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https://www.readbyqxmd.com/read/27919702/design-of-pvp-va-s-630-based-tadalafil-solid-dispersion-to-enhance-the-dissolution-rate
#1
Jin-Seok Choi, Jeong-Sook Park
Tadalafil (TDF) is a Biopharmaceutics Classification System (BCS) class II drug; the efficacy thereof is critically limited by inherent poor water solubility. Solid dispersion (SD) techniques are widely used to improve the bioavailability of drugs that are poorly water-soluble. Herein, we used an SD technique to improve the solubility and in vitro dissolution rate of TDF; a solvent evaporation method was applied involving the use of hydrophilic carriers (PVP/VA S-630) and assistants (malic acid or meglumine)...
December 2, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27916700/elucidation-and-visualization-of-solid-state-transformation-and-mixing-in-a-pharmaceutical-mini-hot-melt-extrusion-process-using-in-line-raman-spectroscopy
#2
Jeroen Van Renterghem, Ashish Kumar, Chris Vervaet, Jean Paul Remon, Ingmar Nopens, Yvan Vander Heyden, Thomas De Beer
Mixing of raw materials (drug+polymer) in the investigated mini pharma melt extruder is achieved by using co-rotating conical twin screws and an internal recirculation channel. In-line Raman spectroscopy was implemented in the barrels, allowing monitoring of the melt during processing. The aim of this study was twofold: to investigate (I) the influence of key process parameters (screw speed - barrel temperature) upon the product solid-state transformation during processing of a sustained release formulation in recirculation mode; (II) the influence of process parameters (screw speed - barrel temperature - recirculation time) upon mixing of a crystalline drug (tracer) in an amorphous polymer carrier by means of residence time distribution (RTD) measurements...
December 1, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27915573/solid-dispersions-enhance-solubility-dissolution-and-permeability-of-thalidomide
#3
Silvana A Barea, Cristiane B Mattos, Ariadne C C Cruz, Vitor C Chaves, Rafael N Pereira, Claudia M O Simões, Jadel M Kratz, Letícia S Koester
Thalidomide (THD) is a BCS class II drug with renewed and growing therapeutic applicability. Along with the low aqueous solubility, additional poor biopharmaceutical properties of the drug, i.e. chemical instability, high crystallinity and polymorphism, lead to a slow and variable oral absorption. In this view, we developed solid dispersions (SDs) containing THD dispersed in different self-emulsifying carriers aiming at an enhanced absorption profile for the drug. THD was dispersed in lauroyl macrogol-32 glycerides (Gelucire® 44/14) and α-tocopherol polyethylene glycol succinate (Kolliphor® TPGS),in the presence or absence of the precipitation inhibitor polyvinylpyrrolidone K30 (PVP K30), by means of the solvent method...
December 5, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27903457/glass-forming-ability-of-compounds-in-marketed-amorphous-drug-products
#4
Nicole Wyttenbach, Martin Kuentz
This note is about the glass-forming ability (GFA) of drugs marketed as amorphous solid dispersions or as pure amorphous compounds. A thermoanalytical method was complemented with an in silico study, which made use of molecular properties that were identified earlier as being relevant for GFA. Thus, molar volume together with effective numbers of torsional bonds and hydrogen bonding were used to map drugs that are as amorphous products on the market either as solid dispersion of without co-processed carrier as amorphous drug in a solid dosage form...
November 27, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27894988/experimental-observations-and-dissipative-particle-dynamic-simulations-on-microstructures-of-ph-sensitive-polymer-containing-amorphous-solid-dispersions
#5
Mengchi Sun, Bingyu Li, Yanchun Li, Yangdan Liu, Qi Liu, Hailun Jiang, Zhonggui He, Yongshan Zhao, Jin Sun
Amorphous solid dispersion (ASD) technique is an effective strategy to increase the dissolution rate of poorly soluble drugs. However, it is inherently unstable, and the molecular basis for achieving kinetic stability is not well understood. In this study, lacidipine-Eudragit_E_100 solid dispersions with 20% drug loading were prepared using the solvent evaporation. Dissolution tested showed that ASD had a significantly high rate, which was dependent on the pH of the medium. Based on time-dependent measurement of supersaturation and particle size, inhibition of crystal growth by Eudragit_E_100 differed at pH 1...
November 25, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27890595/the-formation-and-physical-stability-of-two-phase-solid-dispersion-systems-of-indomethacin-in-supercooled-molten-mixtures-with-different-matrix-formers
#6
Kristian Semjonov, Karin Kogermann, Ivo Laidmäe, Osmo Antikainen, Clare J Strachan, Henrik Ehlers, Jouko Yliruusi, Jyrki Heinämäki
Amorphous solid dispersions (SDs) are a promising approach to improve the dissolution rate of and oral bioavailability of poorly water-soluble drugs. In some cases multi-phase, instead of single-phase, SD systems with amorphous drug are obtained. While it is widely assumed that one-phase amorphous systems are desirable, two-phase systems may still potentially exhibit enhanced stability and dissolution advantages over undispersed systems. The objective of the present study was to understand the solid-state properties of two-phase SDs with amorphous drug and their relation to physical stability...
November 23, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27885872/improvement-of-solubility-dissolution-and-stability-profile-of-artemether-solid-dispersions-and-self-emulsified-solid-dispersions-by-solvent-evaporation-method
#7
Muhammad Tayyab Ansari, Muhammad Sohail Arshad, Altaf Hussain, Zeeshan Ahmad
The purpose of this study was to investigate changes in the water solubility of artemether; a poorly soluble drug used for the treatment of malaria. Different solid dispersions (SD) of artemether were prepared using; artemether and polyethyleneglycol 6000 at ratio 12:88 (Group 1), self-emulsified solid dispersions (SESD) containing artemether, polyethylene glycol 6000, cremophor-A-25, olive oil, hydroxypropylmethylcellulose and transcutol in the ratio 12:75:5:4:2:2, respectively (Group 2). SESD's were also prepared by substituting cremophor-A-25 in Group 2 with poloxamer 188 (noted as Group 3)...
November 25, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27882815/approaches-to-developing-fast-release-pellets-via-wet-extrusion-spheronization
#8
Yu Xia, Chun-Yang Shi, Jian-Guo Fang, Wen-Qing Wang
Microcrystalline cellulose (MCC) is widely regarded as the excellent choice to manufacture pellets via wet extrusion-spheronisation (ES) process due to its excellent water uptake capability, water holding capacity, desirable rheological properties, cohesiveness and plasticity etc. Nevertheless, in spite of all these advantages, limitations associated with the application of MCC also have been reported. The most prevailing limitation is prolonged or incomplete drug release profile due to the lack of disintegration as pellet contracts significantly during the drying process, especially when in combination with poorly soluble drug at a high level...
December 9, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27874293/improved-stability-of-solid-dispersions-of-manidipine-with-polyethylene-glycol-4000-copovidone-blends-application-of-ternary-phase-diagram
#9
Benchawan Chamsai, Sontaya Limmatvapirat, Srisagul Sungthongjeen, Pornsak Sriamornsak
CONTEXT: Manidipine (MDP) is generally used clinically as an antihypertensive agent; however, the bioavailability of orally administered MDP is limited very low due to their very low water solubility. OBJECTIVE: The objectives of this research were, therefore, to increase the solubility of MDP by the formation of ternary solid dispersions (tSD) with polyethylene glycol 4000 (PEG4000) and copovidone and to improve their stability. METHODS: Solid ternary phase diagram was constructed to find homogeneous solid dispersion region after melting and solidifying at low temperature with different quenching substances...
November 22, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27867277/characterization-and-bioavailability-study-of-baicalin-mesoporous-carbon-nanopowder-solid-dispersion
#10
Li Cui, E Sune, Jie Song, Jing Wang, Xiao-Bin Jia, Zhen-Hai Zhang
BACKGROUND: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. OBJECTIVE: The present study was conducted to enhance the dissolution and oral bioavailability of baicalin (BA) through a novel mesoporous carbon nanopowder (MCN) drug carrier. MATERIALS AND METHODS: Solid dispersions (SDs) of BA with MCN were prepared using a solvent evaporation method...
October 2016: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/27864786/clinical-pharmacokinetics-of-an-amorphous-solid-dispersion-tablet-of-elacridar
#11
Emilia Sawicki, Remy B Verheijen, Alwin D R Huitema, Olaf van Tellingen, Jan H M Schellens, Bastiaan Nuijen, Jos H Beijnen, Neeltje Steeghs
Elacridar is an inhibitor of the permeability glycoprotein (P-gp) and the breast cancer resistance protein (BCRP) and is a promising absorption enhancer of drugs that are substrates of these drug-efflux transporters. However, elacridar is practically insoluble in water, resulting in low bioavailability which currently limits its clinical application. We evaluated the in vitro dissolution and clinical pharmacokinetics of a novel amorphous solid dispersion (ASD) tablet containing elacridar. The dissolution from ASD tablets was compared to that from a crystalline powder mixture in a USP type II dissolution apparatus...
November 18, 2016: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/27863672/hot-melt-extruded-transdermal-films-based-on-amorphous-solid-dispersions-in-eudragit-rs-po-the-inclusion-of-hydrophilic-additives-to-develop-moisture-activated-release-systems
#12
Esra'a Albarahmieh, Sheng Qi, Duncan Q M Craig
A series of Eudragit RS PO-based hot melt extruded films were evaluated as potential transdermal systems, with particular emphasis on the inclusion of hydrophilic excipients to allow water sorption, which in turn would allow drug release on application to the skin. More specifically, sucrose, methyl cellulose, xanthan gum (Xantural(®)75), poloxamer (Pluronic(®)F127), Gelucire 44/14 were added to Eudragit RS PO and assessed in terms of physical structure (modulated temperature DSC (MTDSC), thermogravimetric analysis (TGA), powder XRD (PXRD), scanning electron microscopy(SEM)) and in vitro drug release and permeation properties...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27832954/efficient-approach-to-enhance-drug-solubility-by-particle-engineering-of-bovine-serum-albumin
#13
Mouhamad Khoder, Hamdy Abdelkader, Amr ElShaer, Ayman Karam, Mohammad Najlah, Raid G Alany
The aim of this study was to investigate the use of bovine serum albumin (BSA) as a solubility enhancer for indometacin (IND) as a model drug. IND-BSA solid dispersions were prepared by both spray drying and freeze drying techniques using IND:BSA solution (20:1 Molar Ratio (MR)) and IND:BSA suspension (100:1 MR). The solid state of IND in solid dispersions was characterised by SEM, DSC and XRD. The aqueous solubility of IND in the presence of increased amounts of BSA was evaluated. Additionally, IND dissolution and release profiles were evaluated...
November 7, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27829335/amorphous-and-crystalline-particulates-challenges-and-perspectives-in-drug-delivery
#14
Hisham Al-Obaidi, Mridul Majumder, Fiza Bari
Crystalline and amorphous dispersions have been the focus of academic and industrial research due to their potential role in formulating poorly water-soluble drugs. This review looks at the progress made starting with crystalline carriers in the form of eutectics moving towards more complex crystalline mixtures. It also covers using glassy polymers to maintain the drug as amorphous exhibiting higher energy and entropy. However, the amorphous form tends to recrystallize on storage, which limits the benefits of this approach...
November 7, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27824281/on-the-inherent-properties-of-soluplus-and-its-application-in-ibuprofen-solid-dispersions-generated-by-microwave-quench-cooling-technology
#15
Nian-Qiu Shi, Hong-Wei Lai, Yong Zhang, Bo Feng, Xiao Xiao, Hong-Mei Zhang, Zheng-Qiang Li, Xian-Rong Qi
Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, or Soluplus(®), is a relatively new copolymer and a promising carrier of amorphous solid dispersions. Knowledge on the inherent properties of Soluplus(®) (e.g. cloud points, critical micelle concentrations, and viscosity) in different conditions is relatively inadequate, and the application characteristics of Soluplus(®)-based solid dispersions made by microwave methods still need to be clarified. In the present investigation, the inherent properties of a Soluplus(®) carrier, including cloud points, critical micelle concentrations, and viscosity, were explored in different media and in altered conditions...
November 16, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27816263/non-sink-dissolution-behavior-and-solubility-limit-of-commercial-tacrolimus-amorphous-formulations
#16
Niraj S Trasi, Hitesh S Purohit, Hong Wen, Dajun D Sun, Lynne S Taylor
An increasing number of drugs with low aqueous solubility are being formulated and marketed as amorphous solid dispersions because the amorphous form can generate a higher solubility compared to the crystalline solid. The amorphous solubility of a drug can be determined experimentally using various techniques. Most studies in this area investigate the drug in its pure form and do not evaluate any effects from other formulation ingredients. In this study, we use 6 marketed amorphous oral drug products, capsules containing 5 mg of tacrolimus, and various excipients, consisting of 1 innovator product and 5 generics...
November 2, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27810562/improved-oral-absorption-profile-of-itraconazole-in-hypochlorhydria-by-self-micellizing-solid-dispersion-approach
#17
Yoshiki Kojo, Saori Matsunaga, Hiroki Suzuki, Hideyuki Sato, Yoshiki Seto, Satomi Onoue
The present study was aimed to evaluate the applicability of a self-micellizing solid dispersion (SMSD) system of itraconazole (ITZ) with the use of Soluplus(®) to achieve improved dissolution and stable oral absorption of ITZ under hypochlorhydric conditions. The SMSD of ITZ (SMSD/ITZ) was prepared by the freeze-drying method. Physicochemical properties of SMSD/ITZ were assessed in terms of morphology, crystallinity, particle size, thermal behavior, dissolution profile, and stability. The pharmacokinetic profile of SMSD/ITZ was evaluated in both normal rats and omeprazole-treated rats as a hypochlorhydric model...
October 31, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27800558/high-throughput-excipient-discovery-enables-oral-delivery-of-poorly-soluble-pharmaceuticals
#18
Jeffrey M Ting, Swapnil Tale, Anatolii A Purchel, Seamus D Jones, Lakmini Widanapathirana, Zachary P Tolstyka, Li Guo, Steven J Guillaudeu, Frank S Bates, Theresa M Reineke
Polymeric excipients are crucial ingredients in modern pills, increasing the therapeutic bioavailability, safety, stability, and accessibility of lifesaving products to combat diseases in developed and developing countries worldwide. Because many early-pipeline drugs are clinically intractable due to hydrophobicity and crystallinity, new solubilizing excipients can reposition successful and even failed compounds to more effective and inexpensive oral formulations. With assistance from high-throughput controlled polymerization and screening tools, we employed a strategic, molecular evolution approach to systematically modulate designer excipients based on the cyclic imide chemical groups of an important (yet relatively insoluble) drug phenytoin...
October 26, 2016: ACS Central Science
https://www.readbyqxmd.com/read/27790142/physical-properties-and-effect-in-a-battery-of-safety-pharmacology-models-for-three-structurally-distinct-enteric-polymers-employed-as-spray-dried-dispersion-carriers
#19
Ryan M Fryer, Mita Patel, Xiaomei Zhang, Katja S Baum-Kroker, Akalushi Muthukumarana, Brian Linehan, Yin-Chao Tseng
Establishing a wide therapeutic index (TI) for pre-clinical safety is important during lead optimization (LO) in research, prior to clinical development, although is often limited by a molecules physiochemical characteristics. Recent advances in the application of the innovative vibrating mesh spray-drying technology to prepare amorphous solid dispersions may offer an opportunity to achieve high plasma concentrations of poorly soluble NCEs to enable testing and establishment of a wide TI in safety pharmacology studies...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27776286/inventory-of-oral-anticancer-agents-pharmaceutical-formulation-aspects-with-focus-on-the-solid-dispersion-technique
#20
E Sawicki, J H M Schellens, J H Beijnen, B Nuijen
Dissolution from the pharmaceutical formulation is a prerequisite for complete and consistent absorption of any orally administered drug, including anticancer agents (oncolytics). Poor dissolution of an oncolytic can result in low oral bioavailability, high variability in blood concentrations and with that suboptimal or even failing therapy. This review discusses pharmaceutical formulation aspects and absorption pharmacokinetics of currently licensed orally administered oncolytics. In nearly half of orally dosed oncolytics poor dissolution is likely to play a major role in low and unpredictable absorption...
September 20, 2016: Cancer Treatment Reviews
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