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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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Hinrichs, Wouter
University of Groningen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (17/17 displayed)
- 2024Combinations of arginine and pullulan reveal the selective effect of stabilization mechanisms on different lyophilized proteinscitations
- 2018The mechanism behind the biphasic pulsatile drug release from physically mixed poly(DL-lactic(-co-glycolic) acid)-based compactscitations
- 2016Compacted Solid Dosage Form
- 2015Protein release from water-swellable poly(d,l-lactide-PEG)-b-poly(ϵ-caprolactone) implantscitations
- 2015Protein Stability during Hot Melt Extrusion
- 2015Size and molecular flexibility of sugars determine the storage stability of freeze-dried proteinscitations
- 2015Protein Stability during Hot Melt Extrusion: The Effect of Extrusion Temperature, Hydrophilicity of Polymers and Sugar Glass Pre-stabilization
- 2015Polymeric formulations for drug release prepared by hot melt extrusioncitations
- 2013Designing CAF-adjuvanted dry powder vaccinescitations
- 2013Unraveling protein stabilization mechanismscitations
- 2012Preparation and physicochemical evaluation of a new tacrolimus tablet formulation for sublingual administrationcitations
- 2010Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tabletscitations
- 2006Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniquescitations
- 2005Inulin is a promising cryo- and lyoprotectant for PEGylated lipoplexescitations
- 2004Incorporation of lipophilic drugs in sugar glasses by lyophilization using a mixture of water and tertiary butyl alcohol as solventcitations
- 2003Investigations into the stabilization of drugs by sugar glassescitations
- 2001Inulin glasses for the stabilization of therapeutic proteinscitations
Places of action
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article
Incorporation of lipophilic drugs in sugar glasses by lyophilization using a mixture of water and tertiary butyl alcohol as solvent
Abstract
<p>In this study, anew and robust method was evaluated to prepare physically stable solid dispersions. Trehalose, sucrose, and two inulins having different chain lengths were used as carrier. Diazepam, nifedipine, Delta(9)-tetrahydrocannabinol, and cyclosporine A were used as model drugs. The sugar was dissolved in water and the drug in tertiary butyl alcohol (TBA). The two solutions were mixed in a 4/6 TBA/water volume ratio and subsequently freeze dried. Diazepam could be incorporated at drug loads up to 63% w/w. DSC measurements showed that, except in some sucrose dispersions, 97-100% of the diazepam was amorphous. In sucrose dispersions with high drug loads, about 10% of the diazepam had crystallised. After 60 days of exposure at 20degreesC and 45% relative humidity (RH), diazepam remained fully amorphous in inulin dispersions, whereas in trehalose and sucrose crystallization of diazepam occurred. The excellent physical stability of inulin containing solid dispersions can be attributed to the high glass transition temperature (T-g) of inulin. For the other drugs similar results were obtained. The residual amount of the low toxic TBA was only 0.1-0.5% w/w after freeze drying and exposure to 45% RH and 20degreesC. Therefore, residual TBA will not cause any toxicity problems. This study provides a versatile technique, to produce solid dispersions. Inulin glasses are preferred because they provide an excellent physical stability of the incorporated amorphous lipophilic drugs. (C) 2004 Wiley-Liss, Inc.</p>