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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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Zhao, Min
Queen's University Belfast
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (10/10 displayed)
- 2023The effects of surfactants on the performance of polymer-based microwave-induced in situ amorphizationcitations
- 2022Stabilizing Mechanisms of β-Lactoglobulin in Amorphous Solid Dispersions of Indomethacincitations
- 2021Investigation into the role of the polymer in enhancing microwave-induced in situ amorphizationcitations
- 2021Investigation into the role of the polymer in enhancing microwave-induced in situ amorphizationcitations
- 2017Solid state characterisation and taste masking efficiency evaluation of polymer based extrudates of isoniazid for paediatric administrationcitations
- 2015Generation of hydrate forms of paroxetine HCl from the amorphous state: an evaluation of thermodynamic and experimental predictive approachescitations
- 2014The influence of drug physical state on the dissolution enhancement of solid dispersions prepared via hot-melt extrusion: A case study using olanzapinecitations
- 2014An investigation into the dehydration behavior of paroxetine HCl form i using a combination of thermal and diffraction methods: The identification and characterization of a new anhydrous formcitations
- 2012Identification and characterization of stoichiometric and nonstoichiometric hydrate forms of paroxetine HCl: Reversible changes in crystal dimensions as a function of water absorptioncitations
- 2012Development of fully amorphous dispersions of a low Tgdrug via co-spray drying with hydrophilic polymerscitations
Places of action
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article
Investigation into the role of the polymer in enhancing microwave-induced in situ amorphization
Abstract
Microwave-induced in situ amorphization is an emerging technology to tackle the persistent stability issue of amorphous solid dispersions (ASDs) during manufacture and storage. The aim of this study was to introduce new effective polymeric carriers with diverse properties to microwave-induced in situ amorphization and to better understand their functions in relation to the final dissolution performance of microwaved tablets. Tablets composed of indomethacin (IND) and different polymers were compacted, stored at 75% relative humidity for at least 1 week and microwaved at 1000 W to induce amorphization. A series of polymers, polyvinylpyrrolidone/vinyl acetate copolymers (PVP/VA) of different monomer weight ratios displaying varyingproperties in functional groupratio, hygroscopicity, molecular weight (M ), and glass transition temperature (T ) of the polymer were used as model carriers. The results suggested that more than 90% of IND was amorphized after 20 mins microwaving in all 20% (w/w) drug loaded tablets except for IND:PVAc tablets presenting approx. 36% residual crystallinity. Among them, tablets composed of PVP/VA I-335 and PVP K30 achieved complete in situ amorphization upon microwaving. Further analysis indicated that the influencing factors, polymer M and T of moisture-plasticized polymer, played a major role in microwave-induced in situ amorphization. In in vitro dissolution study, ASDs containing PVP/VA I-535 with moderate hydrophilicity and 0.96±1.92% IND residual crystallinity showed the most rapid and complete drug release among all formulations, presenting the most promising dissolution performance. Further study on the chemical stability of such formulation showed a statistically insignificant decrease of drug content after pre-conditioning and microwaving (P = 0.288 > 0.05).