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

J Ethnopharmacol. 2012 Jan 31;139(2):664-7. doi: 10.1016/j.jep.2011.11.052. Epub 2011 Dec 9.

Abstract

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.

Publication types

  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Antineoplastic Agents, Phytogenic / adverse effects
  • Antineoplastic Agents, Phytogenic / blood
  • Antineoplastic Agents, Phytogenic / pharmacokinetics*
  • Asian Continental Ancestry Group*
  • Bacteria / metabolism*
  • Chromatography, High Pressure Liquid
  • Cross-Over Studies
  • Fermentation*
  • Humans
  • Intestines / microbiology*
  • Male
  • Middle Aged
  • Models, Biological
  • Panax*
  • Plant Preparations / administration & dosage
  • Plant Preparations / adverse effects
  • Plant Preparations / blood
  • Plant Preparations / pharmacokinetics*
  • Plants, Medicinal
  • Reproducibility of Results
  • Republic of Korea / epidemiology
  • Sapogenins / administration & dosage
  • Sapogenins / adverse effects
  • Sapogenins / blood
  • Sapogenins / pharmacokinetics*
  • Tandem Mass Spectrometry
  • Young Adult

Substances

  • 20-O-(beta-D-glucopyranosyl)-20(S)-protopanaxadiol
  • Antineoplastic Agents, Phytogenic
  • Plant Preparations
  • Sapogenins