Small bowel absorption of sulfasalazine and its hepatic metabolism in human beings, cats, and rats

Kiron M. Das, Jayanta Roy-Chowdhury, B. Zapp, John W. Fara

Research output: Contribution to journalArticle

54 Citations (Scopus)

Abstract

To elucidate the role of the small bowel and liver in sulfasalazine (SASP) metabolism, we performed studies in patients, cats, and rats. The role of the small bowel in absorption and metabolism of SASP was determined by the amount of administered SASP excreted in ileostomy effluents, and the concentration of serum and urinary SASP and its metabolites, sulfapyridine and 5-amino salicylic acid. Seventy-five to ninety percent of the drug was excreted in ileostomy effluents of 6 patients as SASP, and only 5% of the dose was sulfapyridine. In cats, ileostomy and portal venous cannulations revealed that 20-30% of administered SASP is absorbed from the small bowel without being metabolized. The role of the liver in SASP metabolism was established in vivo and in vitro. SASP metabolites were measured in bile, serum, and urine of 2 patients with a choledochal T-tube and in serum and bile in six cats and four rats. Twenty to fifty percent of the absorbed drug was excreted in bile as SASP and no detectable sulfapyridine appeared in the bile. SASP concentration in peripheral blood and urine ranged between 3 and 12 μg/ml, and no significant amount of sulfapyridine metabolites were detected in the bile, serum, or urine of animals with an ileostomy. In vitro experiments with liver from cats and rats showed nearly complete reduction of SASP into metabolites. These studies reveal that SASP is not metabolized by the liver in vivo, and after absorption from the small bowel, 25-50% of the SASP is excreted unchanged in the bile, and the rest enters the circulation. Implications of these results in the treatment of patients with Crohn's disease of the small intestine are discussed.

Original languageEnglish (US)
Pages (from-to)280-284
Number of pages5
JournalGastroenterology
Volume77
Issue number2
StatePublished - 1979

Fingerprint

Sulfasalazine
Sulfapyridine
Bile
Ileostomy
Cats
Liver
Urine
Serum
Salicylic Acid
Catheterization
Crohn Disease
Pharmaceutical Preparations
Small Intestine

ASJC Scopus subject areas

  • Gastroenterology

Cite this

Small bowel absorption of sulfasalazine and its hepatic metabolism in human beings, cats, and rats. / Das, Kiron M.; Roy-Chowdhury, Jayanta; Zapp, B.; Fara, John W.

In: Gastroenterology, Vol. 77, No. 2, 1979, p. 280-284.

Research output: Contribution to journalArticle

@article{8b197efcc1a7439ba9facd96f4322316,
title = "Small bowel absorption of sulfasalazine and its hepatic metabolism in human beings, cats, and rats",
abstract = "To elucidate the role of the small bowel and liver in sulfasalazine (SASP) metabolism, we performed studies in patients, cats, and rats. The role of the small bowel in absorption and metabolism of SASP was determined by the amount of administered SASP excreted in ileostomy effluents, and the concentration of serum and urinary SASP and its metabolites, sulfapyridine and 5-amino salicylic acid. Seventy-five to ninety percent of the drug was excreted in ileostomy effluents of 6 patients as SASP, and only 5{\%} of the dose was sulfapyridine. In cats, ileostomy and portal venous cannulations revealed that 20-30{\%} of administered SASP is absorbed from the small bowel without being metabolized. The role of the liver in SASP metabolism was established in vivo and in vitro. SASP metabolites were measured in bile, serum, and urine of 2 patients with a choledochal T-tube and in serum and bile in six cats and four rats. Twenty to fifty percent of the absorbed drug was excreted in bile as SASP and no detectable sulfapyridine appeared in the bile. SASP concentration in peripheral blood and urine ranged between 3 and 12 μg/ml, and no significant amount of sulfapyridine metabolites were detected in the bile, serum, or urine of animals with an ileostomy. In vitro experiments with liver from cats and rats showed nearly complete reduction of SASP into metabolites. These studies reveal that SASP is not metabolized by the liver in vivo, and after absorption from the small bowel, 25-50{\%} of the SASP is excreted unchanged in the bile, and the rest enters the circulation. Implications of these results in the treatment of patients with Crohn's disease of the small intestine are discussed.",
author = "Das, {Kiron M.} and Jayanta Roy-Chowdhury and B. Zapp and Fara, {John W.}",
year = "1979",
language = "English (US)",
volume = "77",
pages = "280--284",
journal = "Gastroenterology",
issn = "0016-5085",
publisher = "W.B. Saunders Ltd",
number = "2",

}

TY - JOUR

T1 - Small bowel absorption of sulfasalazine and its hepatic metabolism in human beings, cats, and rats

AU - Das, Kiron M.

AU - Roy-Chowdhury, Jayanta

AU - Zapp, B.

AU - Fara, John W.

PY - 1979

Y1 - 1979

N2 - To elucidate the role of the small bowel and liver in sulfasalazine (SASP) metabolism, we performed studies in patients, cats, and rats. The role of the small bowel in absorption and metabolism of SASP was determined by the amount of administered SASP excreted in ileostomy effluents, and the concentration of serum and urinary SASP and its metabolites, sulfapyridine and 5-amino salicylic acid. Seventy-five to ninety percent of the drug was excreted in ileostomy effluents of 6 patients as SASP, and only 5% of the dose was sulfapyridine. In cats, ileostomy and portal venous cannulations revealed that 20-30% of administered SASP is absorbed from the small bowel without being metabolized. The role of the liver in SASP metabolism was established in vivo and in vitro. SASP metabolites were measured in bile, serum, and urine of 2 patients with a choledochal T-tube and in serum and bile in six cats and four rats. Twenty to fifty percent of the absorbed drug was excreted in bile as SASP and no detectable sulfapyridine appeared in the bile. SASP concentration in peripheral blood and urine ranged between 3 and 12 μg/ml, and no significant amount of sulfapyridine metabolites were detected in the bile, serum, or urine of animals with an ileostomy. In vitro experiments with liver from cats and rats showed nearly complete reduction of SASP into metabolites. These studies reveal that SASP is not metabolized by the liver in vivo, and after absorption from the small bowel, 25-50% of the SASP is excreted unchanged in the bile, and the rest enters the circulation. Implications of these results in the treatment of patients with Crohn's disease of the small intestine are discussed.

AB - To elucidate the role of the small bowel and liver in sulfasalazine (SASP) metabolism, we performed studies in patients, cats, and rats. The role of the small bowel in absorption and metabolism of SASP was determined by the amount of administered SASP excreted in ileostomy effluents, and the concentration of serum and urinary SASP and its metabolites, sulfapyridine and 5-amino salicylic acid. Seventy-five to ninety percent of the drug was excreted in ileostomy effluents of 6 patients as SASP, and only 5% of the dose was sulfapyridine. In cats, ileostomy and portal venous cannulations revealed that 20-30% of administered SASP is absorbed from the small bowel without being metabolized. The role of the liver in SASP metabolism was established in vivo and in vitro. SASP metabolites were measured in bile, serum, and urine of 2 patients with a choledochal T-tube and in serum and bile in six cats and four rats. Twenty to fifty percent of the absorbed drug was excreted in bile as SASP and no detectable sulfapyridine appeared in the bile. SASP concentration in peripheral blood and urine ranged between 3 and 12 μg/ml, and no significant amount of sulfapyridine metabolites were detected in the bile, serum, or urine of animals with an ileostomy. In vitro experiments with liver from cats and rats showed nearly complete reduction of SASP into metabolites. These studies reveal that SASP is not metabolized by the liver in vivo, and after absorption from the small bowel, 25-50% of the SASP is excreted unchanged in the bile, and the rest enters the circulation. Implications of these results in the treatment of patients with Crohn's disease of the small intestine are discussed.

UR - http://www.scopus.com/inward/record.url?scp=0018289765&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0018289765&partnerID=8YFLogxK

M3 - Article

VL - 77

SP - 280

EP - 284

JO - Gastroenterology

JF - Gastroenterology

SN - 0016-5085

IS - 2

ER -