Absorption, enterohepatic circulation, and excretion of 5-aminosalicylic acid in rats

A. Shafii, Jayanta Roy-Chowdhury, K. M. Das

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

After oral administration of sulfasalazine, the majority of the administered dose reaches the colon, where it is split into 5-aminosalicylic acid (5-ASA) and sulfapyridine. 5-ASA is believed to be the effective component in the treatment of inflammatory bowel disease. After intraduodenal administration of 5-ASA (20 mg) in rats, 91% of the drug was absorbed in the proximal small intestine. Peak serum 5-ASA concentration (55 μg/ml) was reached in 1 h. Approximately 61 and 6% of the administered dose were excreted in the urine and bile, respectively, in 24 h, almost exclusively in the acetylated form. When sulfapyridine (20 mg) was administered in addition to 5-ASA, 70% of the sulfapyridine was absorbed in the small intestine, peak serum concentration (50 μg/ml) was reached in 1 h, and 30% of the administered dose was excreted in the urine in 24 h. The results indicate that after oral administration of 5-ASA, a therapeutically significant concentration of the drug is not expected in the terminal ileum which is a common site of involvement in Crohn's disease. The therapeutic implications of these findings are discussed herein.

Original languageEnglish (US)
Pages (from-to)297-299
Number of pages3
JournalAmerican Journal of Gastroenterology
Volume77
Issue number5
StatePublished - 1982

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Enterohepatic Circulation
Mesalamine
Sulfapyridine
Small Intestine
Oral Administration
Urine
Sulfasalazine
Serum
Ileum
Inflammatory Bowel Diseases
Bile
Crohn Disease
Pharmaceutical Preparations
Colon
Therapeutics

ASJC Scopus subject areas

  • Gastroenterology

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Absorption, enterohepatic circulation, and excretion of 5-aminosalicylic acid in rats. / Shafii, A.; Roy-Chowdhury, Jayanta; Das, K. M.

In: American Journal of Gastroenterology, Vol. 77, No. 5, 1982, p. 297-299.

Research output: Contribution to journalArticle

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