Further studies on the hydrolysis of salicyluric acid in intestinal microorganisms and prolonged blood concentration of salicylic acid following rectal administration of salicyluric acid in rabbits.
The blood concentrations of salicyluric acid and salicylic acid following intracecal and rectal administration of salicyluric acid were determined in rabbits. Immediate and very extensive salicylic acid formation in the cecum was found following intracecal administration. After rectal administration, a small amount of salicyluric acid was absorbed in intact form. The rest was rapidly hydrolyzed to salicylic acid, which was subsequently absorbed. The blood concentration of salicylic acid was maintained at 1.3-1.8 micrograms/ml from 2 to 12 h. Three doses of salicyluric acid were administered rectally. The peak level of salicyluric acid increased with dose. However, salicylic acid concentration in the blood following administration of salicyluric acid at 10.0 mg/kg (salicylic acid equivalent) was not double that observed following administration of salicyluric acid at 5.0 mg/kg (salicylic acid equivalent). It appears that a larger amount of salicyluric acid in the rectal lumen may have saturated the glycine deconjugation system.
Nakamura
J
J
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
Shiota
H
H
Haraguchi
Y
Y
Sasaki
H
H
Shibasaki
J
J
D000285:Administration, Rectal; D000818:Animals; D006626:Hippurates / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D006868:Hydrolysis; D007422:Intestines / Q000382:microbiology*; D008297:Male; D011355:Prodrugs; D011817:Rabbits; D012459:Salicylates / Q000097:blood
D006626:Hippurates; D011355:Prodrugs; D012459:Salicylates; C000693:salicylurate