Different orally and rectally applicable forms of 5-ASA and budesonide have
been developed to achieve sufficient high concentrations of the active moi
eties at the site of inflammation (small and/or large bowel) and to limit t
he systemic action of the drugs. This concept of drug targeting could be ac
complished by both special galenic formulations and by utilizing the pharma
cokinetic properties of the agents especially their high intestinal and hep
atic presystemic elimination. Thus, 5-ASA and budesonide represent drugs of
first choice in the treatment of Crohn's disease and ulcerative colitis.
This review describes the various pharmacokinetic and (patho)physiologic fa
ctors and their impact on drug delivery and biological availability of the
different 5-ASA and budesonide preparations.