Effect of food coadministration on 5-aminosalicylic acid oral suspension bioavailability

Autor: Robert C. Lanman, Bruce Morrill, Dennis H. Giesing, Michael B Lanman, Dale K Yu, Larry S Eichmeier, Alfred T Elvin
Rok vydání: 1990
Předmět:
Zdroj: Clinical Pharmacology and Therapeutics. 48:26-33
ISSN: 1532-6535
0009-9236
DOI: 10.1038/clpt.1990.113
Popis: Single doses of 1 gm 5-aminosalicylic acid (5-ASA) suspension was administered to 24 healthy volunteers during both fasting and fed conditions. For subjects in a fasting state, plasma 5-ASA and acetyl 5-ASA concentrations peaked rapidly 1 hour after dosing to 14.72 μg/ml and 11.4 μg/ml, respectively. The elimination half-life of 5-ASA was 51.9 minutes, whereas the acetyl 5-ASA half-life could not be determined. A mean of 78.3% of the dose was excreted in the urine, with 5-ASA accounting for 21.2% of the dose and acetyl 5-ASA accounting for the balance. Only 11.3% of the dose was eliminated in the feces, consisting mostly of acetyl 5-ASA. Food coadministration reduced 5-ASA and acetyl 5-ASA systemic relative bioavailability to 44% and 76%, respectively, compared with the fasting treatment. Urinary excretion of the salicylates was reduced to 46.8%, and fecal salicylate elimination increased almost 100%– to 24.2% of the total dose. Clinical Pharmacology and Therapeutics (1990) 48, 26–33; doi:10.1038/clpt.1990.113
Databáze: OpenAIRE