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The purpose of this study was to investigate the effect of aspirin (5, 10, 20 mg/kg) on the pharmacokinetics of metformin (15 mg/kg) in rabbits. The plasma concentration of metformin was decreased significantly (p<0.05) by co-administration of aspirin (10, 20 mg/kg) compared with control. Area under the plasma concentration-time curve (AUC) of metformin was decreased significantly (p <0.05) by co-administration of aspirin (10, 20 mg/kg) compared with control. Relative bioavailability (R.B%) of metformin by co-administration was 79.3 (5 mg/kg), 57.5 (10 mg/kg) and 62.5 (20 mg/kg). Peak plasma concentration of metformin was significantly (p< 0.05) decreased by co-administration of aspirin (10, 20 mg/kg) compared with control. The elimination rate constant (Kel) of metformin was increased by co-administration of aspirin (10, 20 mg/kg) compared with control. The terminal half-lifes (t1/2) and mean resident time (MRT) of metformin by co-administration of aspirin (10, 20 mg/kg) were decreased significantly (p <0.05) compared with control. It is considered that the significantly decreased plasma concentration and AUC of metformin is due to increase of elimination in urine acidified by co-administration of aspirin. The results suggest that the dosage of metformin should be adjusted
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