In vitro simulation of food effect on dissolution of deramciclane film-coated tablets and correlation with in vivo data in healthy volunteers

The in vitro dissolution profiles of deramciclane 30 mg film-coated tablets, an acid-labile new 5-HT receptor antagonist, were studied under simulated fasting and fed conditions. Artificial gastric juice with pH adjusted to that of fasting conditions was applied either alone or after adding different dietary components. The use of the USP dissolution apparatus 11 (paddle method) showed that the presence of dietary components has markedly affected the amount of unchanged drug dissolved. As a similar tendency bad been observed in food-effect studies in healthy volunteers, cumulative area under the curve (AUC(cum)) for both fed and fasting conditions were compared and an in vitro-in vivo correlation (IVIVC) was evaluated. A linear relationship was established between logarithmic in vivo blood sampling tune and in vitro dissolution time assigned to equal AUC(cum) ratios (AUC(cum), (fed)/AUC(cum), (fasting)). Despite its limitations. in vitro modelling of in vivo conditions might help provide a base for predicting in vivo drug behaviour. (C) 2002 Published by Elsevier Science B.V.