Characterization of ternary solid dispersions of Itraconazole in polyethylene glycol 6000/polyvidone-vinylacetate 64 blends.
The good compatibility between Itraconazole and polyvidone-vinylacetate 64 (PVPVA 64) was pointed out previously. However, the dissolution properties of these systems left room for improvement. Therefore polyethylene glycol 6000 (PEG 6000), known for its solubilizing and wetting properties, was added to the PVPVA 64 matrix. Physicochemical analysis showed that up to 10% of PEG 6000 could be mixed with PVPVA 64. Addition of 10%, 20% or 40% of Itraconazole rendered amorphous solid dispersions consisting of a ternary mixed phase and a PVPVA 64 rich amorphous phase. If the PEG 6000 fraction was elevated up to 25% of the carrier, the PEG 6000 crystallinity degree was around 73+/-0.6%. Up to 20% of Itraconazole could be molecularly dispersed in the 25/75 w/w polymer blend. An Itraconazole melting peak could be detected for the sample containing 40% of drug. Dissolution experiments showed that no benefit was obtained by adding PEG 6000 to the PVPVA 64 matrix for samples containing up to 20% of Itraconazole. The dissolution of the ternary dispersions with 40% of Itraconazole on the other hand showed improvement compared to binary Itraconazole/PVPVA 64 dispersions.
Janssens
Sandrien
S
Laboratorium voor Farmacotechnologie en Biofarmacie, Katholieke Universiteit Leuven, Leuven, Belgium.
de Armas
Hector Novoa
HN
D'Autry
Ward
W
Van Schepdael
Ann
A
Van den Mooter
Guy
G
D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D003890:Desiccation; D008401:Gas Chromatography-Mass Spectrometry; D017964:Itraconazole / Q000008:administration & dosage / Q000737:chemistry*; D011092:Polyethylene Glycols; D011205:Povidone / Q000737:chemistry; D011208:Powders; D012995:Solubility; D013696:Temperature; D014753:Vinyl Compounds / Q000737:chemistry; D014961:X-Ray Diffraction
D000935:Antifungal Agents; D011208:Powders; D014753:Vinyl Compounds; D017964:Itraconazole; D011092:Polyethylene Glycols; D011205:Povidone; C011566:vinyl acetate