| People | Locations | Statistics |
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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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Löbmann, Korbinian
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (49/49 displayed)
- 2024Exploring the effect of protein secondary structure on the solid state and physical stability of protein-based amorphous solid dispersionscitations
- 2024Investigating the influence of protein secondary structure on the dissolution behavior of β-lactoglobulin-based amorphous solid dispersionscitations
- 2023The effects of surfactants on the performance of polymer-based microwave-induced in situ amorphizationcitations
- 2022Development of a multiparticulate drug delivery system for in situ amorphisationcitations
- 2022Stabilizing Mechanisms of β-Lactoglobulin in Amorphous Solid Dispersions of Indomethacincitations
- 2021The Influence of Temperature and Viscosity of Polyethylene Glycol on the Rate of Microwave-Induced In Situ Amorphization of Celecoxibcitations
- 2021The Influence of Drug-Polymer Solubility on Laser-Induced In Situ Drug Amorphization Using Photothermal Plasmonic Nanoparticlescitations
- 2021The effect of the molecular weight of polyvinylpyrrolidone and the model drug on laser-induced in situ amorphizationcitations
- 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
- 2021Utilizing Laser Activation of Photothermal Plasmonic Nanoparticles to Induce On-Demand Drug Amorphization inside a Tabletcitations
- 2021Microwave-Induced in Situ Drug Amorphization Using a Mixture of Polyethylene Glycol and Polyvinylpyrrolidonecitations
- 2021The Use of Glycerol as an Enabling Excipient for Microwave-Induced In Situ Drug Amorphizationcitations
- 2021Studying the impact of the temperature and sorbed water during microwave-induced In Situ amorphizationcitations
- 2021Comparison of co-former performance in co-amorphous formulationscitations
- 2021Enabling formulations of aprepitantcitations
- 2020Hot Melt Coating of Amorphous Carvedilolcitations
- 2020The influence of drug and polymer particle size on the in situ amorphization using microwave irradiationcitations
- 2019Process Optimization and Upscaling of Spray-Dried Drug-Amino acid Co-Amorphous Formulationscitations
- 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
- 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
- 2017Hot Melt Extrusion and Spray Drying of Co-amorphous Indomethacin-Arginine With Polymerscitations
- 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
- 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
- 2015Predicting Crystallization of Amorphous Drugs with Terahertz Spectroscopy.
- 2015Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Dryingcitations
- 2015Evaluation of drug-polymer solubility curves through formal statistical analysiscitations
- 2015Solid-state properties and dissolution behaviour of tablets containing co-amorphous indomethacin-argininecitations
- 2015Predicting Crystallization of Amorphous Drugs with Terahertz Spectroscopycitations
- 2014The influence of pressure on the intrinsic dissolution rate of amorphous indomethacincitations
- 2013Amino acids as co-amorphous stabilizers for poorly water soluble drugs--Part 1citations
- 2011Coamorphous drug systems: enhanced physical stability and dissolution rate of indomethacin and naproxencitations
Places of action
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article
Coamorphous drug systems: enhanced physical stability and dissolution rate of indomethacin and naproxen
Abstract
One of the challenges in drug development today is that many new drug candidates are poorly water-soluble, and one of the approaches to overcome this problem is to transfer a crystalline drug into its amorphous form, thus increasing dissolution rate and apparent solubility of the compound. In this study, a coamorphous drug/drug combination between the two nonsteroidal anti-inflammatory drugs, naproxen and ¿-indomethacin, was prepared and investigated. At molar ratios of 2:1, 1:1 and 1:2, the drugs were quench cooled in order to obtain a coamorphous binary phase. Physical stability was examined at 277.15 and 298.15 K under dry conditions (phosphorus pentoxide) and analyzed with X-ray powder diffraction (XRPD). Intrinsic dissolution testing was carried out to identify dissolution advantages of the coamorphous form over its crystalline counterparts or amorphous indomethacin. Fourier transform infrared spectroscopy (FTIR) was used for analyses at the molecular level to detect potential molecular interactions. Differential scanning calorimetry (DSC) thermograms were employed to assess the glass transition temperatures (T(g)), and the results were compared with predicted T(g)s from the Gordon-Taylor equation. Results showed that naproxen could be made amorphous in combination with indomethacin while this was not possible with naproxen alone. Peak shifts in the FTIR spectra indicated molecular interactions between both drugs, and it is suggested that the two drugs formed a heterodimer. Therefore, samples at the 1:2 and 2:1 ratios showed recrystallization of the excess drug upon storage whereas the 1:1 ratio samples remained amorphous. Intrinsic dissolution testing showed increased dissolution rate of both drugs in the coamorphous form as well as a synchronized release for the 1:1 coamorphous blend. All T(g)s displayed negative deviations from the Gordon-Taylor equation with the 1:1 ratio showing the largest deviation. In a novel approach of predicting the glass transition temperature, the 1:1 drug ratio was inserted as an individual component in the Gordon-Taylor equation with the excess drug representing the second compound. This approach resulted in a good fit to the experimentally determined T(g)s.