PII-083

R. Zheng,1 B. Kim,1 K. Lee,2 S. Yim3; 1Clinical Pharmacology and Therapeutics, Seoul, Korea, Republic of, 2Department of Pharmaceutical Biochemistry, Seoul, Korea, Republic of, 3Department of Clinical Pharmacology, Seoul, Korea, Republic of

BACKGROUND: A major metabolite of ginseng, compound K, has anti-cancer and anti-inflammatory activities. The objective of this study was to compare the pharmacokinetic profiles of compound K after administered fermented red ginseng extracts (FE), red ginseng extracts (RE) and ginseng extracts (GE) in healthy subjects.
METHODS: A randomized, open-label, single dose, parallel design was conducted in 36 healthy Korean male volunteers. All of the subjects were assigned into three treatment groups, each group received one of the study formulations. Blood samples were collected at 0 (predose), 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, and 24 hr after dosing. The pharmacokinetic parameters were obtained using Phoenix® WinNonlin® 6.2 with non-compartmental methods. The plasma concentrations of compound K were detected by the high-performance liquid chromatography with tandem mass spectrometer. The tolerability was assessed by vital signs and electrocardiograms.
RESULTS: A total of 36 subjects completed the study. The time to maximum plasma concentration (Tmax) for FE, GE and RE were 2.5 hr, 10 hr and 8 hr, respectively. The maximum plasma concentration (Cmax) of compound K was 254.45 ± 51.20 ng/mL (means ± SD) for FE, 5.32 ± 5.30 ng/mL for GE and 3.18 ± 1.70 ng/mL for RE, respectively. The area under the plasma concentration-time curve from time zero to time of last concentration (AUClast) of compound K for FE was 1466.83 ± 295.89 ngh/mL, and that for GE and RE were 33.43 ± 40.59 ngh/mL and 12.73 ± 7.83 ngh/mL, respectively. There were no significant adverse events reported during the study.
CONCLUSION: The study confirmed that the FE has a larger AUClast than GE and RE. All of the study formulations were well tolerated in the subjects.