Pharmacokinetics of sulfasalazine metabolites in rats following concomitant oral administration of riboflavin.

Abstract:

:Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabolites in urine was significantly greater (alpha = 0.01) for the group receiving 10 mg/kg riboflavin compared to the controls or the group receiving 1 mg/kg riboflavin. Plasma AUC and Cmax values were also significantly greater (alpha = 0.05) for the 10 mg/kg riboflavin group. These results suggest that at higher doses, a significant fraction of riboflavin reaches the colon intact and stimulates more efficient reduction of the azo bond in sulfasalazine. Since the concentrations of 5-ASA achieved in the colon may be directly related to the efficacy of sulfasalazine in treating inflammatory bowel disease, concomitant administration of riboflavin may enhance sulfasalazine's efficacy in humans.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Chungi VS,Dittert LW,Shargel L

doi

10.1023/a:1015938706685

subject

Has Abstract

pub_date

1989-12-01 00:00:00

pages

1067-72

issue

12

eissn

0724-8741

issn

1573-904X

journal_volume

6

pub_type

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