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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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Grohganz, Holger
University of Copenhagen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (43/43 displayed)
- 2024Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocainecitations
- 2024Anti-plasticizing effect of water on prilocaine and lidocainecitations
- 2024Influence of water and trehalose on α- and β-relaxation of freeze-dried lysozyme formulationscitations
- 2023Thermal investigation on hydrated co-amorphous systems of nicotinamide and prilocainecitations
- 2023Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Millingcitations
- 2022Effects of polymer addition on the non-strongly interacting binary co-amorphous system carvedilol-tryptophancitations
- 2022Impact of Molecular Surface Diffusion on the Physical Stability of Co-Amorphous Systemscitations
- 2021The influence of moisture on the storage stability of co-amorphous systemscitations
- 2021Comparison of co-former performance in co-amorphous formulationscitations
- 2020Determination of the Optimal Molar Ratio in Amino Acid-Based Coamorphous Systemscitations
- 2020Preparation of Co-Amorphous Systems by Freeze-Dryingcitations
- 2019Process Optimization and Upscaling of Spray-Dried Drug-Amino acid Co-Amorphous Formulationscitations
- 2019Exploring the chemical space for freeze-drying excipientscitations
- 2019Influence of Glass Forming Ability on the Physical Stability of Supersaturated Amorphous Solid Dispersionscitations
- 2019In situ co-amorphisation in coated tablets – The combination of carvedilol with aspartic acid during immersion in an acidic mediumcitations
- 2019Co-former selection for co-amorphous drug-amino acid formulationscitations
- 2018Influence of PVP molecular weight on the microwave assisted in situ amorphization of indomethacincitations
- 2018The Role of Glass Transition Temperatures in Coamorphous Drug-Amino Acid Formulationscitations
- 2018Glass-Transition Temperature of the β-Relaxation as the Major Predictive Parameter for Recrystallization of Neat Amorphous Drugscitations
- 2018In vitro and in vivo comparison between crystalline and co-amorphous salts of naproxen-argininecitations
- 2018The use of molecular descriptors in the development of co-amorphous formulationscitations
- 2018Glass-Transition Temperature of the β-Relaxation as the Major Predictive Parameter for Recrystallization of Neat Amorphous Drugs.
- 2018The Influence of Polymers on the Supersaturation Potential of Poor and Good Glass Formerscitations
- 2017Probing Pharmaceutical Mixtures during Milling:citations
- 2017Amorphization within the tabletcitations
- 2017Influence of preparation pathway on the glass forming abilitycitations
- 2017Performance comparison between crystalline and co-amorphous salts of indomethacin-lysinecitations
- 2017Correlation between calculated molecular descriptors of excipient amino acids and experimentally observed thermal stability of lysozymecitations
- 2016Influence of variation in molar ratio on co-amorphous drug-amino acid systemscitations
- 2016Glass forming ability of amorphous drugs investigated by continuous cooling- and isothermal transformationcitations
- 2016Development of a screening method for co-amorphous formulations of drugs and amino acidscitations
- 2016INFLUENCE OF THE COOLING RATE AND THE BLEND RATIO ON THE PHYSICAL STABILTIY OF CO-AMORPHOUS NAPROXEN/INDOMETHACINcitations
- 2016Glass solution formation in water - In situ amorphization of naproxen and ibuprofen with Eudragit® E POcitations
- 2016Investigation of physical properties and stability of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems prepared by quench cooling, coprecipitation and ball millingcitations
- 2016Properties of the Sodium Naproxen-Lactose-Tetrahydrate Co-Crystal upon Processing and Storagecitations
- 2015Formation mechanism of coamorphous drug−amino acid mixturescitations
- 2015Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Dryingcitations
- 2015Well-plate freeze-dryingcitations
- 2015Solid-state properties and dissolution behaviour of tablets containing co-amorphous indomethacin-argininecitations
- 2014Near-Infrared Imaging for High-Throughput Screening of Moisture-Induced Changes in Freeze-Dried Formulationscitations
- 2013Amino acids as co-amorphous stabilizers for poorly water soluble drugs--Part 1citations
- 2013In situ amorphisation of indomethacin with Eudragit® E during dissolutioncitations
- 2011Coamorphous drug systems: enhanced physical stability and dissolution rate of indomethacin and naproxencitations
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article
Anti-plasticizing effect of water on prilocaine and lidocaine
Abstract
<p>It is generally accepted that water, as an effective plasticizer, decreases the glass transition temperatures (T<sub>g</sub>s) of amorphous drugs, potentially resulting in physical instabilities. However, recent studies suggest that water can also increase the T<sub>g</sub>s of the amorphous forms of the drugs prilocaine (PRL) and lidocaine (LID), thus acting as an anti-plasticizer. To further understand the nature of the anti-plasticizing effect of water, interactions with different solvents and the resulting structural features of PRL and LID were investigated by Fourier transform infrared spectroscopy (FTIR) and quantum chemical simulations. Heavy water (deuterium oxides) was chosen as a solvent, as the deuterium and hydrogen atoms are electronically identical. It was found that substituting hydrogen with deuterium showed a minimal impact on the anti-plasticization of water on PRL. Ethanol and ethylene glycol were chosen as solvents to compare the hydrogen bonding patterns occurring between the hydroxyl groups of the solvents and PRL and LID. Comparison of the various T<sub>g</sub>s showed a weaker anti-plasticizing potential of these two solvents on PRL and LID. The frequency shifts of the amide C = O groups of PRL and LID due to the interactions with water, heavy water, ethanol, and ethylene glycol as observed in the FTIR spectra showed a correlation with the binding energies calculated by quantum chemical simulations. Overall, this study showed that the combination of weak hydrogen bonding and strong electrostatic contributions in hydrated PRL and LID could play an important role in inducing the anti-plasticizing effect of water on those drugs.</p>