ABSTRACT
Gastrointestinal transit of an enteric coated delayed release 5-aminosalicylic acid tablet radiolabelled with 111indium has been monitored in a total of 13 patients with Crohn's disease and ulcerative colitis. More than 70% of the tablets disintegrated in the small intestine, on average 3.2 hours after emptying from the stomach. Dispersed preparation was detected in the proximal colon of all the patients, except one with an ileostomy. Mean peak plasma concentrations of 5-aminosalicylic acid and its metabolite acetyl-5-aminosalicylic acid occurred 3-4 hours after gastric emptying. The tablets provide a reliable means of drug delivery to the ileum and proximal colon.
Subject(s)
Aminosalicylic Acids/pharmacokinetics , Inflammatory Bowel Diseases/metabolism , Adult , Aged , Aminosalicylic Acids/administration & dosage , Colitis, Ulcerative/metabolism , Crohn Disease/metabolism , Female , Humans , Male , Mesalamine , Middle Aged , Tablets, Enteric-CoatedABSTRACT
Gastrointestinal transit of an enteric-coated, delayed-release 5-aminosalicylic acid tablet radiolabelled with indium-111 has been monitored in a preliminary study with eight healthy subjects using gamma scintigraphy. Gastric emptying of the tablet was delayed by the presence of food in the stomach. Disintegration occurred about 5 hours after the tablet left the stomach. There was close agreement between the tablet disintegration times and the initial detection of drug in the blood. The site of disintegration could be established in most instances; approximately 80% of the doses resulted in drug dispersion within the ascending colon. The coated tablets provide an effective means of drug delivery to the proximal colon.
Subject(s)
Aminosalicylic Acids/pharmacokinetics , Gastrointestinal Transit , Adult , Aged , Aminosalicylic Acids/administration & dosage , Delayed-Action Preparations , Female , Humans , Male , Mesalamine , Middle Aged , Tablets, Enteric-CoatedABSTRACT
Gastrointestinal transit and release of a delayed-release, enteric-coated tablet of mesalazine (Claversal) were studied in 13 patients with Crohn's disease and ulcerative colitis. The tablets disintegrated a mean of 3.2 h after leaving the stomach, resulting in drug dispersion in the distal small intestine or proximal colon. Tablet disintegration closely correlated with onset of drug absorption. Peak mean concentrations of mesalazine and its main metabolite, Ac-5-ASA, were 0.5 microgram/ml and 1.0 microgram/ml, respectively, and occurred 3 to 4 h after gastric emptying. The plasma levels correlated with scintigraph images of tablet disintegration. It is concluded that the tablets effectively deliver mesalazine to the terminal ileum and proximal colon in patients with inflammatory bowel disease.