OBJECTIVE To develop a pH-and time-based pellets of fluorouracil and evaluate their release characteristics in vitro.METHODS The blank pellets were prepared by extrusion-spheronization method;drug containing pellets were prepared by coating the blank pellets using the Fluorouracil-binder and the swelling material suspension in a fluidized bed coater.To achieve the controlling release,the drug containing pellets then were coated with ethyl cellulose as the controlled layer and Eudragit FS 30D as the outer coating enteric layer.The release behaviors of coated pellets for colon-specific delivery were evaluated in vitro.The effects of different swelling materials,the thicknesses of the swelling layer,EC layer and the enteric polymer layer on the release of fluorouracis were evaluated.RESULTS Tie dissolution rate was decided by the thickness of EC,swelling layer,enteric polymer and by the kinds of the swelling layer.The release characteristics of the fluorouracil pellets,prepared using CMS-Na and drug-binder suspension as the swelling layer with 30%(weight) coating level,using ethyl cellulose as the controlled layer with 12%(weight) coating level and Eudragit FS 30D as outer coating enteric layer with 20%(weight) coating level in the fluidized bed coater,met the requirement of colon-specific pellets.CONCLUSION The pH-and time-based pellets of fluorouracil for colon-specific delivery can be prepared using swelling layer, controlled layer and enteric layer by changing their coating level.
LI Lin-jun;HUNG Gui-hu;XI Yn-wei;YNG Xin-du;GU Ji-feng.
Study on Preparation and Drug Release of pH-and Time-Based Pellets of Fluorouracil for Colon-Specific Delivery [J]. Chinese Pharmaceutical Journal, 2007, 42(05): 357-361
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