Impact of low molecular weight excipient octaacetylmaltose on the liquid crystalline ordering and molecular dynamics in the supercooled liquid and glassy state of itraconazole
PBN-AR
Instytucja
Centrum Nanobiomedyczne (Uniwersytet im. Adama Mickiewicza w Poznaniu)
Informacje podstawowe
Główny język publikacji
en
Czasopismo
European Journal of Pharmaceutics and Biopharmaceutics
ISSN
0939-6411
EISSN
Wydawca
ELSEVIER SCIENCE BV
DOI
URL
Rok publikacji
2014
Numer zeszytu
3
Strony od-do
1094-1104
Numer tomu
88
Identyfikator DOI
Liczba arkuszy
0,50
Słowa kluczowe
en
Itraconazole
Solid dispersion
Molecular dynamics
Local mobility
Isostructural relaxation times
Aging
Streszczenia
Język
en
Treść
Different experimental and theoretical techniques were applied to investigate basic physical properties of very stable and homogeneous solid dispersions formed by itraconazole and octaacetylmaltose. Differential scanning calorimetry as well as semi-empirical calculations have indicated that liquid crystalline ordering in itraconazole was completely suppressed in the binary mixtures. Molecular dynamics studies with the use of broadband dielectric spectroscopy have shown that the width of the structural relaxation process becomes smaller and fragility drops in solid dispersions with respect to the pure itraconazole. Moreover, the dynamics of secondary relaxation processes was affected by acetylated maltose. As demonstrated, β- and γ-secondary modes shift to higher and lower frequencies, respectively. On the other hand, aging experiments revealed that isostructural relaxation times in the glassy state become systematically longer with the addition of modified carbohydrate. This is a very important finding in the context of the current discussion on the factors affecting physical stability of easily crystallizing APIs. It seems that beside intermolecular interactions and local reorientation, the global mobility might control the crystallization of amorphous solid dispersions. Finally, we have demonstrated that itraconazole in binary mixtures dissolves faster and to greater extent with respect to the crystalline and amorphous form of this API
Cechy publikacji
discipline:Nauki farmaceutyczne
discipline:Pharmacy
Original article
Original article presents the results of original research or experiment.
Oryginalny artykuł naukowy
Oryginalny artykuł naukowy przedstawia rezultaty oryginalnych badań naukowych lub eksperymentu.
Inne
System-identifier
PBN-R:612418
CrossrefMetadata from Crossref logo
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