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

作　　者：田秀峰[1,2] 李鹏跃[3] 王宏洁[3] 边宝林[3] 杜守颖[1] 杨健[3] 

机构地区：[1]北京中医药大学,北京100102 [2]炎黄东方(北京)健康科技有限公司,北京100024 [3]中国中医科学院中药研究所,北京100700

出　　处：《中国中药杂志》2012年第16期2461-2464,共4页China Journal of Chinese Materia Medica

基　　金：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)

摘　　要：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 geni- poside was 1.24-158.88 mg .L-1. The main pharmaeokinetic 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 .rain . L-1 ,MRT（llS. 7 ±25.4） rain, and these parameters alter 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 meth- od 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：醒脑静 栀子苷 药代动力学 生物利用度 

分 类 号：R285[医药卫生—中药学]