Bioavailability of aminosalicylic acid and its various salts in humans III: Absorption from tablets

✍ Scribed by Suk Han Wan; Pertti J. Pentikainen; Daniel L. Azarnoff

• Publisher: John Wiley and Sons
• Year: 1974
• Tongue: English
• Weight: 435 KB
• Volume: 63
• Category: Article
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600630512

✦ Synopsis

The relative bioavailability of commercially available preparations of aminosalicylic acid and its sodium, potassium, and calcium salts is presented. The doses administered were 4 g for aminosalicylic acid and 2.8, 2.6, and 2.6 g for the sodium, potassium, and calcium salts, respectively. Absorption from tablets of the salts was rapid and complete, but absorption of the free acid was only 77% of the dose. Dissolution of the relatively insoluble acid is a rate-limiting factor in absorption. Although the amount of free acid administered and the absolute amount absorbed were higher, the area under the plasma concentration curve of unmetabolized drug was less than for the salts. This is attributed to capacity-limited acetylation of drug, especially during the first pass. The amount of bioavailable drug is dependent on the rate of metabolism and, hence, the rate of absorption. Keyphrases Aminosalicylic acid and salts-absorption from commercial tablets compared, humans Bioavailability-absorption of aminosalicylic acid and salts from commercial tablets, humans Absorption-aminosalicylic acid and salts from commercial tablets, humans