Characterization of ternary solid dispersions of itraconazole, PEG 6000, and HPMC 2910 E5.
In order to reduce the crystallinity of PEG 6000, blends were prepared by spray drying and extrusion with the following polymers; PVP K25, PVPVA 64, and HPMC 2910 E5. The maximal reduction of crystallinity in PEG 6000 was obtained by co-spray drying with HPMC 2910 E5. In the next step the model drug Itraconazole was added to the blend and the resulting ternary solid dispersions were characterized. The results of this study show that the addition of PEG 6000 to the Itraconazole/HPMC 2910 E5 system leads to phase separation that in most cases gives rise to recrystallization of either PEG 6000 or Itraconazole. For all ternary dispersions containing 20% of Itraconazole the drug was highly amorphous and the dissolution was improved compared to the binary 20/80 w/w Itraconazole/HPMC 2910 E5 solid dispersion. For all ternary dispersions containing 40% of Itraconazole, the drug was partially crystalline and the dissolution was lower than the dissolution of the binary 40/60 w/w Itraconazole/HPMC 2910 E5 dispersion. These results show that provided Itraconazole is highly amorphous the addition of PEG 6000 to HPMC 2910 E5 leads to an increase in drug release.
Janssens
Sandrien
S
Laboratorium voor Farmacotechnologie en Biofarmacie, K.U.Leuven, Leuven, Belgium.
de Armas
Hector Novoa
HN
Roberts
Clive J
CJ
Van den Mooter
Guy
G
D000935:Antifungal Agents / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D004337:Drug Carriers; D004339:Drug Compounding; D065347:Hypromellose Derivatives; D017964:Itraconazole / Q000737:chemistry*; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008956:Models, Chemical; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D014753:Vinyl Compounds / Q000737:chemistry
D000935:Antifungal Agents; D004337:Drug Carriers; D011759:Pyrrolidines; D014753:Vinyl Compounds; C402301:poly(vinylpyrrolidone-co-vinyl-acetate); D017964:Itraconazole; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D008747:Methylcellulose; D011205:Povidone