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Gastrointestinal transit and release of 5‐aminosalicylic acid from 153 Sm‐labelled mesalazine pellets vs. tablets in male healthy volunteers
Author(s) -
Brunner M.,
Greinwald R.,
Kletter K.,
Kvaternik H.,
Corrado M. E.,
Eichler H. G.,
Müller M.
Publication year - 2003
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1046/j.1365-2036.2003.01564.x
Subject(s) - mesalazine , aminosalicylic acid , medicine , pellets , pharmacokinetics , pharmacology , dosage form , gastroenterology , ulcerative colitis , materials science , disease , composite material
Summary Background : Mesalazine (5‐aminosalicylic acid)‐containing formulations, designed to optimize drug delivery to the ileo‐caecal region, represent a cornerstone in the treatment of inflammatory bowel diseases. Aim : To test, by means of pharmaco‐scintigraphy, whether novel mesalazine‐containing pellets release 5‐aminosalicylic acid in the same target region as mesalazine tablets (Salofalk). Methods : Fourteen healthy male volunteers received a single dose of either pellets or tablets containing 500 mg of mesalazine and 2 mg of 152 Sm 2 O 3 with a 1‐week washout period. The gastrointestinal transit of 153 Sm, incorporated into the formulations, was followed by gamma‐scintigraphy. Mesalazine release was verified by assessing 5‐aminosalicylic acid plasma pharmacokinetics. Results : The formulations reached the ileo‐caecal target region almost at the same time (3.3 ± 1 and 3.8 ± 1 h for pellets and tablets, respectively). Plasma 5‐aminosalicylic acid t max values were comparable and corresponded to the time during which the formulations were located in the target region. Plasma AUC values were significantly lower for pellets, which might be explained by a more prolonged release of 5‐aminosalicylic acid. Conclusions : Novel mesalazine pellets and Salofalk tablets release active 5‐aminosalicylic acid in the same target region and pass through the gastrointestinal tract under fasting conditions in healthy volunteers in a comparable time. From a comparison of in vitro dissolution and plasma concentration data, a slower and more prolonged release of 5‐aminosalicylic acid from pellets is suggested.