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作 者:王灯节 狄留庆[1,2,3] 康安[1,2,3] 李俊松[1,2,3] 丁宁[1] 钱文娟[1] WANG Deng-jie DI Liu-qing KANG An LI Jun-song DING Ning QIAN Wen-juan(College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China Jiangsu Engineering Research Center for Efficient Delivery System ofTCM, Nanjing 210023, China Nanjing Engineering and Technology Research Center for TCM Pellets, Nanjing 210029, China)
机构地区:[1]南京中医药大学药学院,江苏南京210023 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210023 [3]南京市中药微丸产业化工程技术研究中心,江苏南京210029
出 处:《中草药》2017年第4期737-746,共10页Chinese Traditional and Herbal Drugs
基 金:国家自然科学基金资助项目(81273655);江苏省"333高层次人才培养过程"资助项目(BRA2013201);江苏高校优势学科建设工程资助项目(ysxk-2010);江苏省"青蓝工程"创新团队支持计划资助(QLP)
摘 要:目的建立UPLC-MS/MS法同时测定三七总皂苷中10种皂苷成分的分析方法,并研究白及多糖对三七总皂苷各成分药动学参数的影响。方法大鼠分为三七总皂苷组(P组)、三七总皂苷配伍白及多糖组(BP组),分别ig给药,UPLC-MS/MS法测定10种皂苷单体成分的血药浓度,DAS软件计算各成分药动学参数。结果分析方法符合生物样品测定要求。与P组相比,BP组人参皂苷Rb1的AUC显著降低(P<0.01),三七皂苷R1及人参皂苷Rd、Rg1、Rf、CK、Rc、Rh1、Rg2、Rg3的AUC有所降低,但无显著性差异。10种成分总AUC为P组>BP组,差异显著(P<0.01)。与P组相比,BP组人参皂苷Rg1的Cmax降低(P<0.05)。且BP组各成分的tmax普遍延迟,其中人参皂苷Rg1、Rb1、Rf显著延迟(P<0.01),人参皂苷Rg2和三七皂苷R1延迟(P<0.05)。结论所建立的UPLC-MS/MS分析方法适于10种皂苷成分在生物样品中的测定;配伍白及多糖可降低三七总皂苷的血药浓度,减少AUC暴露,延长tmax,说明白及多糖可能增加了三七总皂苷在胃肠道的暴露水平,从而增加作用于胃肠道的药效。Objective To establish a UPLC-MS/MS method for simultaneous determination of 10 components in Panax notoginseng saponins (PNS), and the study the effect of Bletilla striata polysaccharides (BSP) on the pharmacokinetic parameters of PNS. Methods Rats were divided into PNS group (P group) and PNS-BSP compatibility group (BP group) by ig administration. The plasma concentration of 10 saponins was determined by UPLC-MS/MS. The pharmacokinetic parameters were calculated by DAS software. Results The determination method corresponded to the biological sample measurement requirements. Compared with P group, the AUC of Rb1 significantly reduced in BP group (P〈0.01) and the AUCs of notoginsenoside R1, Rg1, Rf, Rd, CK, Rc, Rh1 were lower but without significant difference; The total AUC of 10 components significantly reduced in BP group (P〈0.01); The plasma concentration of Rg1 in BP group was lower compared with that in P group (P〈0.05); The tmax of Rg1, Rb1, and Rf significantly delayed (P〈0.01); The tmax of notoginsenoside R1 and Rg2 delayed compared with P group (P〈0.05). Conclusion The established UPLC-MS/MS analysis method is suitable for the simultaneous determination of 10 components in PNS in rat plasma; PNS-BSP compatibility can reduce the plasma concentration of PNS and AUC exposure and prolong the tmax. This illustrates that BSP may increase the exposure levels of PNS in the gastrointestinal tract so that increase the effect in the gastrointestinal tract.
关 键 词:三七总皂苷 白及多糖 药动学 三七皂苷R1 人参皂苷Rg1 人参皂苷RG2 人参皂苷Rg3 人参皂苷Rc 人参皂苷RD 人参皂苷Rf 人参皂苷CK 人参皂苷RH1 人参皂苷Rb1
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