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

Abstract

Objective To compare the pharmacokinetics of the extended-release MMX® formulation of budesonide (Uceris®) with that of Entocort® 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®, 9 mg Uceris® or 9 mg Entocort® EC. Standard pharmacokinetic parameters were assessed. Results The study included 12 subjects. The 9 mg Uceris® and 9 mg Entocort® EC formulations had comparable area under the concentration–time curve (AUC) data, but 9 mg Uceris® had a notably longer time to first appearance in plasma (median Tlag, 6 h versus 1 h, respectively), and a delayed time to maximum concentration (median Tmax, 15 h versus 5 h, respectively) compared with 9 mg Entocort® EC. The ratio of log-transformed AUC0–last (Uceris®/Entocort® 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.