桂枝茯苓胶囊主要效应成分在比格犬体内的药代动力学  

Pharmacokinetics of Guizhi Fuling capsule in beagle dogs

作　　者：朱克近[1,2,3] 孙晓萍[1,2,3] 常秀娟[1,2,3] 秦建平[1,2,3] 吕新勇[1,2,3] 王振中[1,2,3] 萧伟[1,2,3] 

机构地区：[1]江苏康缘药业股份有限公司,江苏连云港222001 [2]中药制药过程新技术国家重点实验室,江苏连云港222001 [3]江苏省企业院士工作室,江苏连云港222001

出　　处：《中国中药杂志》2011年第8期1015-1018,共4页China Journal of Chinese Materia Medica

基　　金：国家重大新药创制专项(2009ZX09504-004)

摘　　要：目的：研究桂枝茯苓胶囊中主要成分芍药苷、芍药内酯苷、苦杏仁苷在比格犬体内的药代动力学特征。方法：比格犬口服给予桂枝茯苓胶囊0．0448，0．1792g·kg^-1后，前肢静脉收集血浆样本，经固相萃取小柱富集后，HPLC—MS／MS检测血药浓度，DAS2．0软件计算药代动力学参数。结果：芍药苷、芍药内酯苷、苦杏仁苷体内检测定量限分别为0．25，2．64，0．04μg·L^-1，不同剂量下芍药苷t1/2分别为4．33，3．62h；芍药内酯苷t1/2分别为6．16，5．91h，苦杏仁苷t1／2分别为2．43，1．32h；各成分体内AUC0～t与剂量有较好相关性。结论：芍药苷、芍药内酯苷、苦杏仁苷在体内均有较高暴露量，可用二室模型来描述。Objective： To investigate pharmacokinetic parameters of peoniflorin, albiflorin and amygdaloside after administration of Guizhi Fuling capsule in beagle dogs. Method： Plasma was collected from forelimb vein of Beagle dogs after oral administration of GuizhiFuling capsule. HPLC-MS/MS method was used to determine the concentrations of constituents in plasma. The pharmaeokinetie parameters were analyzed by program DAS 2. 0. Result： The limit of quantitation of peoniflorin, albiflorin and amygdaloside were 0. 25, 2. 64, 0. 04 μg·L^-1, respectively. After administrated with different doses, half-life of peoniflorin in dogs were 4. 33, 3.62 h, albiflorin were 6. 16, 5.91 h, amygdaloside were 2.43, 1.32 h. The AUC0-t of all components were related to dose. Conclusion： The pharmaeokinetie course of peoniflorin, albiflorin and amygdaloside can be described by two-compartment model, and these components have high expose.

关 键 词：芍药苷 芍药内酯苷 苦杏仁苷 桂枝茯苓胶囊 药代动力学 

分 类 号：R285.5[医药卫生—中药学]