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AimsThe aims of the study were to: (1) evaluate the gastrointestinal transit, release and absorption of budesonide from tablets with a new multimatrix formulation (M MX®) designed to release the drug throughout the whole colon, and (2) assess the influence of food on budesonide bioavailability. MethodsTwo phase I studies, each comprising 12 healthy males, were performed. Gastrointestinal transit of 153 Sm-labelled tablets containing 9 mg budesonide was evaluated by means of pharmaco-scintigraphy. The effect of food was tested by comparing plasma pharmacokinetics after intake of a high fat and high calorie breakfast with fasting controls. Results153 Sm-labelled tablets reached the ascending colon after a mean ± SD 9.8 ± 6.9 h. Initial tablet disintegration was observed in the ileum in 42% and the ascending and transverse colon in 33% of subjects. Ninety-six per cent of the dose was absorbed into the systemic circulation during passage through the whole colon including the sigmoid. Food significantly decreased C max values from 1429 ± 1014 to 1040 ± 601 pg mL − 1 ( P = 0.028) and AUC values from 14 814 ± 11 254 to 13 486 ± 9369 pg h − 1 mL − 1 ( P = 0.008). Mean residence time and t max increased by 12-29%. There was no drug accumulation after 1 week of once daily oral administration of budesomide. ConclusionsMMX®-budesonide tablets appear suitable for targeted colonic drug delivery. Transit parameters and low systemic bioavailability warrant further studies with the new formulation.