The objective of the present study was to develop and validate a HPLC method with good sensitivity and specificity for the identification and quantification of trimetazidine in human plasma. Trimetazidine and caffeine (internal standard) were isolated from plasma samples by protein precipitation with methanol. The chromatographic separation was accomplished on a Xterra C18 Column with the mobile phase consisting of potassium di-hydrogen phosphate buffer-acetonotrile-triethylamine (90:10:0.04, v/v) (pH 4.16, adjusted with ortho-phosphoric acid), and the flow rate was set at 1.0 mL/min. Detection was performed on a spectrophotometric detector keeping the retention time at about 8.9 and 10.9 min for caffeine and trimetazidine, respectively. This method was successfully applied for pharmacokinetic studies in 8 healthy male Bangladeshi volunteers. After the administration of a single dose of 35 mg of modified release tablet, the resulting mean of major pharmacokinetic parameters such as AUC0–12, AUC0??, Cmax, Tmax and t1/2 of trimetazidine were 457.8 ± 294.4 ng.h.mL-1, 552.4 ± 386.1 ng.h.mL?1, 87.77 ± 43.17 ng.mL?1, 3 ± 1.49 h and 3.417 ± 1.134 h respectively.