Objective:To investigate the in vivo pharmacokinetic characteristics of 17 bioactive components including ginsenoside Rg1,Rb1,Rd,berberine,epiberberine,jatrorthizine,palmatine,columbamine,coptisine,evodiamine,dehydroevodiamine,rutaecarpine,limonin,hyperin,curcumin,demethoxycurcumin and bisdemethoxycurcumin in rat plasma after oral administration of Xintiantai I extract powder (Ⅺ) and Xintiantai I without guide drug beol extract powder (Ⅺ without beol),and study the compatibility effects of guide drug beol on the pharmacokinetics.Methods:A UHPLC-MS/MS method was established and fully validated for the comparative pharmacokinetics of 17 bioactive components.The pharmacokinetics parameters of 17 bioactive components after oral administration of Ⅺ and Ⅺ without beol were calculated by the software of DAS 3.0 and intercompared.Results:The specificity,linearity,lower limit of quantification (LLOQ),precision,accuracy,extraction recovery rates,matrix effects,and stability of the UHPLC-MS/MS assay were good within the acceptance criteria from FDA guidelines.Guide drug beol can significantly increase AUC of G-Rd,palmatine,hyperin,curcumin,demethoxycurcumin,bisdemethoxycurcumin and Cmax of 16 bioactive components except for dehydroevodiamine (P ＜ 0.05),decrease Tmax of G-Rd,berberine,columbamin,coptisine,limonin and MRT of 17 bioactive components in Ⅺ group (P ＜ 0.05).Conclusion:Guide drug beol enhanced the absorption of G-Rd,palmatine,hyperin,curcumin,demethoxycurcumin and bisdemethoxycurcumin.