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Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy
K. Punčochová, B. Vukosavljevic, J. Hanuš, J. Beránek, M. Windbergs, F. Štěpánek,
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- hydrofobní a hydrofilní interakce MeSH
- kinetika MeSH
- konfokální mikroskopie metody MeSH
- krystalizace MeSH
- morfoliny chemie MeSH
- nosiče léků chemie MeSH
- polyethylenglykoly chemie MeSH
- polymery chemie MeSH
- polyvinyly chemie MeSH
- povidon chemie MeSH
- Ramanova spektroskopie metody MeSH
- rozpustnost MeSH
- stabilita léku MeSH
- uvolňování léčiv * MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
In this study, we investigated the release mechanism of the poorly water soluble drug aprepitant from different amorphous solid dispersions using confocal Raman microscopy (CRM). Solid dispersions were fabricated based on either Soluplus®, as an amphiphilic copolymer and solubilizer, or on polyvinylpyrrolidone, as a hydrophilic polymer, in order to elucidate the influence of the polymer characteristics on the drug form and dissolution mechanisms. Aprepitant exhibited its amorphous form in both solid dispersions. However, the release differed depending on the polymer. The high complexation effect of Soluplus was shown to be a crucial factor for stabilization of the amorphous drug, resulting in continuous release without any recrystallization of aprepitant. In contrast, solid dispersions based on polyvinylpyrrolidone showed a different mechanism of dissolution; due to the good affinity of PVP and water, the polymer is dissolving fast, leading to phase separation and local recrystallization of the drug. The study highlights the complexity of release processes from solid dispersions and elucidates the influence of the polymer on drug release kinetics.
Citace poskytuje Crossref.org
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- $a Punčochová, Kateřina $u Department of Chemical Engineering, University of Chemistry and Technology Prague, Prague 6, Czech Republic; Zentiva, k.s., U Kabelovny 130, Prague 10, Czech Republic.
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- $a Non-invasive insight into the release mechanisms of a poorly soluble drug from amorphous solid dispersions by confocal Raman microscopy / $c K. Punčochová, B. Vukosavljevic, J. Hanuš, J. Beránek, M. Windbergs, F. Štěpánek,
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- $a In this study, we investigated the release mechanism of the poorly water soluble drug aprepitant from different amorphous solid dispersions using confocal Raman microscopy (CRM). Solid dispersions were fabricated based on either Soluplus®, as an amphiphilic copolymer and solubilizer, or on polyvinylpyrrolidone, as a hydrophilic polymer, in order to elucidate the influence of the polymer characteristics on the drug form and dissolution mechanisms. Aprepitant exhibited its amorphous form in both solid dispersions. However, the release differed depending on the polymer. The high complexation effect of Soluplus was shown to be a crucial factor for stabilization of the amorphous drug, resulting in continuous release without any recrystallization of aprepitant. In contrast, solid dispersions based on polyvinylpyrrolidone showed a different mechanism of dissolution; due to the good affinity of PVP and water, the polymer is dissolving fast, leading to phase separation and local recrystallization of the drug. The study highlights the complexity of release processes from solid dispersions and elucidates the influence of the polymer on drug release kinetics.
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- $a Vukosavljevic, Branko $u Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbruecken, Germany; Helmholtz Centre for Infection Research (HZI) and Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Delivery, Saarbruecken, Germany.
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- $a Windbergs, Maike $u Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbruecken, Germany; Helmholtz Centre for Infection Research (HZI) and Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Delivery, Saarbruecken, Germany. Electronic address: m.windbergs@mx.uni-saarland.de.
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- $a Štěpánek, František $u Department of Chemical Engineering, University of Chemistry and Technology Prague, Prague 6, Czech Republic. Electronic address: Frantisek.Stepanek@vscht.cz.
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