Abstract:
:We investigated the effects of the hot-melt extrusion (HME) process on the properties of itraconazole (ITZ) amorphous solid dispersions made by thin film freezing (TFF) technology. The ITZ-HPMCAS L (1:2) TFF composition exhibited limited drug release in acidic media. HME of the ITZ-HPMCAS TFF composition with hydrophilic carriers improved the drug release rate in acidic media. The type and level of hydrophilic carrier in the composition affected the dissolution profiles of the extrudates. A design of experiments (DoE) study was conducted to elucidate those effects. Hot-melt extrusion processing variables such as extrusion temperature and screw configuration also played a critical role on the properties of the extruded compositions. A higher degree of mixing reduced the crystallinity of semicrystalline excipients and favored the drug release in the acidic media; moreover, the drug precipitation rate in the neutral pH media was reduced.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Lang B,McGinity JW,Williams RO 3rddoi
10.1021/mp4003706subject
Has Abstractpub_date
2014-01-06 00:00:00pages
186-96issue
1eissn
1543-8384issn
1543-8392journal_volume
11pub_type
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