Enhancing effect of borneol on pharmacokinetics of ginsenoside Rb₁, ginsenoside Rg₁, and notoginsenoside R₁ in healthy volunteers after oral administration of compound Danshen dropping pills

Abstract

Borneol (Bingpian), a monoterpenoid pharmaceutical ingredient, is commonly used as a main composition in traditional Chinese medicine preparations such as compound Danshen dropping pills (CDDP) and has also been approved by the U.S. Food and Drug Administration as a flavoring substance or adjuvant in food. Borneol plays a regulating and guiding role as a messenger drug in CDDP. However, the effect of borneol on the pharmacokinetics of the components of CDDP in human plasma is unclear. In this study, we investigate the effects of borneol on the pharmacokinetics of ginsenoside Rb 1 (Rb 1 ), ginsenoside Rg 1 (Rg 1 ), and notoginsenoside R 1 (NR 1 ) in CDDP. We used a double-cycle crossover-administration model in 12 healthy male volunteers, administered CDDP with borneol (drug T) and without borneol (drug R).The selective response monitoring mode was used for MS quantification in the positive mode. As a result, we found that borneol could significantly affect the pharmacokinetic parameters of notoginsenosides and increase the absorption and systemic exposure of Rb 1 , Rg 1 , and NR 1 in human plasma by $1.85-3.71 times.