Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract

Hyung-Ki Kim, Hyung-Ki Kim

Abstract

Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro. However, previous studies have focused on the pharmacokinetics of a single metabolite or the parent compound and have not described the pharmacokinetics of both compounds in humans. To investigate the pharmacokinetics of ginsenoside Rb1 and compound K, we performed an open-label, single-oral dose pharmacokinetic study using Korean Red Ginseng extract. We enrolled 10 healthy Korean male volunteers in this study. Serial blood samples were collected during 36 h after Korean Red Ginseng extract administration to determine plasma concentrations of ginsenoside Rb1 and compound K. The mean maximum plasma concentration of compound K was 8.35±3.19 ng/mL, which was significantly higher than that of ginsenoside Rb1 (3.94±1.97 ng/mL). The half-life of compound K was 7 times shorter than that of ginsenoside Rb1. These results suggest that the pharmacokinetics, especially absorption, of compound K are not influenced by the pharmacokinetics of its parent compound, except the time to reach the maximum plasma concentration The delayed absorption of compound K support the evidence that the intestinal microflora play an important role in the transformation of ginsenoside Rb1 to compound K.

Keywords: Compound K; Ginsenoside Rb1; Panax ginseng; Pharmacokinetics.

Figures

Fig. 1.. Representative analytical chromatogram of ginsenoside…
Fig. 1.. Representative analytical chromatogram of ginsenoside Rb1 (A), compound K (B), and the internal standard (C).
Fig. 2.. Mean plasma concentration-time curve of…
Fig. 2.. Mean plasma concentration-time curve of ginsenoside Rb1 and compound K after oral administration of Korean Red Ginseng extract in 10 healthy male Korean subjects. ● Plasma ginsenoside Rb1 (Rb1) concentration, ▲ plasma compound K (C-K) concentration.
Fig. 3.. Correlation between the time to…
Fig. 3.. Correlation between the time to reach maximum concentration (Tmax) of plasma ginsenoside Rb1 (Rb1) and compound K (C-K) after oral administration of Korean Red Ginseng extracts in 10 healthy male Korean subjects.

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