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Showing 1 to 20 of 54 for “"Solid dispersion"”.
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IMPROVED AMORPHOUS SOLID DISPERSION PERFORMANCE USING BINARY POLYMER COMBINATIONS
With increasing attrition rate of new molecular entities due to sub-optimum aqueous
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Solubility Improvement by Solid Dispersion and Their Characterization: Indomethacin and Phenytoin
… and phenytoin by formulating ternary solid dispersions with a carrier and an adsorbent. Urea was used as the dispersing agent for indomethacin, while Kollidon<sup>®</sup>VA64 was used for both indomethacin and phenytoin. Solid dispersions with urea and indomethacin were prepared by the …
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Mixed Polysaccharide Esters for Amorphous Solid Dispersion Oral Drug Delivery Vehicles
… properties. We designed very effective amorphous solid dispersion (ASD) oral drug delivery polymers that prevented recrystallization of felodipine for hours and had excellent congruent polymer-drug release from the formulation at 20% drug loading. During the ring-opening reactions of the cellulose …
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Amorphous solid dispersion effects on in vitro solution concentrations of quercetin
… this by incorporating quercetin into amorphous solid dispersions (ASDs) with cellulose derivatives, eliminating crystallinity, and selectively releasing amorphous quercetin under simulated intestinal conditions (pH 6.8, 37C). Amorphous quercetin was dispersed in cellulose esters including …
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Modeling and Prediction of Amorphous Solid Dispersion Formation Using a Molecular Descriptor
… development. Delivering a drug in its amorphous solid-state is a potential method to overcome this issue, since the amorphous form has increased apparent aqueous solubility. However, the amorphous state is only metastable, and is thermodynamically driven to recrystallize. As a result, pure …
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Development and Evaluation of Ternary Amorphous Solid Dispersion of Poorly Water-soluble Compounds
Purpose: Ternary amorphous solid dispersion (TASD) containing an additional component compared to conventional binary ASD further enhances the effectiveness of this strategy. Recently, polyphenolic compounds such as curcumin (CUR) and resveratrol (RES) are shown to have synergistic antioxidant, …
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Predicting aqueous solubility of pharmaceutical agents by solid dispersion prepared by solvent evaporation method
… these strategies, solubility enhancement using solid dispersions is a leading method. To obtain a desirable increase in the solubility of a poorly-soluble compound, a good understanding of the molecular descriptors influencing the enhancement of solubility is essential. Therefore, the major …
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A Dual Approach of Salt Formation and Amorphous Solid Dispersion for Improved Oral Drug Delivery
… issue by combining salt formation and amorphous solid dispersion. Three weakly basic belonging to BCS class II drugs, clofazimine, aripiprazole, and haloperidol, were selected as model drugs. Ten salts of each drug were prepared with counterions with ΔpKa> 3 using a rotary evaporator and …
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Synthesis and Structure-property Evaluation of Novel Cellulosic Polymers as Amorphous Solid Dispersion Matrices for Enhanced Oral Drug Delivery
The use of amorphous solid dispersions (ASDs) is an effective and increasingly widely adopted approach for solubility and bioavailability enhancement of hydrophobic drugs. Cellulose derivatives have strong potential as ASD polymers. We demonstrate herein design, synthesis and structure-property …
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Development of Multivariate Powder X-ray Diffraction Techniques and Total Scattering Analyses to Enable Informatic Calibration of Solid Dispersion Potential
… was to introduce a novel method for predicting solid dispersion potential enabled by the ability to differentiate phase-separated co-solidified products from amorphous molecular solid dispersions. The central hypothesis states that a combination of materials properties exists that defines the …
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Application of Hansen Solubility Parameters and Thermomechanical Techniques to the Prediction of Miscibility of Amorphous Solid Dispersion. Investigating the role of cohesive energy and free volume to predict phase separation kinetics in hot-melt extruded amorphous solid dispersion using dynamic mechanical analyser, shear rheometer and solubility parameters data
Hot-melt extruded solid dispersion technique is increasingly employed to improve the solubility of poorly water-soluble drugs. The technique relies on the enhanced solubility of the amorphous form of the drug compared to its crystalline counterpart. These systems however are thermodynamically …
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The development of PVP-based solid dispersions using hot melt extrusion for the preparation of immediate release formulations
… formulation design. In this respect, research on solid dispersion of hydrophilic carrier has commenced a decade ago to resolve the problem of poorly soluble drug. However, the availability of solid dispersion is commercially limited due to the concerns of its physical instability, unpredictability …
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Investigation of Enhancement of Furosemide Solubilization with Cyclodextrins and a Novel Octenyl Succinate Anhydride Starch
… salt formation, cyclodextrin complexes and solid dispersion etc.</p> <p>Chapter 1 is an introduction into biopharmaceutics classification system (BCS) and novel drug solubilization techniques. It provides a brief history of the BCS and its application in drug development. It also looks into …
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Solid dispersions: formulation, characterisation, permeability and genomic evaluation
… reduced bioavailability. Formulation of solid dispersion of the drug has attracted considerable interest as a means of improving dissolution process of a range of poorly water soluble drugs. This current study investigates the formulation of solid dispersion for a range of poorly water …
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Evaluation and enhancement of physical stability of amorphous solid dispersions
… and gastrointestinal permeation.[8] Amorphous solid dispersions have been widely investigated to increase the gastrointestinal permeability, and the roles played by polymers and other excipients were also studied.[9],[10] However, even after 40 years of active research there have not been many …
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Versatility of hot-melt extrusion for dosage form design
… such as solubility enhancement, taste masking, solid state stability enhancement, and sustained release formulations for oral drug delivery, using one model drug, mefenamic acid. For solubility enhancement and taste masking formulations, Eudragit EPO was blended with MA in different ratios (20, …
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Physical analysis of solid solution formulations
Amorphous solid dispersion is one of the techniques used for enhancing dissolution rate of drugs with low aqueous solubility. The physical stability of the amorphous solid dispersion is the main challenge for their formulation development and commercialisation by pharmaceutical industry. The aims …
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Local drug delivery for treatment of brain tumor associated edema
… (DXM), dexamethasone sodium phosphate (DSP), and solid dispersion of cediranib (AZD/PVP) were achieved. Employing the solid dispersion technique to increase the solubility of cediranib was necessary to enhance its release. Therapeutic efficacy and systemic toxicity of local drug administration via …
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Cellulose-based amorphous solid dispersions enhance rifapentine delivery characteristics and dissolution kinetics in vitro
… rifapentine into pH-responsive amorphous solid dispersions with cellulose derivatives including: hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate suberate (CASub), and 5-carboxypentyl hydroxypropyl cellulose (CHC). Most amorphous solid dispersions reduced …
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Influence of hot melt extrusion processing parameters on the properties of a pharmaceutical formulation
… process that is widely used to produce a solid dispersion matrix. The aim of this dissertation is to evaluate different factors that will affect the pharmaceutical formulation properties that are produced using HME. For HME, there are different variables that will affect the product …
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