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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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Müllertz, Anette
University of Copenhagen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (18/18 displayed)
- 2024Influence of preparation method and choice of phospholipid on co-amorphization, physical stability, and dissolution behavior of equimolar indomethacin-phospholipid systemscitations
- 2024Drug–Phospholipid Co-Amorphous Formulations: The Role of Preparation Methods and Phospholipid Selection
- 2023Amphotericin B and monoacyl-phosphatidylcholine form a stable amorphous complexcitations
- 2023Stability and intrinsic dissolution of vacuum compression molded amorphous solid dispersions of efavirenzcitations
- 2023Coating of Primary Powder Particles Improves the Quality of Binder Jetting 3D Printed Oral Solid Productscitations
- 2022Structured approach for designing drug-loaded solid products by binder jetting 3D printingcitations
- 2021Hot punching for loading of biodegradable microcontainers with budesonide-Soluplus filmcitations
- 2018The Influence of Polymers on the Supersaturation Potential of Poor and Good Glass Formerscitations
- 2016In Vivo Precipitation of Poorly Soluble Drugs from Lipid-Based Drug Delivery Systemscitations
- 2016Supersaturation of zafirlukast in fasted and fed state intestinal media with and without precipitation inhibitorscitations
- 2015Stabilisation of amorphous furosemide increases the oral drug bioavailability in ratscitations
- 2014Physical characterization of photocrosslinked poly(vinyl pyrrolidone) (PVP) hydrogels for drug delivery
- 2014Property profiling of biosimilar mucus in a novel mucus-containing in vitro model for assessment of intestinal drug absorptioncitations
- 2013Spray coating of microcontainers with eudragit using ferromagnetic shadow masks for controlled oral release of poorly water soluble drugs.
- 2013Preparation of an amorphous sodium furosemide salt improves solubility and dissolution rate and leads to a faster Tmax after oral dosing to ratscitations
- 2013Biodegradable microcontainers as an oral drug delivery system for poorly soluble drugs.
- 2010Precipitation of a poorly soluble model drug during in vitro lilpolysiscitations
- 2008Characterization and physical stability of spray dried solid dispersions of probucol and PVP-K30citations
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article
Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats
Abstract
A glass solution of the amorphous sodium salt of furosemide (ASSF) and polyvinylpyrrolidone (PVP) (80: 20 w/w%) was prepared by spray drying. It was investigated if PVP was able to stabilise ASSF during storage and dissolution and whether this influenced the in vivo performance of the glass solution after oral dosing to rats. The glass solution had a glass transition temperature of 121.3 +/- 0.5 degrees C, which was significantly higher than that of the pure drug (101.2 degrees C). ASSF in the glass solution was stable for at least 168 days when stored at 20 degrees C and 0% relative humidity. The glass solution exhibited fast dissolution in simulated intestinal medium, pH 6.5; the intrinsic dissolution rate was found to be 10.1 +/- 0.6 mg/cm(2)/min, which was significantly faster than the pure ASSF. When investigating the stability during dissolution in stimulated intestinal medium at pH 6.5, the ASSF in the glass solution showed signs of crystallinity after 1 min of dissolution, but crystallised to a lesser extent than pure ASSF. The stabilising effect of PVP on ASSF, led to improved relative oral bioavailability in rats of 263%, when compared to the pure ASSF. (C) 2015 Elsevier B.V. All rights reserved.