Disposition of disodium azodisalicylate in healthy subjects. A possible new drug for inflammatory bowel disease.
The disposition of disodium azodisalicylate and salicylazosulfapyridine was studied in 6 healthy volunteers. After a single oral dose (1.0 g disodium azodisalicylate; 2.3 g salicylazosulfapyridine) maximum serum concentrations of the intact compound ranged between 1.4 and 6.8 mumol/L and 32 and 114 mumol/L, respectively. Mean residence time and serum half-life of disodium azodisalicylate were considerably longer than those of salicylazosulfapyridine, probably because of a higher apparent volume of distribution. Both compounds were largely split by colonic bacteria and comparable amounts of the active moiety, (acetyl-)5-aminosalicylic acid, were recovered in feces. During long-term ingestion of disodium azodisalicylate (1.0 g/day) it took 6-19 days to reach a steady state. Serum concentrations of disodium azodisalicylate at steady state were low: 2.2-8.4 mumol/L. The serum half-life was 6-10 days. It is concluded that the disposition of disodium azodisalicylate is similar, in important respects, to that of salicylazosulfapyridine. Disodium azodisalicylate, therefore, deserves therapeutic trial.
van Hogezand
R A
RA
van Hees
P A
PA
Zwanenburg
B
B
van Rossum
J M
JM
van Tongeren
J H
JH
D000284:Administration, Oral; D000636:Aminosalicylic Acids / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D003424:Crohn Disease; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D019804:Mesalamine; D013427:Sulfapyridine / Q000378:metabolism; D012460:Sulfasalazine / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism
D000636:Aminosalicylic Acids; D012460:Sulfasalazine; D019804:Mesalamine; C032587:olsalazine; D013427:Sulfapyridine