目的 采用流化床包衣工艺制备速释型伊曲康唑固体分散体载药微丸.方法 以常见的亲水性辅料为载体材料,溶剂法制备水不溶性药伊曲康唑的固体分散溶液,然后将其喷雾干燥共沉淀于流化床底喷锅内的蔗糖丸芯表面上,直接形成速释型伊曲康唑固体分散体载药微丸,并对其药物溶出度、晶型表征、外观性状、以及溶剂残留等进行系统评价.结果 制备的伊曲康唑载药微丸外观光洁美观,药物以无定形或分子态存在于载药层中,符合固体分散体结构特征.HPMC ES/伊曲康唑(1.5∶1,w/w)固体分散体载药微丸的药物溶出迅速,15 min可达80％以上.为保证溶剂残留在药典规定的限度内,制备的伊曲康唑载药微丸需要在真空80℃干燥6h以上.结论 采用流化床底喷上药包衣技术制备速释型伊曲康唑固体分散体载药微丸,质量可控,工艺可行.%OBJECTIVE To develop immediate-released itraconazole-loaded pellets prepared by fluidized bed spray coating. METHODS With common hydrophilic excipients( HPMC E5, PVP K30, PEG6000, and Poloxamer 188) as the carrier material, solid dispersion solution(dichloromethane-ethanol, 1:1, V/V)containing water-insoluble itraconazole was prepared, and then was sprayed on the surface of the sugar cores in fluidized bed to directly form immediate-reaease drug-loaded pellets containing itraconazole solid dispersion. Subsequently, its drug dissolution, crystal characterization, appearance, and residual solvent were evaluated. RESULTS The obtained pellets are clean and beautiful appearance. And itraconazole in the drug-loaded layer exists in amorphous or molecular state, meets with the solid dispersion structure. It was interesting that, the pellets containing HPMC E5/itraconazole( 1.5: 1 , w/w)solid dispersion were of rapid drug dissolution( 15 min up to 80% ). To ensure that residual solvent within the limits, it was necessary that the obtained pellets were dried more than 6 h at 80 t in vacuum. CONCLUSION It is feasible that immediate-release itraconazole-loaded pellets are prepared by fluidized bed spray coating technology, and its quality could be controlled.
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