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Clinical Trial
, 61 (1), 31-8

Gastrointestinal Transit, Release and Plasma Pharmacokinetics of a New Oral Budesonide Formulation

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Clinical Trial

Gastrointestinal Transit, Release and Plasma Pharmacokinetics of a New Oral Budesonide Formulation

M Brunner et al. Br J Clin Pharmacol.

Abstract

Aims: The aims of the study were to: (1) evaluate the gastrointestinal transit, release and absorption of budesonide from tablets with a new multimatrix formulation (MMX) designed to release the drug throughout the whole colon, and (2) assess the influence of food on budesonide bioavailability.

Methods: Two 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.

Results: (153)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.

Conclusions: MMX-budesonide tablets appear suitable for targeted colonic drug delivery. Transit parameters and low systemic bioavailability warrant further studies with the new formulation.

Figures

Figure 1
Figure 1
A representative scintigraphic image, depicting the dispersion of 153Sm-labelled MMX®-budesonide tablets in the colon. The image shown was acquired approximately 7 h after drug administration
Figure 2
Figure 2
The mean ± SD plasma concentration vs. time profile of budesonide after single-dose administration of 153Sm-labelled MMX®-tablets to 12 healthy males. Lines depict periods between minimal time to arrive and maximal time to leave different gastrointestinal regions
Figure 3
Figure 3
The mean ± SD plasma concentration vs. time profiles of budesonide after single-dose administration of 9 mg MMX®-tablets to 12 males under fasting (▵) and fed conditions (▿)

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