Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers

Abstract The effect of a high-fat meal on the oral bioavailability of deramciclane 30 mg tablet was evaluated in 18 healthy male volunteers in a randomised, single dose, two-way crossover study. The drug was administered following an overnight fast or a standardised high-fat breakfast. The plasma concentrations of deramciclane and N -desmethylderamciclane were determined by using a validated HPLC–MS –MS/MS method. An effect of food on the bioavailability was indicated if the 90% confidence interval (CI) for the ratio of geometric means of fed and fasted treatments was not contained in the equivalence limit of 0.8–1.25 for AUC and C max . The ratios of the mean C max and AUC 0–∞ values of deramciclane were 1.24 (90% CI 1.12–1.38) and 1.31 (90% CI 1.21–1.41) in fed versus fasted subjects, which overlapped but exceeded the equivalence limit. In contrast to the parent compound, the 90% CI of the mean ratios for AUC 0–∞ and C max of N -desmethylderamciclane were within the predefined range. The 24 and 31% increase in C max and AUC 0–∞ of deramciclane, respectively, under fed condition is modest and probably has no clinical significance since it is relatively small compared to the inter-individual variability of these parameters.