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https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#1
Abdelmoumin Zoghbi, Tianjiao Geng, Bo Wang
Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-β-cyclodextrin (HPβCD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HPβCD inclusion complex (KD)...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28431965/origin-of-nanodroplet-formation-upon-dissolution-of-an-amorphous-solid-dispersion-a-mechanistic-isotope-scrambling-study
#2
Anura S Indulkar, Jan E Waters, Huaping Mo, Yi Gao, Shweta A Raina, Geoff G Z Zhang, Lynne S Taylor
It has been observed that certain amorphous solid dispersions (ASDs), upon dissolution, generate drug-rich amorphous nanodroplets. These nanodroplets, present as a dispersed phase, can potentially enhance oral bioavailability of poorly soluble drugs by serving as a drug reservoir that efficiently feeds the continuous aqueous solution phase following absorption of drug. The purpose of this study was to probe the formation mechanism of the nanodroplets. The model system studied was nifedipine (NFD) formulated as an ASD with hydroxypropyl methylcellulose E5 Premium LV (HPMC-E5) or polyvinylpyrrolidone/vinyl acetate (PVPVA)...
April 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28425323/enhanced-solubility-of-piperine-using-hydrophilic-carrier-based-potent-solid-dispersion-systems
#3
Thenmozhi Kathavarayan, Young Je Yoo
CONTEXT: Piperine alkaloid, an important constituent of black pepper exhibits numerous therapeutic properties whereas its usage as a drug is limited due to its poor solubility in aqueous medium, which leads to poor bioavailability. OBJECTIVE: Herein a new method has been developed to improve the solubility of this drug based on the development of solid dispersions with improved dissolution rate using hydrophilic carriers such as sorbitol (Sor), polyethylene glycol (PEG) and polyvinyl pyrrolidone K30 (PVP) by solvent method...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28425305/development-of-a-soluplus%C3%A2-budesonide-freeze-dried-powder-for-nasal-drug-delivery
#4
Michele Pozzoli, Daniela Traini, Paul M Young, Maria B Sukkar, Fabio Sonvico
OBJECTIVE: The aim of this work was to develop an amorphous solid dispersions/solutions (ASD) of a poorly soluble drug, Budesonide (BUD) with a novel polymer Soluplus(®) (BASF, Germany) using a freeze-drying technique, in order to improve dissolution and absorption through the nasal route. SIGNIFICANCE: The small volume of fluid present in the nasal cavity limits the absorption of a poorly soluble drug. Budesonide is a corticosteroid, practically insoluble, and normally administered as a suspension-based nasal spray...
April 20, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28415461/a-new-bioavailability-enhancement-strategy-of-curcumin-via-self-assembly-nano-complexation-of-curcumin-and-bovine-serum-albumin
#5
Hong Yu, Minh-Hiep Nguyen, Wean Sin Cheow, Kunn Hadinoto
Amorphous drug nanoparticles have recently emerged as a superior bioavailability enhancement strategy for poorly soluble drugs in comparison to the conventional microscale amorphous solid dispersions. In particular, amorphous drug nanoparticle complex (or nanoplex) represents an attractive bioavailability enhancement strategy of curcumin (CUR) - a medicinal herb known for its wide-ranging therapeutic activities - attributed to the high payload, cost-effective preparation, and supersaturation generation of the nanoplex...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28414137/novel-dabigatran-etexilate-hemisuccinate-loaded-polycap-physicochemical-characterisation-and-in-vivo-evaluation-in-beagle-dogs
#6
Jung Hyun Cho, Jin Cheul Kim, Hyung-Seo Kim, Dong Shik Kim, Kyeong Soo Kim, Yong Il Kim, Chul Soon Yong, Jong Oh Kim, Yu Seok Youn, Kyung Taek Oh, Jong Soo Woo, Han-Gon Choi
The purpose of this study was to develop a novel dabigatran etexilate hemisuccinate (DEH) salt-loaded polycap with bioequivalence to the dabigatran etexilate mesylate (DEM)-loaded commercial product. DEH prepared with dabigatran etexilate base (DE) and succinic acid was less hygroscopic but less soluble than DEM. Numerous micronized DEHs and DEH-loaded solid dispersions were prepared employing the spiral jet-milling and spray-drying techniques, respectively. Among the formulations prepared, a micronized DEH prepared with the injection air at 1...
April 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28414135/gastrointestinal-behavior-of-itraconazole-in-humans-part-1-supersaturation-from-a-solid-dispersion-and-a-cyclodextrin-based-solution
#7
Joachim Brouwers, Sophie Geboers, Raf Mols, Jan Tack, Patrick Augustijns
This study evaluated the fasted state gastrointestinal behavior of the lipophilic drug itraconazole, orally administered to healthy volunteers as either a solid dispersion (Sporanox(®) capsules) or a cyclodextrin-based solution (Sporanox(®) solution). Following intake of the drug products, gastric and duodenal fluids were aspirated and analyzed for itraconazole concentration, total content and solubilizing capacity. Release of itraconazole from the solid dispersion generated high and metastable supersaturated levels in the stomach, but the dissolved fraction in the duodenum remained extremely low (median 2...
April 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28412483/effect-of-micro-environment-modification-and-polymer-type-on-the-in-vitro-dissolution-behavior-and-in-vivo-performance-of-amorphous-solid-dispersions
#8
Weiwei Sun, Baoliang Pan
This study investigates the effects of micro-environment modification and polymer type on the in-vitro dissolution behavior and in-vivo performance of micro-environment pH modifying solid dispersions (pHM-SD) for the poorly water-soluble model drug Toltrazuril (TOL). Various pHM-SDs were prepared using Ca(OH)2 as a pH-modifier in hydrophilic polymers, including polyethylene glycol 6000 (PEG6000), polyvinylpyrrolidone k30 (PVPk30) and hydroxypropyl methylcellulose (HPMC). Based on the results of physicochemical characterizations and in-vitro dissolution testing, the representative ternary (Ca(OH)2:TOL:PEG6000/HPMC/PVPk30=1:8:24, w/w/w) and binary (TOL:PVPk30=1:3, w/w) solid dispersions were selected and optimized to perform in-vivo pharmacokinetic study...
April 13, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412224/mechanism-based-selection-of-stabilization-strategy-for-amorphous-formulations-insights-into-crystallization-pathways
#9
Khadijah Edueng, Denny Mahlin, Per Larsson, Christel A S Bergström
We developed a step-by-step experimental protocol using differential scanning calorimetry (DSC), dynamic vapour sorption (DVS), polarized light microscopy (PLM) and a small-scale dissolution apparatus (μDISS Profiler) to investigate the mechanism (solid-to-solid or solution-mediated) by which crystallization of amorphous drugs occurs upon dissolution. This protocol then guided how to stabilize the amorphous formulation. Indapamide, metolazone, glibenclamide and glipizide were selected as model drugs and HPMC (Pharmacoat 606) and PVP (K30) as stabilizing polymers...
April 12, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28397829/local-structure-of-ion-pair-interaction-in-lapatinib-amorphous-dispersions-characterized-by-synchrotron-x-ray-diffraction-and-pair-distribution-function-analysis
#10
Gabriel L B de Araujo, Chris J Benmore, Stephen R Byrn
For many years, the idea of analyzing atom-atom contacts in amorphous drug-polymer systems has been of major interest, because this method has always had the potential to differentiate between amorphous systems with domains and amorphous systems which are molecular mixtures. In this study, local structure of ionic and noninonic interactions were studied by High-Energy X-ray Diffraction and Pair Distribution Function (PDF) analysis in amorphous solid dispersions of lapatinib in hypromellose phthalate (HPMCP) and hypromellose (HPMC-E3)...
April 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28394617/understanding-the-impact-of-water-on-the-miscibility-and-microstructure-of-amorphous-solid-dispersions-an-afm-lcr-and-tem-edx-study
#11
Na Li, Christopher J Gilpin, Lynne S Taylor
Miscibility is critical for amorphous solid dispersions (ASDs). Phase-separated ASDs are more prone to crystallization, and thus can lose their solubility advantage leading to product failure. Additionally, dissolution performance can be diminished as a result of phase separation in the ASD matrix. Water is known to induce phase separation during storage for some ASDs. However, the impact of water introduced during preparation has not been as thoroughly investigated to date. The purpose of this study was to develop a mechanistic understanding of the effect of water on the phase behavior and microstructure of ASDs...
April 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28389363/effects-of-wet-granulation-process-parameters-on-the-dissolution-and-physical-stability-of-a-solid-dispersion
#12
Ryo Kinoshita, Tomoaki Ohta, Koji Shiraki, Kenjirou Higashi, Kunikazu Moribe
This study investigated how the process parameters of wet-granulation affect the properties of solid dispersions (SDs), such as dissolution and physical stability. SDs of nilvadipine (NIL) and hypromellose prepared by spray-drying were wet-granulated and dried under various conditions. The NIL concentration at 4h and area under the curve from dissolution tests were taken to indicate dissolution. Then, the NIL crystallinity calculated from powder X-ray diffraction patterns of SD granules stored at 60°C for 3 months was evaluated to indicate physical stability...
April 5, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28389266/the-application-of-modeling-and-prediction-to-the-formation-and-stability-of-amorphous-solid-dispersions
#13
REVIEW
Kevin DeBoyace, Peter Wildfong
Amorphous solid dispersion (ASD) formulation development is frequently difficult owing to the inherent physical instability of the amorphous form, and limited understanding of the physical and chemical interactions that translate to initial dispersion formation and long-term physical stability. Formulation development for ASDs has been historically accomplished through trial and error or experience with extant systems, however, rational selection of appropriate excipients is preferred to reduce time to market and decrease costs associated with development...
April 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28375620/self-association-of-rafoxanide-in-aqueous-media-and-its-application-in-preparing-amorphous-solid-dispersions
#14
Fan Meng, Tongzhou Liu, Elizabeth Schneider, Shehab Alzobaidi, Marco Gil, Feng Zhang
Our primary objective is to characterize the self-association of rafoxanide in alkaline media. The second objective is to illustrate the feasibility of using rafoxanide micellar solution as the feed solution to prepare amorphous solid dispersion via spray drying. Rafoxanide is a poorly water-soluble drug. It is a weak acid, and its poor aqueous solubility is due to its hydrophobicity. The surface-active property of rafoxanide has not been previously reported. It was discovered that the addition of a small percentage of organic solvents is required to elevate the solubility of rafoxanide above the critical micelle concentration to allow for the formation of micelles...
April 4, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28375119/physical-characterization-and-dissolution-performance-assessment-of-etravirine-solid-dispersions-prepared-by-spray-drying-process
#15
Pavan Kommavarapu, Arthanareeswari Maruthapillai, Kamaraj Palanisamy, Ravi Teja Koya
The aim of the current exertion was to prepare Solid Dispersion of Etravirine by Spray drying technique to enhance aqueous solubility and dissolution rate. Solid dispersions (SD) of Etravirine were prepared using Copovidone and Povidone-Copovidone in dichloromethane and physical properties were characterized by Scanning electron microscopy (SEM), X-Ray diffractometry (PXRD), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC). SD's were evaluated for equilibrium solubility and in vitro drug release profile by dissolution testing...
November 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28363028/spectroscopic-investigation-of-the-formation-and-disruption-of-hydrogen-bonds-in-pharmaceutical-semicrystalline-dispersions
#16
Tu Van Duong, Gunter Reekmans, Akkaladevi Venkatesham, Arthur Van Aerschot, Peter Adriaensens, Jan Van Humbeeck, Guy Van den Mooter
We recently found that indomethacin (IMC) can effectively act as a powerful crystallization inhibitor for polyethylene glycol 6000 (PEG) despite the fact that the absence of interactions between the drug and the carrier in the solid state was reported in the literature. However, in the present study, we investigate the possibility of drug-carrier interactions in the liquid state to explain the polymer crystallization inhibition effect of IMC. We also aim to discover other potential PEG crystallization inhibitors...
April 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28359810/an-approach-for-chemical-stability-during-melt-extrusion-of-a-drug-substance-with-a-high-melting-point
#17
Abbe Haser, Siyuan Huang, Tony Listro, David White, Feng Zhang
Poorly water-soluble drug substances that exhibit high melting points are difficult to process by melt extrusion due to chemical instability at high temperatures required for processing. The purpose of this study was to extrude meloxicam (melting point 255°C) by optimizing processing parameters and formulation composition. Five extrusion studies were performed: 1) design space, 2) impact of moisture, 3) impact of melt residence time, 4) specific energy optimization, and 5) altered microenvironment pH. Powder X-ray diffraction and polarized light microscopy were used to confirm amorphous conversion...
March 28, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28344498/investigation-of-the-in-vitro-performance-difference-of-drug-soluplus%C3%A2-and-drug-peg-6000-dispersions-when-prepared-using-spray-drying-or-lyophilization
#18
Mohammad A Altamimi, Steven H Neau
PURPOSE: To evaluate the physicochemical and in vitro characteristics of solid dispersions using BCS II model drugs with Soluplus® and one of its component homopolymers, PEG 6000. METHODS: Nifedipine (NIF) and sulfamethoxazole (SMX) of 99.3% and 99.5% purity, respectively, were selected as BCS II model drugs, such that an improved dissolution rate and concentration in the gastrointestinal tract should increase oral bioavailability. Soluplus® is an amorphous, tri-block, graft co-polymer with polyvinyl caprolactam, polyvinyl acetate, and polyethylene glycol (PCL:PVAc:PEG6000) in the ratio 57:30:13...
March 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28343348/process-analytical-techniques-for-hot-melt-extrusion-and-their-application-to-amorphous-solid-dispersions
#19
REVIEW
Patrick Hitzer, Tim Bäuerle, Tobias Drieschner, Edwin Ostertag, Katharina Paulsen, Holger van Lishaut, Günter Lorenz, Karsten Rebner
Newly developed active pharmaceutical ingredients (APIs) are often poorly soluble in water. As a result the bioavailability of the API in the human body is reduced. One approach to overcome this restriction is the formulation of amorphous solid dispersions (ASDs), e.g., by hot-melt extrusion (HME). Thus, the poorly soluble crystalline form of the API is transferred into a more soluble amorphous form. To reach this aim in HME, the APIs are embedded in a polymer matrix. The resulting amorphous solid dispersions may contain small amounts of residual crystallinity and have the tendency to recrystallize...
March 25, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28342789/enhanced-gastric-stability-of-esomeprazole-by-molecular-interaction-and-modulation-of-microenvironmental-ph-with-alkalizers-in-solid-dispersion
#20
Hien Van Nguyen, Namhyun Baek, Beom-Jin Lee
Due to the instability of esomeprazole magnesium dihydrate (EPM), a proton pump inhibitor, in gastric fluid, enteric-coated dosage form is commonly used for therapeutic application. In this study, we prepared new gastric fluid resistant solid dispersions (SDs) containing alkalizers. Then, new mechanistic evidence regarding the effects of pharmaceutical alkalizers on the aqueous stability of EPM in simulated gastric fluid was investigated. The alkalizer-loaded SD were prepared by dissolving or dispersing EPM, hydroxypropyl methylcellulose (HPMC) 6 cps, and an alkalizer, in ethanol 50% (v/v) followed by spray drying...
March 23, 2017: International Journal of Pharmaceutics
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