TY - JOUR
T1 - Absorption, Enterohepatic Circulation, and Excretion of 5‐Aminosalicylic Acid in Rats
AU - Shafii, Ahmad
AU - Chowdhury, J. Roy
AU - Das, Kiron M.
PY - 1982/5
Y1 - 1982/5
N2 - 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 jug/ml) was reached in 1 b, and 30% of the administered dose was excreted in the urine in 24 b. 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.
AB - 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 jug/ml) was reached in 1 b, and 30% of the administered dose was excreted in the urine in 24 b. 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.
UR - http://www.scopus.com/inward/record.url?scp=0020033661&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0020033661&partnerID=8YFLogxK
U2 - 10.1111/j.1572-0241.1982.tb04770.x
DO - 10.1111/j.1572-0241.1982.tb04770.x
M3 - Article
C2 - 6123257
AN - SCOPUS:0020033661
SN - 0002-9270
VL - 77
SP - 297
EP - 299
JO - The American Journal of Gastroenterology
JF - The American Journal of Gastroenterology
IS - 5
ER -