The in vivo behaviour of a colonic delivery system: a pilot study in man

Autor: R. Musa, I.R. Wilding, Paolo Ventura, G. Hooper, K.P. Steed
Rok vydání: 1994
Předmět:
Zdroj: International Journal of Pharmaceutics. 112:199-206
ISSN: 0378-5173
DOI: 10.1016/0378-5173(94)90355-7
Popis: Eight healthy male volunteers were recruited for a study to determine the in vivo behaviour of an enteric coated, modified release beclomethasone dipropionate formulation. The non-invasive technique of gamma scintigraphy was used to relate position and integrity of the tablet formulation within the gastrointestinal tract to blood levels of beclomethasone dipropionate and its metabolites. Following fasted administration, tablet integrity was maintained in the stomach, and onset of disintegration occurred in the small intestine, leaving a sustained release core which eroded gradually. Complete tablet disintegration occurred in the small bowel in three volunteers and in the proximal colon in the remaining subjects. Low plasma concentrations of beclomethasone monopropionate were detectable in seven volunteers. In only one subject were both beclomethasone monopropionate and beclomethasone alcohol detected in the urine. Transit, disintegration and absorption were consistent with a formulation designed for topical treatment of inflammatory disease in the distal small bowel and proximal colon.
Databáze: OpenAIRE