Bioequivalence of Rebamipide in Korean

Primary Outcome Measures:

• Serum concentration of rebamipide [ Time Frame: Pre-dose (to serve as a control) and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, and 12 hours after oral administration of rebamipide tablet (100 mg) ]
  

Secondary Outcome Measures:

• Genetic polymorphisms in ABCB1 gene (exon 21 and 26) [ Time Frame: A 3-mL blood sample was taken from each subject who participated in our bioequivalence studies before administration of rebamipide. ]
  

A randomized, single-dose, 2-period crossover design with a 7-day washout period was conducted in 30 healthy Korean male volunteers. Subjects were randomly assigned to receive a single 100-mg dose of the test or reference preparation of rebamipide, administered with 240 mL of water after a 12-hour overnight fast. All subjects were selected after passing a clinical screening procedure that included a physical examination and laboratory tests. Serum concentrations of rebamipide up to 12 hours after administration were determined using a validated HPLC method with fluorescence detection. Adverse events (AEs) were continuously monitored by clinical staff via observation, personal interview, and vital signs (temperature, blood pressure, heart rate) during the study period. All adverse events were recorded on the clinical record form per subject up to 1 week after the study. Pharmacokinetic parameters were determined using a noncompartmental method. The preparations were considered bioequivalent if the log-transformed ratios of AUC0-t, AUC0-∞, and Cmax were within the predetermined bioequivalence range (ie, 80-125%), as set by the US Food and Drug Administration (FDA) and Korean legislation. In vitro dissolution profiles of both preparations were examined and the influence of genetic polymorphisms in ABCB1 gene (P-glycoprotein) on the pharmacokinetics of rebamipide was also investigated.