Delayed-release mesalazine (5-aminosalicylic acid): coat dissolution and excretion in ileostomy subjects.
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.
Riley
S A
SA
University Department of Medicine, Hope Hospital, Salford.
Tavares
I A
IA
Bennett
A
A
Mani
V
V
D000328:Adult; D000636:Aminosalicylic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007081:Ileostomy; D008297:Male; D019804:Mesalamine; D008875:Middle Aged; D012995:Solubility
D000636:Aminosalicylic Acids; D003692:Delayed-Action Preparations; D019804:Mesalamine