Abstract: OBJECTIVE To evaluate the effects of high-fat diet on the pharmacokinetics of dipyridamole in Chinese healthy adult subjects. METHODS All of 75 healthy subjects were assigned to receive single dose of dipyridamole tablet 25 mg in either fasting or high-fat diet state, and blood samples were taken at different time points, respectively. Plasma concentrations of dipyridamole were determined by HPLC-MS/MS. RESULTS The main pharmacokinetic parameters of dipyridamole in fasting state and high-fat diet state were as follows: C_max were (594.69±172.14) and (333.64±167.18) ng·mL^-1, fasting C_max decreased by 43.9%(P<0.01); t_1/2were (9.87±4.21) and (10.57±3.75) h; AUC_0-twere (1 733.22±715.49) and (1 268.61±571.07) ng·mL^-1·h; AUC_0-∞ were (1 801.69±707.61) and (1 353.64±602.29) ng·mL^-1·h; AUC_0-t and AUC_0-∞ decreased by 26.8% and 24.9% respectively after meals compared with fasting(P<0.01), median T_max (range) were 0.750.50, 5.00 h and 1.500.49, 4.52 h. CONCLUSION Compared with fasting condition, C_max,AUC_0-t and AUC_0-∞ were significantly decreased after taking the medication after lipid diet, and T_max was significantly delayed, indicating that food has a significant effect on the absorption rate and degree of dipyridamole tablets.