by high performance liquid chromatography(HPLC),and study the pharmacokinetics and bioavailability of geniposide in Beagle dogs after oral administration Xingnaojing.Method: To determine the geniposide in Beagle dogs plasma by HPLC after oral administration or intravenous injection Xingnaojing,and the pharmacokinetic parameters were calculated by the software of Kinetica.Result: The good linearity range of geniposide was 1.24-158.88 mg·L-1.The main pharmacokinetic parameters after oral administration was as follows: Cmax(11.8±0.6) mg·L-1,Tmax(52.0±4.5) min,AUC(1 280.8±172.0) mg·min·L-1,MRT(118.7±25.4) min,and these parameters after intravenous injection was follows: Cmax(107.4±6.3) mg·L-1,AUC(7 930.1±670.0) mg·min·L-1,MRT(92.4±5.1) min.The bioavailability of geniposide in Beagle dogs after oral administration Xingnaojing was(6.46±0.87)%.Conclusion: The HPLC method had good applicability.The extract recovery,method recovery,intra-day precision and inter-day precision of the method were all met the requirements.The stability in conditions of room temperature and freeze-thaw cycle was good.The results indicated that the oral administration bioavailability of geniposide was in low degree.

关键词(KeyWords): 醒脑静;栀子苷;药代动力学;生物利用度
Xingnaojing;geniposide;pharmacokinetics;bioavailability

Abstract:

Keywords:

基金项目(Foundation): 国家“重大新药创制”科技重大专项(2009ZX09502-008);; 国家自然科学基金面上项目(81073057);; 教育部博士点基金项目(20090013110007);; 北京中医药大学复方中药制药创新团队(2011-CXTD-13)

作者(Author): 田秀峰;李鹏跃;王宏洁;边宝林;杜守颖;杨健;
TIAN Xiufeng1,3,LI Pengyue2,WANG Hongjie2,BIAN Baolin2,DU Shouying1,YANG Jian2(1.Beijing University of Chinese Medicine,Beijing 100102,China; 2.Institute of Chinese Materia Madica,China Academy of Chinese Medical Sciences,Beijing 100700,China; 3.Yanhuang Dongfang(Beijing) Healthcare Technology Co.,Ltd.,Beijing 100024,China)

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