Dissolution enhancement of itraconazole by hot-melt extrusion alone and the combination of hot-melt extrusion and rapid freezing--effect of formulation and processing variables.
Mol Pharm
; 11(1): 186-96, 2014 Jan 06.
Article
em En
| MEDLINE
| ID: mdl-24283890
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 (12) 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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Portadores de Fármacos
/
Química Farmacêutica
/
Itraconazol
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Excipientes
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Congelamento
/
Metilcelulose
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Antifúngicos
Idioma:
En
Revista:
Mol Pharm
Assunto da revista:
BIOLOGIA MOLECULAR
/
FARMACIA
/
FARMACOLOGIA
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Estados Unidos