Pseudo-ginsenoside GQ is a new semisynthetic ocotillol-type saponin with remarkable anti-myocardial ischemia activity. The purpose of this study was to characterize the pharmacokinetics of pseudo-ginsenoside GQ (PGQ) after sublingual intravenous administration in rats. Rats (n=200) were given 3.0, 12.0, 48.0 mgkg1, and were taken blood at 2, 5, 10, 20, and 40 min and 1, 2, 4, 6, 8, 12, and 24h after drug administration. Ginsenoside Rb1 was used as the internal standard. Serum concentrations of PGQ were determined using HPLC-ELSD. By using the mean concentrations at each time point (n=6), pharmacokinetic parameters were estimated for PGQ using a 2-compartment model with the reciprocal of the predicted concentration as the weight factor. The linear relationship between AUC and the dose of PGQ was obtained in the range of 3.0–48.0 mg • kg1.