How Does the Addition of Kollidon®VA64 Inhibit the Recrystallization and Improve Ezetimibe Dissolution from Amorphous Solid Dispersions?
| Autor: | Renata Jachowicz, Anna Górska, Agata Antosik-Rogóż, Daniel Kramarczyk, Marian Paluch, Karolina Gawlak, Joanna Szafraniec-Szczęsny, Justyna Knapik-Kowalczuk, Sebastián Peralta, Mateusz Kurek |
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| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Recrystallization (geology)
Materials science Solid dispersion Pharmaceutical Science lcsh:RS1-441 dissolution 02 engineering and technology macromolecular substances 030226 pharmacology & pharmacy Article Contact angle lcsh:Pharmacy and materia medica 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Vinyl acetate Dissolution contact angle chemistry.chemical_classification solid dispersion technology industry and agriculture Polymer 021001 nanoscience & nanotechnology Ezetimibe amorphization Amorphization Amorphous solid chemistry Chemical engineering Spray drying Wetting 0210 nano-technology ezetimibe |
| Zdroj: | Digibug: Repositorio Institucional de la Universidad de Granada Universidad de Granada (UGR) Digibug. Repositorio Institucional de la Universidad de Granada instname Pharmaceutics, Vol 13, Iss 147, p 147 (2021) Pharmaceutics Volume 13 Issue 2 |
| Popis: | 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. Polish National Science Centre, grant number 2015/16/W/NZ7/00404 |
| Databáze: | OpenAIRE |
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