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The aim of the present study was to investigate the effect of sucralfate pretreatment on the pharmacokinetics of rosiglitazone following a single oral dose in healthy male volunteers. After an overnight fast, and according to a randomized schedule, each volunteer (n = 9) received a single oral dose of rosiglitazone 8 mg (Avandia® tablets, 4 mg × 2) with or without pretreatment of sucralfate 2 g (Recolfate® tablets, 1 g × 2) in an open‐label crossover study with a 2‐week washout period. Plasma samples were collected over a period of 24 hours at regular intervals. Safety assessment included monitoring of the vital signs, blood parameters, and ECG. No statistically significant differences (p > 0.05) were observed for any of the calculated rosiglitazone pharmacokinetic parameters in the two treatment groups. The mean parameters, AUC_0‐∞ and C_max, following rosiglitazone administration alone were 3825.02 ng·h/ml and …