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Effect of food coadministration on 5‐aminosalicylic acid oral suspension bioavailability
Author(s) -
Yu Dale K,
Elvin Alfred T,
Morrill Bruce,
Eichmeier Larry S,
Lanman Robert C,
Lanman Michael B,
Giesing Dennis H
Publication year - 1990
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1990.113
Subject(s) - bioavailability , urine , feces , pharmacology , aminosalicylic acid , pharmacokinetics , chemistry , dosing , excretion , oral administration , medicine , biochemistry , biology , paleontology
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