How Does the Addition of Kollidon<sup>®</sup>VA64 Inhibit the Recrystallization and Improve Ezetimibe Dissolution from Amorphous Solid Dispersions?
Joanna Szafraniec-Szczęsny,
Agata Antosik-Rogóż,
Mateusz Kurek,
Karolina Gawlak,
Anna Górska,
Sebastian Peralta,
Justyna Knapik-Kowalczuk,
Daniel Kramarczyk,
Marian Paluch,
Renata Jachowicz
Affiliations
Joanna Szafraniec-Szczęsny
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
Agata Antosik-Rogóż
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
Mateusz Kurek
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
Karolina Gawlak
Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland
Anna Górska
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
Sebastian Peralta
Pharmacy and Pharmaceutical Technology Department, School of Pharmacy, University of Granada, Campus de Cartuja s/n., 18071 Granada, Spain
Justyna Knapik-Kowalczuk
Faculty of Science and Technology, Institute of Physics and SMCEBI, University of Silesia, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland
Daniel Kramarczyk
Faculty of Science and Technology, Institute of Physics and SMCEBI, University of Silesia, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland
Marian Paluch
Faculty of Science and Technology, Institute of Physics and SMCEBI, University of Silesia, 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland
Renata Jachowicz
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
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 composition-dependent 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.
