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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
Stability and intrinsic dissolution of vacuum compression molded amorphous solid dispersions of efavirenz
Abstract
<p>In this study, the stability and intrinsic dissolution of vacuum compression molded (VCM) amorphous solid dispersions (ASDs) of efavirenz (EFV) were investigated in relation to its solubility limits in seven polymers determined by the melting point depression (MPD) method. The extrapolated solubility limits of EFV at 22 °C ranged from 3 to 68% (w/w) with PVOH being the only polymer suggesting immiscibility with EFV according to both MPD and Hansen solubility parameters (HSPs). All ASDs with EFV loadings below or close to their calculated solubility limit did not show any signs of crystallization upon conditioning for 7 months at either 22 or 37 °C and 23 or 75% relative humidity. However, all ASDs with EFV loading above the solubility limit crystallized at high humidity, while the ASDs with cellulose derived carrier polymers proved kinetically stable at low humidity over 7 months. While the EFV intrinsic dissolution rates from the VCM ASDs were partly depending on the polymer dissolution rate, no correlation was observed between EFV matrix crystallization and its miscibility in the polymer. Altogether, the observations of the study underline the importance of combining preformulation miscibility determination and dissolution studies to rationally decide on both stability and viability of ASD formulations.</p>