title: 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%).
  
  
  CONCLUSIONS
  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.
authors.affiliation: Pharmaceutical Consulting, Encinitas, CA 92024, USA. rew.nicholls@sbcglobal.net
authors.forename: Andrew
authors.initials: A
authors.lastname: Nicholls
authors.forename: Raúl
authors.initials: R
authors.lastname: Harris-Collazo
authors.forename: Michael
authors.initials: M
authors.lastname: Huang
authors.forename: Yun
authors.initials: Y
authors.lastname: Hardiman
authors.forename: Richard
authors.initials: R
authors.lastname: Jones
authors.forename: Luigi
authors.initials: L
authors.lastname: Moro
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D019819:Budesonide / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002214:Capsules; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D008297:Male; D008875:Middle Aged; D013607:Tablets; D055815:Young Adult
chemical_list: D002214:Capsules; D003692:Delayed-Action Preparations; D013607:Tablets; D019819:Budesonide
keywords: Bioavailability; bioequivalence; budesonide; ulcerative colitis