Intestinal Fate of 5‐aminosalicylic Acid: Regional and Systemic Kinetic Studies in Relation to Inflammatory Bowel Disease

I n Vivo Evaluation of 5-ASA Colon-Specific Tablets Using Experimental-Induced Colitis Rat Animal Model

“…It has been reported that 5-ASA is extensively absorbed and metabolized in the upper gastrointestinal tract by first pass metabolism and is not made available to the desired site, i.e., colon (15). With this objective, colonic delivery tablets based on natural polymers like guar gum and pectin were designed to pass through the upper part of gastrointestinal tract in the intact form without diffusion of active ingredients.…”

“…However, it has been reported that 5-ASA is extensively absorbed and metabolized in the upper gastrointestinal tract by first pass metabolism and is not made available to the desired site, i.e., colon (15). To improve the site availability of the drug, several approaches have been utilized (16,17).…”

A clinical trial on absorption and N‐acetylation of oral and rectal mesalazine

“…In detail, blood samples were taken just before and 20, 40 min, and 1, 1·5, 2, 2·5, 3,4,5,6,7,8,9,10,11,12,16,24,30,36 and 48 h after drug administration. In detail, blood samples were taken just before and 20, 40 min, and 1, 1·5, 2, 2·5, 3,4,5,6,7,8,9,10,11,12,16,24,30,36 and 48 h after drug administration.…”

Clinical Pharmacokinetic and Pharmacodynamic Considerations in the Treatment of Ulcerative Colitis

“…Absorbed mesalazine undergoes presystemic N-acetylation in intestinal mucosa and the liver. This pharmacologically inactive N-acetylated mesalazine is mainly excreted into the urine [17,20]. After rectal administration, 10-35% of the drug is absorbed [17], whereas after oral administration, depending on the dose and the type of formulation used, 15-67% of the drug is absorbed and excreted into the urine [21].…”