A previous study reported that ginsenoside Rd (GRd) after oral administration has a valuable effect against 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced recurrent ulcerative colitis. In this study, we use HPLC method to investigate the oral bioavailablity of GRd and found that GRd was very poorly absorbed following oral administration in vivo. Simultaneously, the amount of GRd was degraded 71.77 +/- 4.8% in the gastric juice, the amount of GRd in the colon 6 h after oral administration was 19.8 +/- 13.7% of the given dose. In further experiment, we found 81.25 +/- 9.74% of the given dose of GRd in the colon of mice after duodenal administration. GRd was detected and stable in the intestine contents of mice. These pharmacokinetic characteristics suggested that GRd affected the ulcerative colitis directly other than its a few other metabolic products. So that, it has a natural colon-targeting feature and it may be possibly developed as a therapeutic agent to inflammatory bowel disease.