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Naji, M. |
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Motta, Antonella |
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Aletan, Dirar |
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Mohamed, Tarek |
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Ertürk, Emre |
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Taccardi, Nicola |
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Kononenko, Denys |
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Petrov, R. H. | Madrid |
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Alshaaer, Mazen | Brussels |
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Bih, L. |
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Casati, R. |
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Muller, Hermance |
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Kočí, Jan | Prague |
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Šuljagić, Marija |
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Kalteremidou, Kalliopi-Artemi | Brussels |
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Azam, Siraj |
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Ospanova, Alyiya |
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Blanpain, Bart |
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Ali, M. A. |
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Popa, V. |
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Rančić, M. |
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Ollier, Nadège |
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Azevedo, Nuno Monteiro |
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Landes, Michael |
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Rignanese, Gian-Marco |
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Holm, René
University of Southern Denmark
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (17/17 displayed)
- 2024Impact of drug compounds mechanical/deformation properties on the preparation of nano- and microsuspensionscitations
- 2024Impact of drug compounds mechanical/deformation properties on the preparation of nano- and microsuspensionscitations
- 2024A Systematic Investigation of Process Parameters for Small-Volume Aqueous Suspension Production by the Use of Focused Ultrasonication
- 2024A Systematic Investigation of Process Parameters for Small-Volume Aqueous Suspension Production by the Use of Focused Ultrasonication
- 2024Is roller milling – the low energy wet bead media milling – a reproducible and robust milling method for formulation investigation of aqueous suspensions?citations
- 2021Simultaneous determination of cyclodextrin stability constants as a function of pH and temperature – A tool for drug formulation and process designcitations
- 2020In Vivo Performance of Innovative Polyelectrolyte Matrices for Hot Melt Extrusion of Amorphous Drug Systemscitations
- 2019Modified Polymer Matrix in Pharmaceutical Hot Melt Extrusion by Molecular Interactions with a Carboxylic Coformercitations
- 2019Montmorillonite-surfactant hybrid particles for modulating intestinal P-glycoprotein-mediated transportcitations
- 2018Influence of PVP molecular weight on the microwave assisted in situ amorphization of indomethacincitations
- 2018Comparison of two DSC-based methods to predict drug-polymer solubilitycitations
- 2017Amorphization within the tabletcitations
- 2016Roller compaction scale-up using roll width as scale factor and laser-based determined ribbon porosity as critical material attributecitations
- 2016Glass solution formation in water - In situ amorphization of naproxen and ibuprofen with Eudragit® E POcitations
- 2015Evaluation of drug-polymer solubility curves through formal statistical analysiscitations
- 2013Preparation of an amorphous sodium furosemide salt improves solubility and dissolution rate and leads to a faster Tmax after oral dosing to ratscitations
- 2008Characterization and physical stability of spray dried solid dispersions of probucol and PVP-K30citations
Places of action
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article
Influence of PVP molecular weight on the microwave assisted in situ amorphization of indomethacin
Abstract
<p>In situ amorphization is an approach that enables a phase transition of a crystalline drug to its amorphous form immediately prior to administration. In this study, three different polyvinylpyrrolidones (PVP K12, K17 and K25) were selected to investigate the influence of the molecular weight of the polymer on the degree of amorphization of the model drug indomethacin (IND) upon microwaving. Powder mixtures of crystalline IND and the respective PVP were compacted at 1:2 (w/w) IND:PVP ratios, stored at 54% RH and subsequently microwaved with a total energy input of 90 or 180 kJ. After storage, all compacts had a similar moisture content (∼10% (w/w)). Upon microwaving with an energy input of 180 kJ, 58 ± 4% of IND in IND:PVP K12 compacts was amorphized, whereas 31 ± 8% of IND was amorphized by an energy input of 90 kJ. The drug stayed fully crystalline in all IND:PVP K17 and IND:PVP K25 compacts. After plasticization by moisture, PVP K12 reached a Tg below ambient temperature (16 ± 2 °C) indicating that the Tg of the plasticized polymer is a key factor for the success of in situ amorphization. DSC analysis showed that the amorphized drug was part of a ternary glass solution consisting of IND, PVP K12 and water. In dissolution tests, IND:PVP K12 compacts showed a delayed initial drug release due to a lack of compact disintegration, but reached a higher total drug release eventually. In summary, this study showed that the microwave assisted in situ amorphization was highly dependent on the Tg of the plasticized polymer.</p>