chapter  4
56 Pages

The Pharmacokinetics of Ibuprofen in Humans and Animals

WithDion R Brocks, Fakhreddin Jamali

This chapter discusses the presence of a presystemic inversion process, it would be anticipated that the percentage of the dose systemically available as the therapeutically active S enantiomer would be higher than that after an immediate release dosage form containing the same amount of racemic compound. The pharmacokinetic properties of ibuprofen have been studied intensely. It was the first 2-arylpropionic acid nonstereoidal anti-inflammatory drug (NSAID) developed and marketed for treatment of arthritic disorders, and in many countries it has been granted non-prescription status for treatment of pain and fever. Ibuprofen is usually given as its acid form, although salt and ester formulations are available in some countries. The synovial membrane has been postulated to be the site of action of NSAIDs, and several studies have in turn examined synovial fluid concentrations of ibuprofen and its enantiomers. Because NSAIDs are indicated for connective-tissue disease, it is relevant to understand the ability of these drugs to bind to those tissues.