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 ℃ 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.
SHAN Li, SHI Yan, WANG Yu-li, ZHAO Lin-lin, YANG Mei-yan, JIANG Qing-yu, GAO Chun-sheng.
Formulation and Characterization of Immediate-Release Itraconazole-Loaded Pellets Prepared by Fluidized Bed Spray Coating[J]. Chinese Pharmaceutical Journal, 2013, 48(1): 54-58
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