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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
https://www.readbyqxmd.com/read/28601524/rifampin-stability-and-solution-concentration-enhancement-through-amorphous-solid-dispersion-in-cellulose-%C3%AF-carboxyalkanoate-matrices
#7
Hale Çiğdem Arca, Laura I Mosquera-Giraldo, Junia M Pereira, Nammalwar Sriranganathan, Lynne S Taylor, Kevin J Edgar
Tuberculosis (TB) is a deadly infectious disease; approximately 2 billion people are currently latently infected with the causative agent Mycobacterium tuberculosis. Approximately 8 million new active cases and 2 million deaths due to TB are recorded annually(1). Rifampin (Rif) is a vital first line TB treatment drug. Its effectiveness is hampered by the high dose required (600 mg 1x/day) and by its moderate, variable bioavailability. These issues can be explained by Rif instability at gastric pH, limited solubility at neutral pH, polymorphism, and stimulation of its own metabolism...
June 7, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28595530/encapsulation-of-solid-dispersion-in-solid-lipid-particles-for-dissolution-enhancement-of-poorly-water-soluble-drug
#8
Khanh Thi My Tran, Toi Van Vo, Phuong Ha-Lien Tran, Beom-Jin Lee, Wei Duan, Thao Truong-Dinh Tran
BACKGROUND: The aim of this research was to engineer solid dispersion lipid particles (SD-SLs) in which a solid dispersion (SD) was encapsulated to form the core of solid lipid particles (SLs), thereby achieving an efficient enhancement in the dissolution of a poorly water-soluble drug. METHODS: Ultrasonication was introduced into the process to obtain micro/nanoscale SLs. The mechanism of dissolution enhancement was investigated by analysing the crystalline structure, molecular interactions, and particle size of the formulations...
June 5, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28591516/impact-of-drug-rich-colloids-of-itraconazole-and-hpmcas-on-membrane-flux-in-vitro-and-oral-bioavailability-in-rats
#9
Aaron M Stewart, Michael E Grass, Timothy J Brodeur, Aaron K Goodwin, Michael M Morgen, Dwayne T Friesen, David T Vodak
Improving the oral absorption of compounds with low aqueous solubility is a common challenge that often requires an enabling technology. Frequently, oral absorption can be improved by formulating the compound as an amorphous solid dispersion (ASD). Upon dissolution, an ASD can reach a higher concentration of unbound drug than the crystalline form, and often generates a large number of sub-micron, rapidly-dissolving drug-rich colloids. These drug-rich colloids have the potential to decrease the diffusional resistance across the unstirred water layer of the intestinal tract (UWL) by acting as rapidly-diffusing shuttles for unbound drug...
June 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28590055/enhanced-dissolution-and-bioavailability-of-nateglinide-by-microenvironmental-ph-regulated-ternary-solid-dispersion-in-vitro-and-in-vivo-evaluation
#10
Sarika Wairkar, Ram Gaud, Namdeo Jadhav
OBJECTIVES: Nateglinide, an Antidiabetic drug (BCS II), shows pH-dependent solubility and variable bioavailability. The purpose of study was to increase dissolution and bioavailability of Nateglinide by development of its microenvironmental pH-regulated ternary solid dispersion (MeSD). METHODS: MeSD formulation of Nateglinide, poloxamer-188 and Na2 CO3 was prepared by melt dispersion in 1 : 2 : 0.2 w/w ratio and further characterised for solubility, In-vitro dissolution, microenvironmental pH, crystallinity/amorphism, physicochemical interactions, bioavailability in Wistar rats...
June 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28584898/factors-affecting-the-dissolution-of-indomethacin-solid-dispersions
#11
Wei Zhang, Chen-Ning Zhang, Yue He, Ban-Yan Duan, Guang-Yi Yang, Wei-Dong Ma, Yong-Hong Zhang
The aim of this study was to investigate the influence of factors such as carrier type, drug/carrier ratio, binary carriers, and preparation method on the dissolution of an insoluble drug, indomethacin (IM), under supersaturation conditions. Using a solvent evaporation (SE) method, poloxamer 188 and PVP K30 showed better dissolution among the selected carriers. Furthermore, as the ratio of carriers increased (drug/carrier ratio from 1:0.5 to 1:2), the dissolution rate increased especially in almost two times poloxamer 188 solid dispersions (SDs), while the reverse results were observed for PVP K30 SDs...
June 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28583589/a-comparative-assessment-of-nanocomposites-vs-amorphous-solid-dispersions-prepared-via-nanoextrusion-for-drug-dissolution-enhancement
#12
Meng Li, Nicolas Ioannidis, Costas Gogos, Ecevit Bilgili
Nanoextrusion was used to produce extrudates of griseofulvin, a poorly water-soluble drug, with the objective of examining the impact of drug particle size and polymeric matrix type-size of the extrudates on drug dissolution enhancement. Hydroxypropyl cellulose (HPC) and Soluplus® were used to stabilize wet-milled drug suspensions and form matrices of the extrudates. The wet-milled suspensions along with additional polymer (HPC/Soluplus®) were fed to a co-rotating twin-screw extruder, which dried the suspensions and formed various extrudates...
June 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28583588/processing-thermally-labile-drugs-by-hot-melt-extrusion-the-lesson-with-gliclazide
#13
Siyuan Huang, Kevin P O'Donnell, Sophie M Delpon de Vaux, John O'Brien, John Stutzman, Robert O Williams Iii
The formation of molecularly dispersed amorphous solid dispersions by the hot-melt extrusion technique relies on the thermal and mechanical energy inputs, which can cause chemical degradation of drugs and polymeric carriers. Additionally, drug degradation may be exacerbated as drugs convert from a more stable crystalline form to a higher energy amorphous form. Therefore, it is imperative to study how drug degrades and evaluate methods to minimize drug degradation during the extrusion process. In this work, gliclazide was used as a model thermally labile drug for the degradation kinetics and process optimization studies...
June 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28579005/tadalafil-solid-dispersion-formulations-based-on-pvp-va-s-630-improving-oral-bioavailability-in-rats
#14
Jin-Seok Choi, Sang-Eun Lee, Woo Suk Jang, Jong Chan Byeon, Jeong-Sook Park
Here, solid dispersion (SD) techniques were utilized to improve the oral bioavailability of tadalafil (TDF). Poly(vinyl pyrrolidone-covinyl acetate) (PVP/VA S-630; 60% VP and 40% VA; MW 50,000) SD formulations were previously found to improve the solubility and dissolution (%) of TDF. The effect of various weak acids and bases on SD formulations was also investigated herein. PVP/VA S-630 SD formulations in combination with weak acids and bases increased the apparent solubility of TDF. After 1h, the apparent solubility of PVP/VA S-630 SD formulations with MgO, meglumine, and tartaric acid were significantly higher by 387...
June 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28577997/interfacial-interaction-track-of-amorphous-solid-dispersions-established-by-water-soluble-polymer-and-indometacin
#15
Jing Li, Na Fan, Xin Wang, Chang Li, Mengchi Sun, Jian Wang, Qiang Fu, Zhonggui He
The present work studied interfacial interactions of amorphous solid dispersions matrix of indometacin (IMC) that established using PVP K30 (PVP) and PEG 6000 (PEG) by focusing on their interaction forces and wetting process. Infrared spectroscopy (IR), raman spectroscopy, X-ray photoelectron spectra and contact angle instrument were used throughout the study. Hydrogen bond energy formed between PEG and IMC were stronger than that of PVP and IMC evidenced by molecular modeling measurement. The blue shift of raman spectroscopy confirmed that hydrogen bonding forces were formed between IMC and two polymers...
June 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28570079/amorphous-polymeric-drug-salts-as-ionic-solid-dispersion-forms-of-ciprofloxacin
#16
Hanah Mesallati, Anita Umerska, Krzysztof J Paluch, Lidia Tajber
Ciprofloxacin (CIP) is a poorly soluble drug that also displays poor permeability. Attempts to improve the solubility of this drug to date have largely focused on the formation of crystalline salts and metal complexes. The aim of this study was to prepare amorphous solid dispersions (ASDs) by ball milling CIP with various polymers. Following examination of their solid state characteristics and physical stability, the solubility advantage of these ASDs was studied, and their permeability was investigated via parallel artificial membrane permeability assay (PAMPA)...
June 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28560506/biomimetic-dissolution-a-tool-to-predict-amorphous-solid-dispersion-performance
#17
Michael M Puppolo, Justin R Hughey, Traciann Dillon, David Storey, Susan Jansen-Varnum
The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane...
May 30, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28559844/impact-of-dendrimers-on-solubility-of-hydrophobic-drug-molecules
#18
REVIEW
Sonam Choudhary, Lokesh Gupta, Sarita Rani, Kaushalkumar Dave, Umesh Gupta
Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28552065/micelles-as-delivery-system-for-cancer-treatment
#19
Dilek Keskin, Ayşen Tezcaner
Micelles are nanoparticles formed by the self-assembly of amphiphilic block copolymers in certain solvents above concentrations called critical micelle concentration (CMC). Micelles are used in different fields like food, cosmetics, medicine, etc. These nanosized delivery systems are under spotlight in the recent years with new achievements in terms of their in vivo stability, ability to protect entrapped drug, release kinetics, ease of cellular penetration and thereby increased therapeutic efficacy. Drug loaded micelles can be prepared by dialysis, oil-in-water method, solid dispersion, freezing, spray drying, etc...
May 25, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28551427/amorphous-solid-dispersion-of-meloxicam-enhanced-oral-absorption-in-rats-with-impaired-gastric-motility
#20
Hiroki Suzuki, Keisuke Yakushiji, Saori Matsunaga, Yukinori Yamauchi, Yoshiki Seto, Hideyuki Sato, Satomi Onoue
Meloxicam (MEL) shows a slow onset of action in severe pain patients due to delayed gastric motility. This study aimed to develop an amorphous solid dispersion (ASD) of MEL to achieve rapid oral absorption in severe pain patients. ASD formulations of MEL with hydroxypropylmethylcellulose (ASD-MEL/HPMC) and polyacrylates and polymethacrylates (ASD-MEL/EUD) were prepared and physicochemically characterized. Oral absorption behavior of MEL samples was also clarified in both normal and propantheline (PPT)-pretreated rats with impaired gastric motility...
May 24, 2017: Journal of Pharmaceutical Sciences
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