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https://www.readbyqxmd.com/read/28531833/development-of-an-in-vivo-relevant-drug-product-performance-method-for-an-amorphous-solid-dispersion
#1
Brian W Pack, Yelizaveta Babayan, Mark A Schrad, Paul A Stroud, David C Sperry, Kevin C White, Aktham Aburub
The purpose of this work was to develop a meaningful in vitro dissolution method for evacetrapib spray-dried dispersion (SDD) tablets that is discriminating for crystalline drug substance (DS) content. Justification of the method conditions included evaluation of dissolution media, rotation speed, surfactant selection and level of surfactant to achieve sink conditions. Discrimination was illustrated by testing SDD tablets spiked with 10%, 20%, and 30% crystalline DS. The results demonstrated a 13%, 22% and 32% drop in the dissolution end point, respectively, as compared to unspiked SDD tablets...
May 17, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28523384/the-need-for-restructuring-the-disordered-science-of-amorphous-drug-formulations
#2
REVIEW
Khadijah Edueng, Denny Mahlin, Christel A S Bergström
The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago...
May 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28521994/double-coated-enrofloxacin-microparticles-with-chitosan-and-alginate-preparation-characterization-and-taste-masking-effect-study
#3
Mengxi Liu, Daiping Yin, Hualin Fu, Fengying Deng, Guangneng Peng, Gang Shu, Zhixiang Yuan, Fei Shi, Juchun Lin, Ling Zhao, Lizi Yin, Guoqing Fan
Enrofloxacin (ENRO) is widely used as an antimicrobial drug for treatment of uncomplicated and complicated infections in veterinary medicine. Its bitter taste limits its clinical applications in veterinary. To mask the bitter taste of this drug, double-coated taste-masking microparticles of ENRO (DTME) were prepared through stearic acid solid dispersion and chitosan-alginate microparticle coating technologies. The taste-masking effect was evaluated by pig feeding experiment. Results showed that DTME exhibited a spherical-like shape (170490μm)...
August 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28502181/rapid-nano-gram-scale-screening-method-of-micro-arrays-to-evaluate-drug-polymer-blends-using-high-throughput-printing-technology
#4
Vincenzo Taresco, Iria Louzao, David Scurr, Jonathan Booth, Kevin Treacher, James McCabe, Eleanor Turpin, Charles A Laughton, Cameron Alexander, Jonathan C Burley, Martin C Garnett
A miniaturized, high-throughput assay was optimized to screen polymer-drug solid dispersions using a 2-D Ink-jet printer. By simply printing nanoliter amounts of polymer and drug solutions onto an inert surface, drug:polymer micro-dots of tunable composition were produced in an easily-addressable micro-array format. The amount of material printed for each dried spot ranged from 25 ng to 650 ng. These arrays were used to assess the stability of drug:polymer dispersions with respect to recrystallization, using polarized light microscopy...
May 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28489944/studying-the-crystallization-of-various-polymorphic-forms-of-nifedipine-from-binary-mixtures-with-the-use-of-different-experimental-techniques
#5
O Madejczyk, E Kaminska, M Tarnacka, M Dulski, K Jurkiewicz, K Kaminski, M Paluch
In this paper the crystal growth of nifedipine from pure system and from binary mixtures composed of active substance (API) and two acetylated disaccharides, maltose and sucrose (NIF-acMAL, NIF-acSUC, 5:1 weight ratio), was investigated. Optical snapshots supported by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) measurements showed that mainly β and α forms of nifedipine grow up in all investigated samples. They also revealed that the morphology of growing crystals strongly depends on the presence of modified carbohydrates and temperature conditions...
May 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28460985/phase-behavior-structure-and-rheology-of-candelilla-wax-fully-hydrogenated-soybean-oil-mixtures-with-and-without-vegetable-oil
#6
N O Ramírez-Gómez, N C Acevedo, J F Toro-Vázquez, J J Ornelas-Paz, E Dibildox-Alvarado, J D Pérez-Martínez
Vegetable oil organogelation is one of the most promising strategies to eliminate trans fatty acids in plastic fats. Organogels prepared with edible wax are stable at refrigerator and room temperature. Some functional properties (i.e., texture) of wax organogels can be improved by adding saturated triacylglycerols. Mixtures of fully hydrogenated soybean oil (FH) and candelilla wax (CW) were studied with and without the addition of high oleic safflower oil (HOSFO). Crystallization and melting behavior, X-ray diffraction, and crystalline microstructure of the mixtures were analyzed...
November 2016: Food Research International
https://www.readbyqxmd.com/read/28460615/formulation-characterization-and-in-vitro-evaluation-of-fast-dissolving-tablets-containing-gliclazide-hydrotropic-solid-dispersions
#7
Jyotsana R Madan, Virendra J Kamate, Rajendra Awasthi, Kamal Dua
BACKGROUND: Low aqueous solubility is a major problem faced with new drug molecules. The purpose of this research was to provide a fast dissolving oral dosage form of gliclazide (GLZ) using the concept of mixed hydrotropy. METHODS: Solubility of GLZ was determined individually in sodium salicylate, nicotinamide, lactose, sodium acetate, urea, trisodium citrate and sodium benzoate. Highest solubility was obtained in 40% sodium benzoate solution. In order to decrease the individual hydrotrope amount, mixed hydrotropic agents were used...
April 26, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28458364/improved-dissolution-of-dipyridamole-with-the-combination-of-ph-modifier-and-solid-dispersion-technology
#8
Yoshiki Kojo, Saori Matsunaga, Hiroki Suzuki, Chika Taniguchi, Yohei Kawabata, Koichi Wada, Yukinori Yamauchi, Yoshiki Seto, Hideyuki Sato, Satomi Onoue
The aim of this study was to develop a pH-independent release formulation of dipyridamole (DP) by the combined use of pH-modifier technology and solid dispersion (SD) technology employing enteric polymer, Eudragit(®) S100 (Eud). Tartaric acid (TA) was selected as an appropriate pH-modifier in terms of improving the dissolution behavior of DP under neutral conditions. Upon optimization of the ratio of TA to DP, SD of DP with Eud and TA (SD-Eud/DP/TA) was prepared by a freeze-drying method. Scanning electron microscopic images revealed that DP was dispersed in the polymer in SD-Eud/DP/TA, and DP in SD-Eud/DP/TA was in an amorphous state, supported by powder X-ray diffraction and differential scanning calorimetry analyses...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28455777/insights-into-nano-and-micron-scale-phase-separation-in-amorphous-solid-dispersions-using-fluorescence-based-techniques-in-combination-with-solid-state-nuclear-magnetic-resonance-spectroscopy
#9
Hitesh S Purohit, James D Ormes, Sugandha Saboo, Yongchao Su, Matthew S Lamm, Amanda K P Mann, Lynne S Taylor
PURPOSE: Miscibility between the drug and the polymer in an amorphous solid dispersion (ASD) is considered to be one of the most important factors impacting the solid state stability and dissolution performance of the active pharmaceutical ingredient (API). The research described herein utilizes emerging fluorescence-based methodologies to probe (im)miscibility of itraconazole (ITZ)-hydroxypropyl methylcellulose (HPMC) ASDs. METHODS: The ASDs were prepared by solvent evaporation with varying evaporation rates and were characterized by steady-state fluorescence spectroscopy, confocal imaging, differential scanning calorimetry (DSC), and solid state nuclear magnetic resonance (ssNMR) spectroscopy...
April 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28450170/use-of-acidifier-and-solubilizer-in-tadalafil-solid-dispersion-to-enhance-the-in-vitro-dissolution-and-oral-bioavailability-in-rats
#10
Jin-Seok Choi, Soon-Hyung Kwon, Sang-Eun Lee, Woo Suk Jang, Jong Chan Byeon, Hyeong Mo Jeong, Jeong-Sook Park
The purpose of this study is to improve the solubility, in vitro dissolution, and oral bioavailability in rats of tadalafil (TDF) by using SD technique with a weak acid and a copolymer. TDF-SD was prepared via solvent evaporation, coupled with the incorporation of an acidifier and solubilizer. Tartaric acid enhanced the solubility of TDF over 5-fold in DW, and Soluplus(®) enhanced the solubility of TDF over 8.7-fold and 19.2-fold compared to that of TDF (pure) in DW and pH 1.2 for 1h, respectively. The optimal formulation of TDF-SD3 was composed of TDF vs Tartaric acid vs Soluplus(®) vs Aerosil=1:1:3:3...
April 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#11
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
#12
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
#13
Kathavarayan Thenmozhi, 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...
May 5, 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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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