Abstract: OBJECTIVE To study the pharmacokinetics changes of the active compounds of Shengmai injection (including ginsenoside Rg₁, ginsenoside Re and schizandrin) in normal and myocardial ischemia Beagle dogs. METHODS Agilent ZORBAX SB-C₁₈ chromatography column was applied. The gradient mobile phase was HCN-H₂O system. Ginsenoside Rg₁, ginsenoside Re and schizandrin were detected by the positive electrospray ionization method under single ion monitoring (SIM) mode. The pharmacokinetic parameters of different active compounds were analyzed by WinNonlin 6.3 software and SPSS 19.0. RESULTS After modeling, the values of T_1/2 of ginsenoside Rg₁ showed shorter. The apparent volume of ginsenoside Re showed larger, and the values of renal clearance reduced. The values of T_1/2, mean residence time and apparent volume of schizandrin showed higher, while the values of renal clearance of schizandrin reduced. CONCLUSION After injecting Shengmai injection, the pharmacokinetics results obtained from this study show that the pharmacokinetics of ginsenoside Rg₁, ginsenoside Re and schizandrin in Beagle dogs of myocardial ischemia are significantly different from normal dogs.