Effect of food on the pharmacokinetics of budesonide controlled ileal release capsules in patients with active Crohn's disease

Aim: To study the influence of food on the systemic availability of budeson ide in patients with active Crohn's disease. Methods: Eight patients with an established diagnosis of Crohn's disease ea ch received 9 mg budesonide controlled ileal release (CIR) capsules (Entoco rt capsules) orally on two separate occasions: once in a fasting state and once after a heavy breakfast. For reference, deuterium-labelled (H-2(8)) bu desonide, 0.5 mg, was given intravenously. Plasma concentrations of budeson ide and H-2(8)-budesonide were determined for 12 h, and their pharmacokinet ic parameters were calculated. Results: Average systemic availability of budesonide during fasting conditi ons was 10.7%, area under the curve was 27.5 nmol/L x h and peak plasma con centration was 4.1 nmol/L. Corresponding postprandial values were 13.2%, 27 .0 nmol/L x h and 3.8 nmol/L. Food increased the mean absorption time from 4.5 to 6.8 h (P=0.0012). Body clearance of budesonide was about 25% higher after eating (P=0.0015). Conclusions: Food had little influence on systemic availability and peak pl asma concentrations of budesonide administered in CIR capsules. Absorption was retarded postprandially, likely due to delayed gastric emptying. Budeso nide in CIR capsules can be administered at the same dose regardless of pra ndial status in patients with Crohn's disease.