Absorption, metabolism, and excretion of salicylic phenolic glucuronidc in rats

✍ Scribed by Gerha. Rd Levy; Leonard Weintraub; Tai Matsuzawa; Stanley R. Oles

• Publisher: John Wiley and Sons
• Year: 1966
• Tongue: English
• Weight: 192 KB
• Volume: 55
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600551135

✦ Synopsis

Salicylic phenolic glucuronide is excreted rapidly by apparent first-order kinetics (t>a about 0.7 hr.) after intravenous administration to adult rats. Only a small fraction of an injected dose is hydrolyzed in vim to salicylic acid. The glucuronide is apparently not absorbed significantly as such from the gastrointestinal tract. Part o f an orally administered dose is absorbed apparently from the lower region of the intestinal tract after hydrolysis to salicylic acid.

IIE PHAKMACOKINETICS of elimination of sali-T cylic acid and its major Irietdbolite, salicyluric acid, have been studied in some detail in man and rats (lL4). Much less is known about the kinetics of elimination of salicylic phenolic glucuronidc, another irrilportarit rnetabolitc of salicylic acid.' This glucur,onidc has been prepared in pure form and (since technical problems did not permit its intravenous administration to man) its absorption, metabolism, and excretion have. been studicd in rats.

A previous study has shown that the pharrnacokinetics of salicylate elimination in man and rats :ire quite similar (4).

EXPERIMENTAL

Synthesis of Salicylic Phenolic G1ucuronide.-Methyl (tr:i-O-acetyl-ol-D-glucopy~dnosyl bromide) uronatc: was prepared from glucuronolactone by the procedure of Bollenback et ul. (6). From it, ocarboxypheriyl-P-D-glucopyranosiduronic acid (salicylic phenolic glucuronide) was obtained by methods described by Lunsford and Murphey (7), m.p. 144.5-146'.