Bioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers.

Objective: To compare the pharmacokinetics of the extended-release MMX (R) formulation of budesonide (Uceris (R)) with that of Entocort (R) EC, an extended (controlled ileal) release formulation of budesonide. Methods: Using an open-label, randomized, three-period crossover, Latin square design, healthy male or female volunteers received single doses of 6 mg Uceris (R), 9 mg Uceris (R) or 9 mg Entocort (R) EC. Standard pharmacokinetic parameters were assessed. Results: The study included 12 subjects. The 9 mg Uceris (R) and 9 mg Entocort (R) EC formulations had comparable area under the concentration-time curve (AUC) data, but 9 mg Uceris (R) had a notably longer time to first appearance in plasma (median T-lag, 6 h versus 1 h, respectively), and a delayed time to maximum concentration (median T-max, 15 h versus 5 h, respectively) compared with 9 mg Entocort (R) EC. The ratio of log-transformed AUC(0-last) (Uceris (R)/Entocort (R) EC) was 91% (90% confidence interval [CI] 77%, 108%) and the corresponding maximum concentration ratio was 79% (90% CI 63%, 100%). Conclusion: Uceris was associated with a similar extent (AUC) of systemic exposure to budesonide compared with that following Entocort. However, for Uceris, the pharmacokinetic profile was delayed, a pattern consistent with greater colonic delivery of the active substance.