白及多糖配伍对三七总皂苷中10种成分药动学的影响

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(P0.01),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(P0.01)。与P组相比,BP组人参皂苷Rg1的Cmax降低(P0.05)。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(P0.01),人参皂苷Rg2和三七皂苷R1延迟(P0.05)。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。

Effect of Bletilla striata polysaccharides on pharmacokinetics of 10 components in Panax notoginseng saponins

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 t_max of Rg₁, Rb₁, and Rf significantly delayed (P<0.01); The t_max 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 t_max. This illustrates that BSP may increase the exposure levels of PNS in the gastrointestinal tract so that increase the effect in the gastrointestinal tract.