Release Control of Prednisolone from Suppository Prepared Using Powder of Pulverized Tablet

Akitoshi TATSUMI, Shoko ODA, Tomoko NAKAMOTO, Reiko MURAOKA, Yoshiko TAKAHASHI, Kuniyoshi TANAKA, Toshiyuki SHIKATA, Sumiyo TATSUMI, Noriko TAGAWA, Yoshiharu KOBAYASHI, Tsuneo HAMAGUCHI, Muneo KADOBAYASHI
2008 Yakugaku zasshi  
Prednisolone suppositories have been used successfully for the treatment of ulcerative colitis in hospital settings. However, the raw material of prednisolone suppository, JP prednisolone powder (JP Powder), was recently removed from the market. Therefore we studied the eŠects of raw material and suppository base on the release of prednisolone suppository for the purpose of designing a new suppository with similar eŠects to those of suppository prepared using JP powder (old suppository). New
more » ... positories consisting of the powder of pulverized tablet as raw material and Witepsol H-15 and Witepsol E-75 as suppository base were prepared according to the fusion method. Suppository release test was performed by reciprocating dialysis tube method with tapping (RDT method) and dialysis tubing method (DT method). Both RDT method and DT method were performed using a suppository dissolution apparatus (modiˆed JP disintegration apparatus) and a JP15 paddle apparatus, respectively. The test ‰uid was 50 mM phosphate buŠer solution (pH 7.4) maintained at 37±0.5°C. The results of release test by RDT method were similar to those of DT method. Release rate of prednisolone from the new suppository was much faster than that of old suppository. The addition of Witepsol E-75 to new suppository base markedly delayed the release of prednisolone from the new suppository. Release rate of prednisolone from the new suppository, consisting of pulverized tablet and Witepsol H-15 and Witepsol E-75 (76:24), corresponded well with that of the old suppository. It was suggested that this suppository could be used as incoming preparation of suppository prepared using JP powder.
doi:10.1248/yakushi.128.641 pmid:18379182 fatcat:6hjvdnxxrfdt7pjit5kpqht5i4