Bioavailability of 5-aminosalicyclic acid from slow release 5-aminosalicyclic acid drug and sulfasalazine in normal children.
The bioavailability of a controlled release 5-aminosalicyclic acid preparation (Pentasa) was investigated in nine healthy children after a medication period of six days (1000 mg/day) and compared with sulfasalazine (Salazopyrin) (2000 mg/day). The local bioavailability in the distal gut lumen, reflected by the 5-aminosalicylic acid concentration in the fecal water, showed comparable values after Pentasa (4.44 mmol/liter) and Salazopyrin (6.25 mmol/liter). The concentration of N-acetyl-5-ASA was significantly higher after Pentasa, reflecting the more proximal release of 5-aminosalicyclic acid compared with Salazopyrin. No relation was found between the 5-aminosalicylic acid fecal water concentration water concentration and the 5-aminosalicylic acid dose per kilogram of body weight. The urinary excretion of 5-aminosalicylic acid and N-acetyl-5-aminosalicylic acid was higher after Pentasa than after Salazopyrin (32% vs 25%). Dose interval plasma concentration curves showed low values after both preparations. Based on the concept that the fecal water concentration is decisive for the efficacy of 5-aminosalicylic acid in distal inflammatory bowel disease, Pentasa treatment offers a relevant alternative in cases of Salazopyrin intolerance or allergy in children. The higher systemic bioavailability from Pentasa warrants monitoring of the renal function.
Christensen
L A
LA
Department of Medical Gastroenterology, Aalborg Hospital, Denmark.
Fallingborg
J
J
Jacobsen
B A
BA
Abildgaard
K
K
Rasmussen
H H
HH
Rasmussen
S N
SN
Hansen
S H
SH
D000636:Aminosalicylic Acids / Q000493:pharmacokinetics*; D001682:Biological Availability; D002648:Child; D003692:Delayed-Action Preparations; D005243:Feces / Q000737:chemistry; D005260:Female; D006801:Humans; D008297:Male; D019804:Mesalamine; D012460:Sulfasalazine / Q000493:pharmacokinetics*
D000636:Aminosalicylic Acids; D003692:Delayed-Action Preparations; D012460:Sulfasalazine; D019804:Mesalamine