How Does the Addition of Kollidon®VA64 Inhibit the Recrystallization and Improve Ezetimibe Dissolution from Amorphous Solid Dispersions?
Metadatos
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MDPI
Materia
Ezetimibe Solid dispersion Amorphization Dissolution Contact angle
Date
2021Referencia bibliográfica
Szafraniec-Szcz ˛esny, J.; Antosik-Rogóz, A.; Kurek, M.; ˙ Gawlak, K.; Górska, A.; Peralta, S.; Knapik-Kowalczuk, J.; Kramarczyk, D.; Paluch, M.; Jachowicz, R. How Does the Addition of Kollidon®VA64 Inhibit the Recrystallization and Improve Ezetimibe Dissolution from Amorphous Solid Dispersions? Pharmaceutics 2021, 13, 147. https://doi.org/10.3390/ pharmaceutics13020147
Patrocinador
Polish National Science Centre, grant number 2015/16/W/NZ7/00404Résumé
Amorphization serves as a strategy for the improvement of poor dissolution characteristics
of many drug compounds. However, in many formulations the content of polymeric stabilizer is high,
which is undesirable from the perspective of future applications. Thus, studying the compositiondependent stability of amorphous solid dispersions seems to be demanded. In this paper, we describe
the amorphization of ezetimibe, a lipid-lowering drug, in the spray drying process and investigate
the effect of polyvinylpyrrolidone-co-poly(vinyl acetate) (PVP/VA) content on the physical stability
and dissolution characteristics of the drug. Fully amorphous systems were obtained when the
concentration of the polymer in solid dispersion was as low as 20%. The amorphization led to the
dissolution enhancement by even 70%, with a noticeable sudden increase at around 40% of PVP/VA
content and very small variations for systems having 66–90% PVP/VA. It was also correlated to
wettability characteristics of solid dispersions, which may suggest that in the vicinity of 40% of the
polymer content, the behavior of the system becomes independent of the PVP/VA content.