Pharmacokinetic comparison of ginsenoside metabolite IH-901 from fermented and non-fermented ginseng in healthy Korean volunteers

Ethnopharrnacological relevance: IH-901 (20-O-beta-D-glucopyranosyl-20(S)-protopanaxadiol) is a novel ginseng saponin metabolite formed by human intestinal bacteria and is known to have antitumor and antimetastatic effects. However, there has been no pharmacokinetic study of IH-901 in human beings. Aim of the study: The aim of this study was to investigate the pharmacokinetic differences of IH-901 from fermented and non-fermented ginseng. Materials and methods: To investigate whether the pharmacokinetics of IH-901 differ between fermented and non-fermented ginseng, an open label, randomized, single dose, fasting, two-period, cross-over, pharmacokinetic study was conducted. A total of 24 healthy Korean male volunteers participated in this study. All subjects were allocated into two equal groups and administered 3g of fermented or non-fermented Panax ginseng. Serial blood samples for pharmacokinetic analysis were collected in the 24h after dosing. Plasma IH-901 concentration was measured by a validated high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Pharmacokinetic parameters including AUC(t), C-max, and T-max were calculated by noncompartmental models in the BA-CALC program (KFDA, 2008, 1.0.0, Korea). Results: After oral administration of fermented ginseng, 5 subjects experienced diarrhea. The means of AUC(t) and C-max were significantly different between the two groups. In the fermented ginseng group, AUC(t) was 2083.09 +/- 91.97 ng h/mL, a 15.5-fold increase over that of IH-901 from the non-fermented group (134.50 +/- 63.10 ng h/mL), and the mean C-max was 325.00 +/- 91.97 ng/mL in the fermented ginseng group, a 27-fold higher value than that in the non-fermented group (13.88 +/- 7.24 ng/mL). T-max was 3.29 +/- 1.00 and 12.04 +/- 4.96 h in the fermented and non-fermented group, respectively. Conclusions: The results of this study showed that the pharmacokinetic parameters of IH-901 from fermented Panax ginseng are different from those of non-fermented ginseng, from which IH-901 is formed by intestinal fermentation. (C) 2011 Elsevier Ireland Ltd. All rights reserved.