A NEW RAPIDLY DISINTEGRATING FORMULATION OF CISAPRIDE IS BIOEQUIVALENT TO STANDARD CISAPRIDE TABLETS IN THE ELDERLY

Thirty-six healthy, elderly subjects were enrolled in an open-label, r andomised, crossover study to determine the relative bioavailability o f a new, rapidly disintegrating formulation of cisapride (Propulsid(R) Quicksolv(R)) compared with the currently marketed cisapride preparat ion (Propulsid(R)). Subjects received a single 10mg dose of each formu lation, separated by a 1-week washout period. Blood samples for determ ination of cisapride concentrations were taken regularly until 48 hour s after drug administration. After ingestion of Propulsid(R) Quicksolv (R), the log-transformed least square means value for area under the p lasma concentration-time curve up to the last measurable time-point (A UC(last)) was 444.9 mu g/L.h, AUC extrapolated to infinity (AUC(infini ty)) was 488.8 mu g/L.h, and maximum plasma drug concentration (C-max) was 43.3 mu g/L. After ingestion of Propulsid(R), the corresponding v alues were 449.1 mu g/L.h, 513.7 mu g/L.h, and 43.9 mu g/L, respective ly. The limits of the 90% confidence intervals for these log-transform ed parameters were all within the range set to declare bioequivalence (80 to 125%). Mild to moderately severe gastrointestinal symptoms occu rred in one subject after administration of Propulsid(R) Quicksolv(R). Neither formulation was orally irritating, and no clinically signific ant changes in vital signs, ECGs or laboratory test parameters were no ted. The 10mg Propulsid(R) Quicksolv(R) tablet was bioequivalent to th e marketed Propulsid(R) tablet in healthy, elderly subjects and was al so a convenient, well-tolerated alternative to the Propulsid(R) tablet .