Pharmacokinetic Studies of Multi-bioactive Components in Rat Plasma After Oral Administration of Xintiantai Ⅰ Extract and Effects of Guide Drug Borneol on Pharmacokinetics

Objective: To investigate the pharmacokinetic characteristics of 17 bioactive components including ginsenoside Rg1, Rb1, Rd, berberine, epiberberine, jatrorrhizine, 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 borneol extract powder (XI without borneol), and study the compatibility effects of guide drug borneol 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 borneol 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 borneol can significantly increase AUC of G-Rd, palmatine, hyperin, curcumin, demethoxycurcumin, bisdemethoxycurcumin and of 16 bioactive components except for dehydroevodiamine ( < 0.05), decrease of G-Rd, berberine, columbamin, coptisine, limonin and MRT of 17 bioactive components in XI group ( < 0.05).

Conclusion: Guide drug borneol enhanced the absorption of G-Rd, palmatine, hyperin, curcumin, demethoxycurcumin and bisdemethoxycurcumin.