Open AccessBioavailability profile of Uceris MMX extended-release tablets compared with Entocort EC capsules in healthy volunteers
Author(s) -
Andrew Nicholls,
Raúl Harris-Collazo,
Michael Huang,
Yun Hardiman,
Richard J. Jones,
Luigi Moro
Publication year - 2013
Publication title -
journal of international medical research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.421
H-Index - 57
eISSN - 1473-2300
pISSN - 0300-0605
DOI - 10.1177/0300060513476588
Subject(s) - pharmacokinetics , medicine , bioavailability , crossover study , budesonide , bioequivalence , confidence interval , pharmacology , area under the curve , gastroenterology , chromatography , corticosteroid , chemistry , alternative medicine , pathology , placebo
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 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® EC. The ratio of log-transformed AUC 0–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.