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https://www.readbyqxmd.com/read/28711592/producing-amorphous-solid-dispersions-via-co-precipitation-and-spray-drying-impact-to-physicochemical-and-biopharmaceutical-properties
#1
Amanda K P Mann, Luke Schenck, Athanas Koynov, Alfred C F Rumondor, Xiaoling Jin, Melanie Marota, Chad Dalton
Many small molecule active pharmaceutical ingredients (APIs) exhibit low aqueous solubility, and benefit from generation of amorphous dispersions of the API and polymer to improve their dissolution properties. Spray drying and hot melt extrusion are two common methods to produce these dispersions; however, for some systems these approaches may not be optimal, and it would be beneficial to have an alternative route. Herein, amorphous solid dispersions of Compound A, a low solubility weak acid, and copovidone were made by conventional spray drying and co-precipitation...
July 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28705623/water-induced-phase-separation-of-miconazole-poly-vinylpyrrolidone-co-vinyl-acetate-amorphous-solid-dispersions-insights-with-confocal-fluorescence-microscopy
#2
Sugandha Saboo, Lynne S Taylor
The aim of this study was to evaluate the utility of confocal fluorescence microscopy (CFM) to study the water-induced phase separation of miconazole-poly (vinylpyrrolidone-co-vinyl acetate) (mico- PVPVA) amorphous solid dispersions (ASDs), induced during preparation, upon storage at high relative humidity (RH) and during dissolution. Different fluoresecent dyes were added to drug-polymer films and the location of the dyes was evaluated using CFM. Orthogonal techniques, in particular atomic force microscopy (AFM) coupled with nanoscale infrared spectroscopy (AFM-nanoIR), were used to provide additional analysis of the drug-polymer blends...
July 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28689964/improving-the-solubility-of-nilotinib-through-novel-spray-dried-solid-dispersions
#3
Maikel Herbrink, Jan H M Schellens, Jos H Beijnen, Bastiaan Nuijen
The tyrosine kinase inhibitor nilotinib has a very low aqueous solubility and a low and variable oral bioavailability. A pharmaceutical formulation with an improved solubility may enhance the bioavailability and reduce the variability thereof and of the pharmacokinetics. The aim of this study was to enhance the solubility of nilotinib by developing a spray dried solid dispersion. A broad selection of polymer excipients were tested for solubilizing properties. The spray drying technique was used to produce solid dispersions of nilotinib hydrochloride (NH) in matrices of the best performing polymers...
July 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28687987/evaluation-of-the-crystallization-tendency-of-commercially-available-amorphous-tacrolimus-formulations-exposed-to-different-stress-conditions
#4
Niraj S Trasi, Hitesh S Purohit, Lynne S Taylor
PURPOSE: Tacrolimus, an immunosuppressant, is a poorly water soluble compound whereby the commercially available capsule formulations contain the drug in amorphous form. The goal of this study was to evaluate the robustness of the innovator product and five generic formulations to crystallization following storage at stress conditions. METHODS: Products were purchased from a pharmacy and stored at 40°C/75% relative humidity (RH), open dish conditions. Crystallinity was determined using X-ray diffraction...
July 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28681332/association-of-silver-nanoparticles-and-curcumin-solid-dispersion-antimicrobial-and-antioxidant-properties
#5
Thais Francine Alves, Marco V Chaud, Denise Grotto, Angela Faustino Jozala, Raksha Pandit, Mahendra Rai, Carolina Alves Dos Santos
The last century, more precisely after 1945, was marked by major advances in the treatment of infectious diseases which promoted a decrease in mortality and morbidity. Despite these advances, currently the development of antimicrobial resistance has been growing drastically and therefore there is a pressing need to search for new compounds. Silver nanoparticles (AgNps) have been demonstrating good antimicrobial activity against different bacteria, viruses, and fungi. Curcumin (CUR) extracted from rhizomes of Curcuma longa has a variety of applications including antiinflammatory, antioxidant, and antibacterial agent...
July 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28677032/molecular-mechanism-of-polymer-assisting-supersaturation-of-poorly-water-soluble-loratadine-based-on-experimental-observations-and-molecular-dynamic-simulations
#6
Shenwu Zhang, Mengchi Sun, Yongshan Zhao, Xuyang Song, Zhonggui He, Jian Wang, Jin Sun
Polymers have been usually used to retard nucleation and crystal growth in order to maintain supersaturation, yet their roles in inhibition of nucleation and crystal growth are poorly understood. In our work, the polymer-based supersaturation performances and molecular mechanisms of poorly aqueous soluble loratadine were investigated. Two common hydrophilic polymers (hydroxylpropylmethyl cellulose acetate succinate (HPMC-AS) and poly(vinylpyrrolidone-co-vinyl-acetate) (PVP-VA)) were used. It was found that HPMC-AS was a better polymer to prevent drug molecules from aggregation and to maintain the supersaturated state in solution than PVP-VA...
July 5, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28673860/3d-printing-of-tablets-using-inkjet-with-uv-photoinitiation
#7
Elizabeth A Clark, Morgan R Alexander, Derek J Irvine, Clive J Roberts, Martin J Wallace, Sonja Sharpe, Jae Yoo, Richard J M Hague, Chris J Tuck, Ricky D Wildman
Additive manufacturing (AM) offers significant potential benefits in the field of drug delivery and pharmaceutical/medical device manufacture. Of AM processes, 3D inkjet printing enables precise deposition of a formulation, whilst offering the potential for significant scale up or scale out as a manufacturing platform. This work hypothesizes that suitable solvent based ink formulations can be developed that allow the production of solid dosage forms that meet the standards required for pharmaceutical tablets, whilst offering a platform for flexible and personalised manufacture...
June 30, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28672810/development-and-characterization-of-an-amorphous-solid-dispersion-of-furosemide-in-the-form-of-a-sublingual-bioadhesive-film-to-enhance-bioavailability
#8
Viviana De Caro, Alessia Ajovalasit, Flavia Maria Sutera, Denise Murgia, Maria Antonietta Sabatino, Clelia Dispenza
Administered by an oral route, Furosemide (FUR), a diuretic used in several edematous states and hypertension, presents bioavailability problems, reported as a consequence of an erratic gastrointestinal absorption due to various existing polymorphic forms and low and pH-dependent solubility. A mucoadhesive sublingual fast-dissolving FUR based film has been developed and evaluated in order to optimize the bioavailability of FUR by increasing solubility and guaranteeing a good dissolution reproducibility. The Differential Scanning Calorimetry (DSC) analyses confirmed that the film prepared using the solvent casting method entrapped FUR in the amorphous state...
June 24, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28665158/dissolution-and-bioavailability-enhancement-of-alpha-asarone-by-solid-dispersions-via-oral-administration
#9
Li Deng, Yu Wang, Tao Gong, Xun Sun, Zhi-Rong Zhang
Alpha (α)-asarone (1-propenyl-2,4,5-methoxybenzol) (ARE) has been extensively used to treat chronic obstructive pulmonary diseases (COPD), bronchial asthma, pneumonia and epilepsy. Due to its poor solubility and bioavailability, ARE was clinically administered via intravenous injection. However, severe allergies were often reported due to the presence of solublizers in the injection formulation. In our study, we sought to explore the biopharmaceutical classification of ARE, elucidate the mechanisms behind ARE absorption, and to develop a viable formulation to improve the oral bioavailability of ARE...
June 30, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28663037/freeze-dried-solid-dispersion-of-exemestane-a-way-to-negate-an-aqueous-solubility-and-oral-bioavailability-problems
#10
Shamandeep Kaur, Sunil K Jena, Sanjaya K Samal, Vaishali Saini, Abhay T Sangamwar
This study was envisaged to demonstrate the potential of exemestane loaded phospholipid/sodium deoxycholate solid dispersions (EXE-PL/SDC-SDs) on the solubility and oral bioavailability of EXE. Initial studies were performed to screen the best suitable phospholipid among lysophosphatidylcholine, Phospholipon® P80H and Lipoid® E80S for solid dispersion preparation. Further studies were carried out to optimize the molar concentration of phospholipid and sodium deoxycholate (SDC) for EXE-PL/SDC-SDs preparation...
June 27, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28661679/viewing-molecular-and-interface-interactions-of-curcumin-amorphous-solid-dispersions-for-comprehending-dissolution-mechanisms
#11
Jing Li, Xin Wang, Chang Li, Na Fan, Jian Wang, Zhonggui He, Jin Sun
Tautomeric curcumin amorphous solid dispersions (Cur ASDs) formulated with various typical polymers (polyethylene glycol 6000 (PEG), polyvinylpyrrolidone K30 (PVP), Eudragit EPO (EuD), EuD/hydroxypropylmethyl cellulose E50 (HPMC), and PVP/EuD) were probed using in situ Raman imaging plus spectroscopy and molecular modeling techniques, and dissolution mechanism of Cur ASDs were revealed mainly through molecular and interfacial interactions formed between Cur and polymer. The results demonstrated that Cur of keto form existed in Cur-PEG, Cur of enol form was shown in Cur-PVP, while Cur-EuD or Cur ASDs formulated with EuD as component had Cur of keto form and enol form...
July 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28648863/two-phase-amorphous-amorphous-solid-drug-dispersion-with-enhanced-stability-solubility-and-bioavailability-resulting-from-ultrasonic-dispersion-of-an-immiscible-system
#12
Luz María Martínez, Marcelo Videa, Tania López Silva, Samuel Castro, Adolfo Caballero, Víctor J Lara-Díaz, Fabiola Castorena-Torres
Amorphization of active pharmaceutical ingredients (APIs) and the preparation of solid dispersions are strategies that can be synergized to improve the solubility of oral drugs. Immiscibility between an API and a carrier in the molten state that could be perceived as a problem in the preparation of solid dispersions, may actually introduce an advantage. In the present work, a two-phase amorphous-amorphous solid dispersion (AASD) was prepared by ultrasonicating a molten immiscible mixture of indomethacin (IND) and glucose (GLU) prior quenching...
June 22, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28647524/preparation-and-evaluation-of-bsa-based-hydrosol-nanoparticles-cross-linked-with-genipin-for-oral-administration-of-poorly-water-soluble-curcumin
#13
Narges Shahgholian, Ghadir Rajabzadeh, Bizhan Malaekeh-Nikouei
One of the most interesting functions of albumin is the ability to interact with bioactive compounds. This study describes preparation of protein-based nanoparticles (NPs) for the preparation of solid dispersion of curcumin (CN). Fabrication of hydrosol system of dispersed CN in bovine serum albumin (BSA) was approached, followed by cross-linking with glutaraldehyde (Gta). Response surface methodology (RSM) was used to investigate the influence of input factors (pH, CN content and organic phase ratio (r)), on the particle size and CN entrapment efficiency (EE)...
June 21, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28642200/enhancement-of-solubility-and-dissolution-rate-of-baicalein-wogonin-and-oroxylin-a-extracted-from-radix-scutellariae
#14
Hang Yu, Jae-Sang Chang, Sun Young Kim, Yoon G Kim, Hoo-Kyun Choi
Baicalein, wogonin, and oroxylin A are three major hydrophobic components in the extract of Radix scutellariae with wide spectrum of pharmacological applications. The purpose of this study was to enhance the solubility, dissolution rate and stability of baicalein, wogonin and oroxylin A by solid dispersion (SD) technique. SD of the extract with various polymers was prepared to select the best carrier. Solubility study, chemical stability study and dissolution study were performed to characterize the SD. The solubility of all three components, after forming solid dispersion with povidone K-30 (PVP K-30) was significantly increased in pH 6...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28630183/bioavailability-of-lumefantrine-is-significantly-enhanced-with-a-novel-formulation-approach-a-randomized-open-label-pharmacokinetic-study-in-healthy-volunteers
#15
Jay Prakash Jain, F Joel Leong, Lan Chen, Sampath Kalluri, Vishal Koradia, Daniel S Stein, Marie-Christine Wolf, Gangadhar Sunkara, Jagannath Kota
The artemether-lumefantrine combination requires food intake for optimal absorption of lumefantrine. In an attempt to enhance bioavailability of lumefantrine, new solid dispersion formulations (SDF) were developed, and the pharmacokinetics of two SDF variants were assessed in a randomized, open-label, sequential two-part study in healthy volunteers. In Part 1, relative bioavailability of the two SDF variants was compared with the conventional formulation after administration of a single dose of 480 mg under fasted conditions in three parallel cohorts...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28627470/investigation-of-itraconazole-ternary-amorphous-solid-dispersions-based-on-povidone-and-carbopol
#16
Fan Meng, Jordan Meckel, Feng Zhang
We investigate a ternary system that consists of itraconazole (ITZ) and two polymers: povidone K12 and Carbopol 907. The interactions between these two polymers and their effects on the properties of ternary ITZ amorphous solid dispersions (ASDs) are studied. These two polymers can form a water-insoluble complex in acidic aqueous media. The critical pH is determined to be 4.17. The weight percentage of Carbopol 907 in the interpolymer complex range from 59 to 70%, depending on the initial ratios between these two polymers in the starting solutions...
June 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28625814/a-multi-technique-characterization-of-the-stability-of-surfactant-containing-solid-dispersion-based-buccal-patches-prepared-by-hot-melt-injection-moulding
#17
Muqdad Alhijjaj, Peter Belton, Sheng Qi
This study investigates the stability of typically complex multi-component hydrophilic solid dispersions that could be used in a clinical application. Felodipine solid dispersions in two types of blends consisting of PEG, PEO and Tween 80 or Vit E TPGS were prepared by hot melt-injection moulding (HMIM) across a range of drug loadings and subjected to a range of storage conditions. Microscopy, thermal analysis, spectroscopy and powder X-ray diffraction were used to characterize the systems. The semi-solid surfactant TPGS showed a better solubilizing effect on the drug than the liquid surfactant Tween 80 in the fresh state and offered some degree of protection over the chemical degradation of PEG/PEO...
June 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28610878/electrospraying-of-polymer-solutions-study-of-formulation-and-process-parameters
#18
Annelies Smeets, Christian Clasen, Guy Van den Mooter
Over the past decade, electrospraying has proven to be a promising method for the preparation of amorphous solid dispersions, an established formulation strategy to improve the oral bioavailability of poorly soluble drug compounds. Due to the lack of fundamental knowledge concerning adequate single nozzle electrospraying conditions, a trial-and-error approach is currently the only option. The objective of this paper is to study/investigate the influence of the different formulation and process parameters, as well as their interplay, on the formation of a stable cone-jet mode as a prerequisite for a reproducible production of monodisperse micro- and nanoparticles...
June 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28603020/hot-melt-extrusion-hme-as-solvent-free-technique-for-a-continuous-manufacturing-of-drug-loaded-mesoporous-silica
#19
Natalja Genina, Batol Hadi, Korbinian Löbmann
The aim of the study was to explore hot melt extrusion (HME) as a solvent-free drug loading technique for preparation of stable amorphous solid dispersions (ASD) using mesoporous silica (PSi). Ibuprofen (IBU) and carvedilol (CAR) were used as poorly soluble active pharmaceutical ingredients (APIs). Due to the high friction of a API: PSi mixture below the loading limit of the API, it was necessary to add the polymer Soluplus(®) (SOL) in order to enable the extrusion process. As a result the APIs distributed between the PSi and SOL phase after HME...
June 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28602799/self-micellizing-solid-dispersions-enhance-the-properties-and-therapeutic-potential-of-fenofibrate-advantages-profiles-and-mechanisms
#20
Nian-Qiu Shi, Yong Zhang, Yan Li, Hong-Wei Lai, Xiao Xiao, Bo Feng, Xian-Rong Qi
The goal of this work was to compare fenofibrate (FEN)-containing self-micellizing solid dispersion (SmSD) and non-self-micellizing solid dispersion (NsSD) systems. Exploration of underlying mechanisms to improve FEN dissolution/solubility profiles was conducted to understand the enhanced therapeutic potential. SmSD and NsSD of FEN systems (SmSD/FEN and NsSD/FEN) were fabricated using a fuse-quench cooling method. The self-micellizing Soluplus(®) cloud point was then determined experimentally and FEN phase solubility was measured in solutions containing self-micellizing Soluplus(®) or non-self-micellizing polymers...
June 7, 2017: International Journal of Pharmaceutics
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