A pharmacoscintigraphic evaluation of oral budesonide given as controlled-release (Entocort) capsules
Version of Record online: 5 MAR 2003
Alimentary Pharmacology & Therapeutics
Volume 17, Issue 4, pages 525–536, February 2003
How to Cite
Edsbäcker, S., Bengtsson, B., Larsson, P., Lundin, P., Nilsson, Å., Ulmius, J. and Wollmer, P. (2003), A pharmacoscintigraphic evaluation of oral budesonide given as controlled-release (Entocort) capsules. Alimentary Pharmacology & Therapeutics, 17: 525–536. doi: 10.1046/j.1365-2036.2003.01426.x
- Issue online: 5 MAR 2003
- Version of Record online: 5 MAR 2003
- Accepted for publication 8 August 2002
Aims : To investigate the gastrointestinal pharmacokinetics of controlled-release (Entocort) and standard budesonide capsules.
Methods : Six Crohn's disease patients and eight healthy controls were given controlled-release capsules containing budesonide and an inert 111In label, following breakfast. In the patients, a standard capsule containing deuterium-labelled budesonide was given simultaneously. In the controls, on a separate occasion, the controlled-release capsules were given in the fasting state. Gastrointestinal transit was recorded by a gamma camera. Plasma budesonide and deuterium-labelled budesonide were used to estimate drug release, and urine cortisol was used to assess systemic effects.
Results : Budesonide delivery to the ileo-colonic region was significantly greater after the intake of the controlled-release capsules [69%; 95% confidence interval (CI), 54–84] than after the standard capsules (30%; 95% CI, 15–45) (P = 0.005). Fasting had little impact on uptake. The transit and pharmacokinetics of budesonide were similar in both subject groups, although systemic availability was higher in patients (21%; 95% CI, 13–33) than in controls (12%; 95% CI, 10–14) (P = 0.009). Urinary cortisol was, however, similar in both groups.
Conclusions : A major fraction of budesonide is released in the ileum and throughout the colon, the intended target for the controlled-release formulation. The prandial state has little effect on budesonide uptake.