Time course of free and N4-acetylated sulfapyridine concentrations in the plasma and saliva of man after sulfasalazine (salicylazosulfapyridine) administration: preliminary findings.
The time course of free and N4-acetylated sulfapyridine (SP) concentrations in the saliva and whole plasma was determined in a healthy male volunteer after a single 2.0 g oral dose of salicylazosulfapyridine (SASP) as four-500 mg commercial, uncoated tablets. The mean (+/- S.D.) plasma: saliva concentration ratios for free and acetylated SP was 2.04 (+/- 0.24) and 3.12 (+/-0.43), respectively, and were independent of plasma concentration and saliva pH. The elimination half-lives of SP and N4-acetyl SP could be determined from either salivary or plasma concentration-time data. These preliminary results suggest that measurement of saliva concentrations of free and acetylated SP may be a convenient, noninvasive method for monitoring indirectly the plasma concentrations of SP and acetyl SP in patients treated with SASP and for determining acetylator phenotype.
D000085:Acetates / Q000378:metabolism; D000328:Adult; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D012463:Saliva / Q000378:metabolism*; D013424:Sulfanilamides / Q000378:metabolism*; D013427:Sulfapyridine / Q000097:blood / Q000378:metabolism*; D012460:Sulfasalazine / Q000494:pharmacology*
D000085:Acetates; D013424:Sulfanilamides; D012460:Sulfasalazine; D013427:Sulfapyridine