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Showing 1 to 20 of 34 for “"Amorphous solid dispersions"”.
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Dissolution Behavior of Amorphous Solid Dispersions
… drug. Solubility enhancement techniques, such as amorphous solid dispersions (ASDs), can be used in oral dosage forms to increase the apparent solubility of the drug in the gastrointestinal tract thus increasing the bioavailability of the drug. However, the drug solution generated from the …
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Evaluation and enhancement of physical stability of amorphous solid dispersions
… of poorly water-soluble drugs.[1],[2] The amorphous forms of APIs have attracted considerable attention as the amorphous forms tend to exhibit significantly higher levels of supersaturation in aqueous media when compared to the crystalline forms.[3],[4] For drugs which bioavailability is …
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ACID-BASE INTERACTIONS IN AMORPHOUS SOLID DISPERSIONS: FORMULATION STRATEGY FOR TYROSINE KINASE INHIBITORS
Song, Yang. Ph.D., Purdue University, December 2015. Acid-base Interactions in
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Nuclear Magnetic Resonance for the Characterisation of Hot-Melt Extruded Pharmaceutical Amorphous Solid Dispersions
… poor solubility. The formulation of drug/polymer amorphous solid dispersions (ASDs) is one of the most successful strategies for improving the oral bioavailability of poorly soluble APIs. Hot-melt extrusion (HME) is one method for preparing ASDs that is growing in importance in the pharmaceutical …
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Cellulose-based amorphous solid dispersions enhance rifapentine delivery characteristics and dissolution kinetics in vitro
… by incorporating 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 …
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Assessment of nanocomposites vs. amorphous solid dispersions for dissolution enhancement of bcs class ii drugs
… formulations (nanocomposites) and amorphous solid dispersions, shortly ASDs, are two major pharmaceutical formulation platforms used for the bioavailability enhancement of poorly water-soluble drugs. While they both have several advantages-disadvantages, a scientific comparative …
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The effect of additives on the molecular mobility, physical stability and dissolution of amorphous solid dispersions
… compounds. However, crystallization of the amorphous phase during storage or dissolution could negate the solubility advantage. The objectives were to (i) develop an accelerated testing method for predicting the solid-state physical stability of drugs in amorphous solid dispersions (ASD), …
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Drug-Polymer and Drug-Lipid Miscibility for the Development of Amorphous Solid Dispersions and Solid Lipid Nanoparticles
… in the treatment of prostatic carcinoma. FLT amorphous solid dispersions (SDs) and solid lipid nanoparticles (SLNs) were prepared to overcome limited solubility. Investigation of drug-polymer and drug-lipid miscibility was carried out to enhance drug performance by assessing solubility and …
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Investigating Crystallization Tendency, Miscibility and Molecular interactions of drug-polymer systems for the development of amorphous solid dispersions
… the performance of prepared or reported SDs (solid dispersions). Crystallization tendencies of five different drugs [i.e. Curcumin (CUR), indomethacin (IND), flutaminde (FLU), dipyridamole (DIP), griseofulvin (GRI)] in absence and presence of four different polymers [i.e. polyethylene glycol …
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The Influence of PVAP on the Stability of Amorphous Solid Dispersions of Itraconazole Produced using Hot Melt Extrusion Technology
… (ITZ) in neutral pH aqueous media and in the solid-state during storage over time. Polyvinyl pyrrolidone vinyl acetate (PVPVA) was incorporated into PVAP as a carrier matrix with the aim of lowering the melt viscosity and increasing the plasticity of PVAP while maintaining its high glass …
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Investigation of Amorphous Solid Dispersions of Poorly Water-soluble Drugs in Poly (2-hydroxyethyl Methacrylate) Hydrogels for Enhanced Solubility and Controlled Release
… was to investigate the potential of applying amorphous solid dispersions (ASD) in crosslinked PHEMA hydrogels to enhance the dissolution behavior of poorly water-soluble drugs. The first part of the study identifies physicochemical properties affecting the solid state and physical stability of …
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Development of Methods to Predict and Enhance the Physical Stability of Hot Melt Extruded Solid Dispersions
The application of amorphous solid dispersions is one of the most widely used formulation strategies for the enhancement of in-vitro and in-vivo performance of poorly water-soluble drugs. However, because of their meta-stable nature, the physical stability of amorphous solid dispersions has been …
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Solubility Enhancement via Melt Extrusion: Drug-polymer Solubility, Physicochemical Characterization and Quality by Design
… poor biopharmaceutical properties. Formation of solid dispersions is a very widely applied technique for solubility enhancement of water insoluble drugs. In order to form stable solid dispersions it is important to select appropriate excipients that will maintain the drug in its amorphous form …
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A Dual Approach of Salt Formation and Amorphous Solid Dispersion for Improved Oral Drug Delivery
… solve this 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 …
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Characterization of different hydrophilic polymers and their applicability in hot melt extrusion technology
… administration, and mainly include conventional solid dosage forms such as pellets, tablets, and/ or milled material filled in capsules. Since most of the actives studied under current research have low aqueous solubility, it was necessary to utilize a novel technology such as hot melt extrusion …
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ACID-BASE REACTIONS IN DIFFERENT SOLID-STATE FORMS
… systems with samples including salts, amorphous solid dispersions, and in formulated products. Salt formation of active pharmaceutical ingredients (APIs) is widely recognized as one of the most commonly used approaches to modify the solubility and dissolution rate. Formulating poorly …
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Amorphous solid dispersion effects on in vitro solution concentrations of quercetin
… to achieve 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 …
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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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Further exploring the pharmaceutical applications of novel microwave-induced in situ amorphization
… and problematic downstream processing issues of amorphous solid dispersions (ASDs). However, the current available research in this field is limited and some issues identified in the existing studies require further exploration. The aims of this study were to fill in these gaps by: 1) …
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