Influence of polyethylene glycol chain length on compatibility and release characteristics of ternary solid dispersions of itraconazole in polyethylene glycol/hydroxypropylmethylcellulose 2910 E5 blends

Janssens, Sandrien; Denivelle, Samgar; Rombaut, Patrick; Mooter, Guy Van den

doi:10.1016/j.ejps.2008.06.014

Cited by 32 publications

(17 citation statements)

References 16 publications

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“…The majority of published research data or marketed solid dispersions are based on carriers like polyethylene glycol, polyvinylpyrrolidone, polyvinylpyrrolidone-co-vinylacetate 64 or hydroxypropyl methylcellulose (and derivatives) (2,3). Although combinations of polymers or polymers with surface active compounds have been proposed as a means to obtain new carrier systems with advanced properties (4)(5)(6), there is clear need for new carriers. We recently introduced the graft copolymer of ethyleneglycol and vinylalcohol (EG/ VA) as a potential new carrier in the formulation of solid dispersions.…”

Section: Introductionmentioning

confidence: 99%

Comparison Between Hot-Melt Extrusion and Spray-Drying for Manufacturing Solid Dispersions of the Graft Copolymer of Ethylene Glycol and Vinylalcohol

et al. 2010

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Section: Introductionmentioning

confidence: 99%

Comparison Between Hot-Melt Extrusion and Spray-Drying for Manufacturing Solid Dispersions of the Graft Copolymer of Ethylene Glycol and Vinylalcohol

et al. 2010

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“…PEG 4000 was chosen as a principal constituent of the gfSDF due to its relatively low melting temperature (Vasa et al, 2014) and good miscibility properties with other high tolerable gel-forming hydrophilic polymer such as hydroxypropyl methylcellulose (HPMC) and hydroxypropyl cellulose (HPC) (Janssens et al, 2008;Joshi, 2011;Wang and Tang, 2008). Tween 20 (polysorbate 20) was chosen as the plasticizer in order to increase the fluidity of the hot paste during syringe extrusion and to act as solubilizer for poorly soluble drugs (HLP of 16.7).…”

Section: Introductionmentioning

confidence: 99%

Novel in situ gel-forming solid dosage form (gfSDF) prepared by the simple syringe-based moulding: A screening study

Falavigna

Škalko‐Basnet

Cavallari

et al. 2017

European Journal of Pharmaceutical Sciences

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The aim of this study was to prepare and optimize a novel type of in situ gel-forming solid dosage form (gfSDF) to be used in the treatment of mucosal/skin ulcerations. For this purpose, a simple but reliable syringe-based hot melt/moulding method was employed. Chloramphenicol (antibiotic) and ibuprofen (anti-inflammatory) were chosen as model active pharmaceutical ingredients (APIs) to be loaded into the gfSDFs. To optimize the formulations, the gfSDFs of different compositions were studied in terms of APIs release from the matrix, solid-state characteristics, gellification properties and gfSDFs resistance to mechanical stress. Release studies showed that both APIs were released at a constant rate at different pH (pH5 and 7.4, respectively) and the changes in the formulation composition affected the release behaviour. Differential scanning calorimetry (DSC) results evidenced the complete solubilization of both API in the solid matrix. Texture analysis showed that the gfSDFs were capable of swelling once in a contact with aqueous environment and that the textural properties changed extemporaneously from the solid to gel form. The gel formed after hydration exhibited high cohesiveness and adhesiveness, an indication of good mucoadhesion properties. Friability testing confirmed satisfactory physical strength for a solid dosage form.

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“…Although the release of dexamethasone from PVA alone was very fast and from CAB extremely slow, a predictable reduction in the release rate of the drug was achieved by adding increasing proportions of CAB to the PVA/drug mixture . Researchers in Belgium have also demonstrated dissolution enhancement of the antifungal agent itraconazole and the anti‐HIV drug UC 781 through various binary combinations of HPMC, polyvinylpyrrolidone/vinyl acetate copolymer (PVP‐VA), polyethylene glycol, E100, and others . Recent studies in our laboratories have highlighted the effectiveness of polymer blends composed of novel cellulosic polymers including suberate, adipate, and sebacate esters of cellulose acetate propionate mixed with commercial cellulose‐based and synthetic polymers.…”

Section: Introductionmentioning

confidence: 99%

“…30 Researchers in Belgium have also demonstrated dissolution enhancement of the antifungal agent itraconazole and the anti-HIV drug UC 781 through various binary combinations of HPMC, polyvinylpyrrolidone/vinyl acetate copolymer (PVP-VA), polyethylene glycol, E100, and others. [31][32][33][34] Recent studies in our laboratories have highlighted the effectiveness of polymer blends composed of novel cellulosic polymers including suberate, adipate, and sebacate esters of cellulose acetate propionate mixed with commercial cellulose-based and synthetic polymers. Blending two moderately hydrophobic cellulosic polymers, or combining a hydrophobic cellulosic polymer with a more hydrophilic synthetic polymer, afforded synergistic crystal growth inhibition of the poorly soluble CYP-3A4 inhibitor ritonavir.…”

Section: Introductionmentioning

confidence: 99%

Pairwise Polymer Blends for Oral Drug Delivery

Marks

Wegiel

Taylor

et al. 2014

Journal of Pharmaceutical Sciences

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Blends of polymers with complementary properties hold promise for addressing the diverse, demanding polymer performance requirements in amorphous solid dispersions (ASDs), but we lack comprehensive property understanding for blends of important ASD polymers. Herein, we prepare pairwise blends of commercially available polymers polyvinylpyrrolidone (PVP), the cationic acrylate copolymer Eudragit 100 (E100), hydroxypropyl methylcellulose acetate succinate (HPMCAS), carboxymethyl cellulose acetate butyrate (CMCAB), hydroxypropyl methylcellulose (HPMC), and the new derivative cellulose acetate adipate propionate (CAAdP). This study identifies miscible binary blends that may find use, for example, in ASDs for solubility and bioavailability enhancement of poorly water-soluble drugs. Differential scanning calorimetry, FTIR spectroscopy, and film clarity were used to determine blend miscibility. Several polymer combinations including HPMCAS/PVP, HPMC/CMCAB, and PVP/HPMC appear to be miscible in all proportions. In contrast, blends of E100/PVP and E100/HPMC showed a miscibility gap. Combinations of water-soluble and hydrophobic polymers like these may permit effective balancing of ASD performance criteria such as release rate and polymer-drug interaction to prevent nucleation and crystal growth of poorly soluble drugs. Miscible polymer combinations described herein will enable further study of their drug delivery capabilities, and provide a potentially valuable set of ASD formulation tools.

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Influence of polyethylene glycol chain length on compatibility and release characteristics of ternary solid dispersions of itraconazole in polyethylene glycol/hydroxypropylmethylcellulose 2910 E5 blends

Cited by 32 publications

References 16 publications

Comparison Between Hot-Melt Extrusion and Spray-Drying for Manufacturing Solid Dispersions of the Graft Copolymer of Ethylene Glycol and Vinylalcohol

Comparison Between Hot-Melt Extrusion and Spray-Drying for Manufacturing Solid Dispersions of the Graft Copolymer of Ethylene Glycol and Vinylalcohol

Novel in situ gel-forming solid dosage form (gfSDF) prepared by the simple syringe-based moulding: A screening study

Pairwise Polymer Blends for Oral Drug Delivery

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