Formulation and characterization of immediate-release itraconazole-loaded pellets prepared by fluidized bed spray coating / 中国药学杂志

ABSTRACT

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°C 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. Copyright 2013 by the Chinese Pharmaceutical Association.