Steady-State Kinetics of 5-Aminosalicylic Acid and Sulfapyridine during Sulfasalazine Prophylaxis in Ulcerative Colitis

S. Bondesen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

O. H. Nielsen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

J. B. Schou Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

P. H. Jensen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

L. B. Lassen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

V. Binder Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

P. A. Krasilnikoff Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

P. Danø Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

S. Honoré Hansen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

S. Nørby Rasmussen Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

E. F. Hvidberg Dept. of Medicine, Community Hospital, Elsinore; Dept. of Medical Gastroenterology C, Herlev, University of Copenhagen, Herlev; Dept. of Pediatrics, Aalborg Hospital, Aalborg; Dept. of Pediatrics, Viborg Hospital, Viborg; Dept. of Pediatrics, Gentofte Hospital, University of Copenhagen, Hellerup; Dept. of Organic Chemistry, Royal Danish School of Pharmacy, Copenhagen, Denmark; Dept. of Medicine P, Division of Gastroenterology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark; Dept. of Clinical Pharmacology, Rigshospitalet, University of Copenhagen, Copenhagen, Denmark

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Abstract

Fifteen adult and 19 pediatric outpatients with ulcerative colitis were studied to determine the steady-state kinetics of 5-aminosalicylic acid (5-ASA) released from salazosulfapyridine (SASP). Results of excretion in adults (mean 24-h recovery of 5-ASA, 21% in urine and 57% in feces) were compatible with those of healthy volunteers. Since mean SASP dose/kg body weight (about 50 mg/kg) and compliance (reflected in sulfapyridine recovery) were equal in adults and pediatric patients, the results of the patient groups could be compared. Near-complete azo reduction of SASP occurs in children. Absorption and excretion of 5-ASA and metabolism to acetyl-5-ASA did not differ statistically between pediatric and adult patients. However, the fecal excretion of the drug and its metabolites was significantly lower in young patients, although fecal concentrations were the same. The present results demonstrate that SASP is an excellent sustained-release drug for the delivery of 5-ASA to the lower part of the bowel system and provide a reference for comparison of 5-ASA kinetics after treatment with newer 5-ASA preparations.

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Steady-State Kinetics of 5-Aminosalicylic Acid and Sulfapyridine during Sulfasalazine Prophylaxis in Ulcerative Colitis

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Steady-State Kinetics of 5-Aminosalicylic Acid and Sulfapyridine during Sulfasalazine Prophylaxis in Ulcerative Colitis

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