Aim To investigate the pharmacokinetic characteristics of schizonepetin and its bioavailability in rats.Methods An HPLC method was established to analyze the plasma concentration of schizonepetin with different intragastric and intravenous administration doses to rats.Pharmacokinetic parameters were calculated by noncompartmental model in Kinetica 4.4.Results The Cmax and AUC0-∞ showed non-linearrelation after intragastric administration of 47.87,23.94 and 11.97 mg·kg-1.The Cmax and AUC0-∞ after intravenous administration of 11.97 mg·kg-1 were 6.5 mg·L-1 and 18 mg·h·L-1.And the absolute bioavailability was 69.1 %.Conclusion This method for the pharmacokinetic and absolute bioavailability study of schizonepetin in rats is simple,rapid and accurate.