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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
Places of action
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article
Precipitation of a poorly soluble model drug during in vitro lilpolysis
Abstract
Precipitation of cinnarizine during in vitro lipolysis of a self-microemulsifying drug delivery system (SMEDDS) was characterized to gain a better understanding of the mechanisms behind the precipitation. During in vitro lipolysis of the SMEDDS with or without cinnarizine, samples were taken at several timepoints and ultracentrifuged. Cinnarizine content in the pellet increased from 4% to 59% during lipolysis. The precipitation of cinnarizine during in vitro lipolysis correlated well with the degree of lipid digestion, determined by sodium hydroxide addition. The pellet from the endpoint of lipolysis was isolated and subjected to dissolution in biorelevant media. Dissolution rate of cinnarizine from pellets containing precipitated cinnarizine was initially 10-fold higher than dissolution from blank pellet spiked with crystalline cinnarizine, reaching more than 50% drug dissolved in the first minute. Pellets were further characterized by X-ray powder diffraction (XRPD) and polarized light microscopy (PLM). Both methods indicated the presence of liquid crystalline phases of calcium fatty acid soaps, but no presence of crystalline cinnarizine in the pellet. Overall, dissolution studies along with XRPD and PLM analysis indicate that cinnarizine precipitating during in vitro lipolysis of this SMEDDS is not crystalline, suggesting an either amorphous form or a molecular dispersion.