Disposition of mesalazine from mesalazine-delivering drugs in patients with inflammatory bowel disease, with and without diarrhoea.
The disposition of mesalazine from the azo compounds sulphasalazine and olsalazine (Dipentum) and from the slow-release mesalazine drugs Pentasa, Asacol, and Salofalk was studied in 20 patients with inflammatory bowel disease. Ten of them had diarrhoea, and 10 had normal stools. On the last 2 days of a 7-day maintenance treatment with each of the study drugs urine and faeces were collected for determination of mesalazine, acetyl-mesalazine, and unsplit azo compound. In patients with and without diarrhoea the urinary and the faecal excretion of acetyl-mesalazine was lowest during treatment with olsalazine. The proportion of acetyl-mesalazine in faeces was highest during treatment with Pentasa in both groups. The presence of diarrhoea was associated with a decrease in the proportion of acetyl-mesalazine in faeces during treatment with all drugs, not significant only for Pentasa. The proportion of unsplit azo compound in faeces increased in the case of diarrhoea to almost 50%. It is concluded that in patients with inflammatory bowel disease diarrhoea substantially influences the disposition from all these drugs except Pentasa.
Dept. of Gastrointestinal and Liver Diseases, University Hospital Nijmegen, The Netherlands.
M C
MC
Rijk
A
A
van Schaik
J H
JH
van Tongeren
D000328:Adult; D000368:Aged; D000636:Aminosalicylic Acids / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use* / Q000652:urine; D003692:Delayed-Action Preparations / Q000592:standards; D003967:Diarrhea / Q000209:etiology*; D004337:Drug Carriers; D005243:Feces / Q000737:chemistry; D005260:Female; D005772:Gastrointestinal Transit; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000150:complications / Q000188:drug therapy* / Q000652:urine; D008297:Male; D019804:Mesalamine; D008875:Middle Aged; D012460:Sulfasalazine / Q000627:therapeutic use*
D000636:Aminosalicylic Acids; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D012460:Sulfasalazine; D019804:Mesalamine; C032587:olsalazine