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Delayed‐release mesalazine (5‐aminosalicylic acid): coat dissolution and excretion in ileostomy subjects.
Author(s) -
Riley SA,
Tavares IA,
Bennett A,
Mani V
Publication year - 1988
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1988.tb03383.x
Subject(s) - mesalazine , aminosalicylic acid , dissolution , ileostomy , chemistry , excretion , ingestion , pharmacology , chromatography , biochemistry , medicine , ulcerative colitis , organic chemistry , disease
1. Delayed‐release mesalazine has been formulated to deliver 5‐ aminosalicylic acid to the colon. We have therefore studied the ileostomy excretion and coat dissolution of this preparation. 2. Following ingestion of a single tablet 88% (range 69‐114%) of the 400 mg dose appeared unchanged in the ileosomy effluent over the subsequent 12 h. 3. Ileostomy effluent pH appeared to be a major determinant of 5‐ aminosalicylic acid release. 4. In vitro studies revealed rapid coat dissolution above pH 7.0, slow dissolution between pH 6.0 and 7.0 and non‐dissolution at pH 2.0 and 4.0.