ETHNOPHARMACOLOGICAL 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 24 h 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.
RCT Entities:
ETHNOPHARMACOLOGICAL RELEVANCE: IH-901 (20-O-beta-D-glucopyranosyl-20(S)-protopanaxadiol) is a novel ginsengsaponin 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 24 h 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.