OBJECTIVE: To study the effects of Danshen tablets or Danshen injection combination on the pharmacokinetics of doxorubicin in rats in vivo. METHODS: 18 SD rats were randomly divided into group A, B and C. Group A was given doxorubicin 8 mg/kg intravenously via left jugular trunk; group B was given Danshen injection 0.5 ml intravenously via left jugular trunk, and 0.5 h later given doxorubicin 8 mg/kg intravenously via left jugular trunk; group C was given Danshen suspension 1 ml (18 tablets dissolved in 50 ml pure water) intragastrically, and 7 d later given doxorubicin 8 mg/kg intravenously via left jugular trunk. 0.6 ml venous blood were extracted from the right jugular vein 0, 0.083, 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12 and 24 hours after medication. The plasma concentration of doxorubicin was determined by HPLC; the pharmacokinetic parameters were calculated by using 3p97 software; the difference of pharmacokinetic parameters were compared among 3 groups. RESULTS: Compared with group A, CL and Vss of group B increased while AUC0-t ?decreased (P<0.05); Vss of group C decreased (P<0.05), k10 increased and t1/2β decreased. CONCLUSIONS: Danshen tablet/Danshen injection can increase the distribution speed of doxorubicin into tissues, and both can improve the concentration of drug in tumor focus.