OBJECTIVE: To study the pharmacokinetics of the active ingredients of Shenmai injection, including ginsenoside Rg1 and ginsenoside Re, in normal Beagle dogs and those with myocardial ischemia. METHODS: 6 Beagle dogs were given isoproterenol hydrochloride (1.1 mg/kg) sc to establish the model of myocardial ischemia (model group). Another 6 Beagle dogs were given isometric normal saline (2.2 ml/kg) sc as controls group. The two groups of dogs respectively received corresponding drugs sc at 8:00 am and 13:00 pm on day 1 and at 8:00 am on day 2. Each group of dogs were given Shenmai injection (1.6 ml/kg) iv 1 h after administration on day 2, and such intravenous drip lasted for about 1 h. Blood was collected from each group 0,0.25, 0.5, 0.75, 1 (the end of iv), 1.5, 2, 3, 4, 6, 8, 12 and 24 h from the start of iv. Liquid chromatography-mass spectrometry was adopted to determine the concentrations of ginsenoside Rg1 and ginsenoside Re in blood, and WinNonlin 6.3 was used to calculate pharmacokinetic parameters for comparison. RESULTS: For ginsenoside Re in the dogs of the model group, t1/2 was (2.69±1.12) h, AUC0-24 h was (2 060.78±812.18) h·μg/L, Vz was (46.16±20.98) ml and CL was (9.02±4.45) ml/h; compared to the normal control group, AUC0-24 h was much greater and Vz and CL were significantly lower, showing a statistically significant difference (P<0.05). No significant difference in the pharmacokinetic parameters of ginsenoside Rg1 was shown between 2 groups(P>0.05). CONCLUSIONS: Myocardial ischemia may affect the removal of ginsenoside Re in Beagle dogs, but has no effect on the pharmacokinetic process of ginsenoside Rg1.