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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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Frijlink, Henderik W.
University of Groningen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (32/32 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
- 2018The mechanism behind the biphasic pulsatile drug release from physically mixed poly(DL-lactic(-co-glycolic) acid)-based compactscitations
- 2017Dry powder inhalationcitations
- 2017Increased drug load and polymer compatibility of bilayered orodispersible filmscitations
- 2016Compacted Solid Dosage Form
- 2016Single dose sublingual testosterone and oral sildenafil versus a dual-route/dual-release fixed-dose combination tabletcitations
- 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 extrusion:application and characterizationcitations
- 2015Polymeric formulations for drug release prepared by hot melt extrusioncitations
- 2014Pharmacokinetics of a Prototype Formulation of Sublingual Testosterone and a Buspirone Tablet, Versus an Advanced Combination Tablet of Testosterone and Buspirone in Healthy Premenopausal Womencitations
- 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
- 2008Pore shape in the sodium chloride matrix of tablets after the addition of starch as a second componentcitations
- 2008Pore shape in the sodium chloride matrix of tablets after the addition of starch as a second componentcitations
- 2008Using the internal stress concept to assess the importance of moisture sorption-induced swelling on the moisture transport through the glassy HPMC filmscitations
- 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
- 2005The effect of powder blend and tablet structure on drug release mechanisms of hydrophobic starch acetate matrix tabletscitations
- 2005Location-dependent analysis of porosity and pore direction in tabletscitations
- 2005Location-dependent analysis of porosity and pore direction in tabletscitations
- 2004Pulmonary delivery of therapeutic peptides via dry powder inhalationcitations
- 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
- 2003Investigations into the stabilization of drugs by sugar glasses:III. The influence of various high-pH bufferscitations
- 2001Plasticisation of amylodextrin by moisture. Consequences for compaction behaviour and tablet propertiescitations
- 2001Inulin glasses for the stabilization of therapeutic proteinscitations
- 2001Effect of molecular weight and glass transition on relaxation and release behaviour of poly(DL-lactic acid) tabletscitations
Places of action
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article
Preparation and physicochemical evaluation of a new tacrolimus tablet formulation for sublingual administration
Abstract
The aim of this study was to develop a new fast-disintegrating tablet formulation containing 1mg tacrolimus for sublingual application. First, solid dispersions containing tacrolimus (2.5%, 5% and 10% w/w) incorporated in Ac-Di-Sol®and carriers (inulin 1.8kDa and 4kDa, and polyvinylpyrrolidone (PVP) K30) were prepared by freeze drying. Subsequently, a tablet formulation composed of a mixture of the solid dispersions, Ac-Di-Sol®, mannitol, Avicel®PH-101 and sodium stearyl fumarate was optimized concerning drug load in the solid dispersions and the type of carrier. Tablet weight was kept constant at 75mg by adjusting the amount of Avicel®PH-101. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) results indicated the absence of the drug in the crystalline state, which was confirmed by the scanning electron microscopy (SEM). These results suggest that tacrolimus incorporated in all of the solid dispersions was fully amorphous. Dissolution of the tablets containing solid dispersions with a low drug load highly depends on the type of carrier and increased in the order: PVP K30 <inulin 4kDa <inulin 1.8kDa. Solid dispersions with a drug load of 10% w/w incorporated in the carriers yielded optimal formulations. In addition, the physicochemical characteristics and the dissolution behavior of the tablet formulation containing inulin 1.8 kDa-based solid dispersions with a drug load of 10% w/w did not change after storage at 20°C/45%RH for 6 months indicating excellent storage stability. © 2012 Informa Healthcare USA, Inc.