Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/2-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion compound on release of suppository was investigated. Complex formation was confirmed by ¹H- and ^(13)C-NMR spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with HPβCD. The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/HPβCD complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.