In-vitro evaluation of biphenylyl acetic acid-beta-cyclodextrin conjugates as colon-targeting prodrugs: drug release behaviour in rat biological media.

@article{Hirayama1996InvitroEO,
  title={In-vitro evaluation of biphenylyl acetic acid-beta-cyclodextrin conjugates as colon-targeting prodrugs: drug release behaviour in rat biological media.},
  author={Fumitoshi Hirayama and Kyoji Minami and Kaneto Uekama},
  journal={The Journal of pharmacy and pharmacology},
  year={1996},
  volume={48 1},
  pages={27-31}
}
Biphenylyl acetic acid was selectively conjugated to one of the primary hydroxyl groups of beta-cyclodextrin through an ester- or amide-linkage, and the physicochemical properties (aqueous solubility and hydrolysis) were investigated. Aqueous solubility of the conjugates was lower than those of either drug or parent beta-cyclodextrin. The amide conjugate was stable in aqueous solution and in rat biological fluids and gastrointestinal contents. The ester conjugate was hydrolysed to beta… CONTINUE READING