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5‐aminosalicylic acid release from a new controlled‐release mesalazine formulation during gastrointestinal transit in healthy volunteers
Author(s) -
BRUNNER M.,
LACKNER E.,
EXLER P. S.,
FLUITER H. C.,
KLETTER K.,
TSCHURLOVITS M.,
DUDCZAK R.,
EICHLER H.G.,
MÜLLER M.
Publication year - 2006
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 - 10.1111/j.1365-2036.2006.02721.x
Subject(s) - mesalazine , ascending colon , medicine , aminosalicylic acid , pharmacokinetics , gastroenterology , ulcerative colitis , pharmacology , absorption (acoustics) , inflammatory bowel disease , dosing , physics , disease , acoustics
Summary Background Mesalazine (5‐aminosalicylic acid, 5‐ASA) containing formulations represent a cornerstone in the treatment of inflammatory bowel diseases. A novel formulation with an Eudragit L/S mixture coating has been developed to provide selective release of 5‐ASA to the ileo‐caecal region and the colon. Aim To determine the release of 5‐ASA during the gastrointestinal transit. Methods A single oral dose of mesalazine EC 500 mg gastroresistant tablets (Asamax) was administered to eight healthy male volunteers. Gastrointestinal transit and tablet disintegration were monitored by scintigraphy. 5‐ASA release was verified by assessing plasma pharmacokinetics. Results Initial tablet disintegration was observed 5.65 ± 0.86 h after dosing, corresponding to the detection of 5‐ASA in plasma. This occurred in the ileo‐caecal region in three subjects and the ascending colon in the remaining five. The relative percentage of 5‐ASA absorption was more pronounced in the ascending colon (41 ± 27.4%) than the ileo‐caecal region (6.6 ± 9.2%). Conclusion This mesalazine EC gastroresistant tablets release locally active 5‐ASA specifically in the ileo‐caecal region and the ascending colon.