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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
The influence of drug physical state on the dissolution enhancement of solid dispersions prepared via hot-melt extrusion: A case study using olanzapine
Abstract
In this study, we examine the relationship between the physical structure and dissolution behavior of olanzapine (OLZ) prepared via hot-melt extrusion in three polymers [polyvinylpyrrolidone (PVP) K30, polyvinylpyrrolidone-co-vinyl acetate (PVPVA) 6:4, and Soluplus® (SLP)]. In particular, we examine whether full amorphicity is necessary to achieve a favorable dissolution profile. Drug–polymer miscibility was estimated using melting point depression and Hansen solubility parameters. Solid dispersions were characterized using differential scanning calorimetry, X-ray powder diffraction, and scanning electron microscopy. All the polymers were found to be miscible with OLZ in a decreasing order of PVP>PVPVA>SLP. At a lower extrusion temperature (160°C), PVP generated fully amorphous dispersions with OLZ, whereas the formulations with PVPVA and SLP contained 14%–16% crystalline OLZ. Increasing the extrusion temperature to 180°C allowed the preparation of fully amorphous systems with PVPVA and SLP. Despite these differences, the dissolution rates of these preparations were comparable, with PVP showing a lower release rate despite being fully amorphous. These findings suggested that, at least in the particular case of OLZ, the absence of crystalline material may not be critical to the dissolution performance. We suggest alternative key factors determining dissolution, particularly the dissolution behavior of the polymers themselves.