Aim To investigate the pharmacokinetics and excretion of cryptotanshinone in pigs which had the obvious antibacterial and anti-inflammatory activity. Methods The plasma concentration of ryptotanshinone was determined by high performance liquid chromatography with dibenyl as a internal standard at absorption wavelength of 254 nm. A mixture of methanol and water (85: 15) was used as the mobile phase with a flow rate of 1 mL min-1, The concentration-time profile of cryptotanshinone was found to be best fitted to a first order absorption two compartment open model after iv a single dose (10mg kg-1) in pigs. Results The main pharmacokinetic parameters of cryptotanshinone were as follows: t1/2α 2.36 h, t1/2β 64.78 min, AUC 23.83 mg min L-1, V1 3.47 L mg-1,VB 45.25 L kg-1.The excretion of cryptotanshinone in porcine urine in 24-48 hour was very few after i.v. a administration of cryptotanshinone. Conclusion The results provide important information for the clinical use of cryptotanshinone and for developing the novel antibacterial drug.