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"solid dispersion"

Haoshi Gao, Yue Wei, Long Xi, Yuanyuan Sun, Tianhong Zhang
Bergenin (BN) is a Biopharmaceutics Classification System class IV (BCS IV) drug with poor hydrophilicity and lipophilicity and is potentially eliminated by the efflux function of P-glycoprotein (P-gp). These factors may explain its low oral bioavailability. In the present study, a BN-phospholipid complex solid dispersion (BNPC-SD) was prepared by solvent evaporation and characterized based on differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, infrared diffraction, solubility, octanol-water partition coefficient, and in vitro dissolution...
March 19, 2018: AAPS PharmSciTech
Poovizhi Ponnammal, Parijat Kanaujia, Yin Yani, Wai Kiong Ng, Reginald B H Tan
In order to improve the aqueous solubility and dissolution of Tacrolimus (TAC), amorphous solid dispersions of TAC were prepared by hot melt extrusion with three hydrophilic polymers, Polyvinylpyrrolidone vinyl acetate (PVP VA64), Soluplus® and Hydroxypropyl Cellulose (HPC), at a drug loading of 10% w / w . Molecular modeling was used to determine the miscibility of the drug with the carrier polymers by calculating the Hansen Solubility Parameters. Powder X-ray diffraction and differential scanning calorimetry (DSC) studies of powdered solid dispersions revealed the conversion of crystalline TAC to amorphous form...
March 16, 2018: Pharmaceutics
L S Usmanova, M A Ziganshin, I T Rakipov, N M Lyadov, A E Klimovitskii, T A Mukhametzyanov, A V Gerasimov
Inhalation administration is a promising alternative to the invasive drug delivery methods. The particle size required for ideal drug aerosol preparation is between 1 and 3  μ m. The application of microspherical particles of solid dispersions enhances bioavailability of poorly soluble drugs due to the solubilization. In the present work, the spray drying process of the production of microspherical particles of solid dispersions of polyvinylpyrrolidone K29-32 with model hydrophobic drug, phenacetin, was optimized using the results of DSC, PXRD, and viscometry...
2018: BioMed Research International
Daniel J Ellenberger, Dave A Miller, Sandra U Kucera, Robert O Williams
Vemurafenib is a poorly soluble, low permeability drug that has a demonstrated need for a solubility-enhanced formulation. However, conventional approaches for amorphous solid dispersion production are challenging due to the physiochemical properties of the compound. A suitable and novel method for creating an amorphous solid dispersion, known as solvent-controlled coprecipitation, was developed to make a material known as microprecipitated bulk powder (MBP). However, this approach has limitations in its processing and formulation space...
March 14, 2018: AAPS PharmSciTech
Gudrun A Fridgeirsdottir, Rob Harris, Ian Dryden, Peter M Fischer, Clive J Roberts
Solid dispersions can be a successful way to enhance the bioavailability of poorly soluble drugs. Here 60 solid dispersion formulations were produced using ten chemically diverse, neutral, poorly soluble drugs, three commonly used polymers, and two manufacturing techniques, spray drying and melt extrusion. Each formulation underwent a six-month stability study at accelerated conditions, 40 °C and 75% relative humidity (RH). Significant differences in times to crystallisation (onset of crystallisation) were observed between both the different polymers and the two processing methods...
March 13, 2018: Molecular Pharmaceutics
Hojun Song, Cheol Moon, Beom-Jin Lee, Euichaul Oh
Herein, we aimed to prepare porous granules of pravastatin and evaluate their applicability to orally disintegrating tablets (ODTs). Pravastatin solid dispersion granules (PSDGs-A) were prepared by dispersing pravastatin sodium in D-mannitol (the dispersion medium) in the presence of ammonium bicarbonate (the sublimation agent) using a spray-drying process. The PSDGs-A were round, irregularly shaped, mesoporous agglomerates with appropriate particle size, bulk density, and flowability for the tableting process...
March 9, 2018: Journal of Pharmaceutical Sciences
Aymeric Ousset, Pierre-François Chavez, Joke Meeus, Florent Robin, Martin Alexander Schubert, Pascal Somville, Kalliopi Dodou
The evaluation of drug-polymer miscibility in the early phase of drug development is essential to ensure successful amorphous solid dispersion (ASD) manufacturing. This work investigates the comparison of thermodynamic models, conventional experimental screening methods (solvent casting, quench cooling), and a novel atomization screening device based on their ability to predict drug-polymer miscibility, solid state properties ( T g value and width), and adequate polymer selection during the development of spray-dried amorphous solid dispersions (SDASDs)...
March 7, 2018: Pharmaceutics
Laura I Mosquera-Giraldo, Na Li, Venecia R Wilson, Brittany L B Nichols, Kevin J Edgar, Lynne S Taylor
During dissolution of amorphous solid dispersions (ASDs), various phase transformation can occur, which will ultimately impact the degree of supersaturation. This study employed dissolution and diffusion measurements to compare the performance of various ASD formulations based on the maximum amount of free drug in solution that was able to permeate through a cellulose based membrane. Telaprevir (TPV) was used as the model drug compound, and ASDs were prepared with different drug loadings and using four different polymers...
March 7, 2018: Molecular Pharmaceutics
Zhengtian Song, Sreya Sarkar, Andrew D Vogt, Gerald D Danzer, Casey J Smith, Ellen J Gualtieri, Garth J Simpson
The low limits of detection afforded by second harmonic generation (SHG) microscopy coupled with image analysis algorithms enabled quantitative modeling of the temperature-dependent crystallization of active pharmaceutical ingredients (APIs) within amorphous solid dispersions (ASDs). ASDs, in which an API is maintained in an amorphous state within a polymer matrix, are finding increasing use to address solubility limitations of small-molecule APIs. Extensive stability testing is typically performed for ASD characterization, the time-frame for which is often dictated by the earliest detectable onset of crystal formation...
March 5, 2018: Analytical Chemistry
Julien Maincent, Robert O Williams
The use of amorphous solid dispersions (ASD) to overcome poor drug solubility has gained interest in the pharmaceutical industry over the past decade. ASDs are challenging to formulate because they are thermodynamically unstable, and the dispersed drugs tend to recrystallize. Until now, most research on ASDs has focused on immediate-release formulations, supersaturation, and stability; only a few studies have recently reported on the manufacturing of sustained-release ASDs. Sustained-release ASDs can minimize the frequency of administration and prevent high concentrations that can lead to toxicity...
March 1, 2018: Drug Delivery and Translational Research
Carlos E S Bernardes, Catarina Garcia, Filipe Pereira, Joana Mota, Paula C Pereira, Maria-João Cebola, Catarina Pinto Reis, Isabel Correia, M Fátima M da Piedade, Manuel Eduardo Minas da Piedade, Patricia Rijo
The abietane 7α-acetoxy-6β-hydroxyroyleanone (AHR), obtained from plant extracts, is an attractive lead for drug development, given its known antimicrobial properties. Two basic requirements to establish any compound as a new drug, are the development of a convenient extraction process and the characterization of its structural and thermal properties. In this work seven different methods were tested to optimize the extraction of AHR from Plectranthus grandidentatus Gürke. Supercritical fluid extraction (SFE) proved to be the method of choice, delivering an amount of AHR (57...
March 1, 2018: Molecular Pharmaceutics
Joanna Szafraniec, Agata Antosik, Justyna Knapik-Kowalczuk, Krzysztof Chmiel, Mateusz Kurek, Karolina Gawlak, Marian Paluch, Renata Jachowicz
The anticancer drug bicalutamide was co-milled with either Macrogol6000 or Poloxamer407, and the physicochemical parameters that drive the phase transition of binary systems and influence the dissolution modification of bicalutamide were studied. Milled binary systems with reduced particle size were assessed by scanning electron microscopy and laser diffraction measurements. The results of thermal analysis supported by X-ray diffractometry confirmed the reduction of the crystallinity of bicalutamide co-milled with Macrogol6000...
February 23, 2018: International Journal of Pharmaceutics
Kristian Semjonov, Maia Salm, Tiina Lipiäinen, Karin Kogermann, Andres Lust, Ivo Laidmäe, Osmo Antikainen, Clare J Strachan, Henrik Ehlers, Jouko Yliruusi, Jyrki Heinämäki
Solid dispersions (SDs) hold a proven potential in formulating poorly water-soluble drugs. The present paper investigates the interfacial phenomena associated with the bulk powder flow, water sorption, wetting and dissolution of the SDs prepared by a modified melt and quench-cooling (QC) method. Poorly water-soluble indomethacin (IND) was QC molten with solubilizing graft copolymer (Soluplus® ) or polyol sugar alcohol (xylitol, XYL). The interfacial interactions of SDs with air/water were found to be reliant on the type (amorphous/crystalline) and amount of the carrier material used...
February 23, 2018: International Journal of Pharmaceutics
Christian Luebbert, Gabriele Sadowski
Amorphous solid dispersions (ASD) are intended to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients. However, the development of long-term stable ASDs is often limited by the unwanted crystallization of the incorporated active pharmaceutical ingredient. Robust detection and quantification of crystal formation- especially at temperatures and humidites relevant for long-term storage tests - are essential for understanding crystallization phenomena. In this work, the crystallization kinetics in spray-dried nifedipine/poly (vinyl acetate) ASDs was investigated by measuring the time-dependent water sorption behavior at constant storage conditions...
February 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Elena Piera Porcu, Massimo Cossu, Giovanna Rassu, Paolo Giunchedi, Guido Cerri, Jana Pourová, Iveta Najmanová, Thomas Migkos, Veronika Pilařová, Lucie Nováková, Přemysl Mladěnka, Elisabetta Gavini
Potential positive effects of flavonol quercetin on humans were suggested by many studies. However, it is not clear if these effects are mediated by quercetin or its metabolites. The in vivo confirmation of quercetin effects is largely hindered by its low water solubility and thus impossibility to test directly its impact. Therefore, a solid dispersion of quercetin with polyvinylpyrrolidone (PVP) was developed to prepare an injectable formulation of water-soluble quercetin. The optimized formulation provided a 20,000-fold increase in quercetin solubility...
February 20, 2018: International Journal of Pharmaceutics
Joseph W Lubach, Jonathan Hau
PURPOSE: To investigate the nature of drug-excipient interactions between indomethacin (IMC) and methacrylate copolymer Eudragit® E (EE) in the amorphous state, and evaluate the effects on formulation and stability of these amorphous systems. METHODS: Amorphous solid dispersions containing IMC and EE were spray dried with drug loadings from 20% to 90%. PXRD was used to confirm the amorphous nature of the dispersions, and DSC was used to measure glass transition temperatures (Tg )...
February 20, 2018: Pharmaceutical Research
Tanvi M Deshpande, Anisul Quadir, Sakae Obara, Stephen W Hoag
Hydroxypropyl methylcellulose acetate succinate (HPMCAS) has been widely used in amorphous solid dispersions and as an enteric coating polymer. Under aqueous coating conditions and at elevated coating temperatures, HPMCAS particles tend to aggregate and clog the spray-nozzle, hence interrupting the coating process. This research focused on how plasticizers and surfactants, excipients used for aqueous coating, affect the properties and stability of HPMCAS. This information would be useful in identifying suitable excipients for developing a stable HPMCAS aqueous enteric coating formulation...
February 16, 2018: International Journal of Pharmaceutics
Yuqi Chen, Wencong Huang, Jiali Chen, Hanning Wang, Shujuan Zhang, Subin Xiong
The aim was to explore the effects of non-polar and polar protic solvents composed of dichloromethane (DCM) and ethanol (EtOH) on the properties of felodipine (FLDP) and Soluplus in solutions, casting films and spray dried drug-rich or polymer-rich solid dispersions (SDs). Measurement of intrinsic viscosity and solubility indicated that FLDP and Soluplus were miscible. EtOH-DCM ranging from 20:80 to 50:50 induced the strongest molecular interactions for FLDP-Soluplus-solvents systems. Accordingly, the casting films and spray dried powders of FLDP and Soluplus were prepared using pure EtOH or DCM and their mixtures as solvents...
February 15, 2018: Journal of Pharmaceutical Sciences
Fuzheng Ren, Hanjing Sun, Lin Cui, Yike Si, Ning Chen, Guobin Ren, Qiufang Jing
Drugs in amorphous solid dispersions (ASDs) are highly dispersed in hydrophilic polymeric carriers, which also help to restrain recrystallization and stabilize the ASDs. In this study, microscopic observation after antisolvent recrystallization was developed as a rapid screening method to select appropriate polymers for the initial design filgotinib (FTN) ASDs. Using solvent evaporation, FTN ASDs with the polymers were prepared, and accelerated experimentation validated this screening method. Fourier-transform infrared spectroscopy, Raman scattering, and nuclear magnetic resonance revealed hydrogen-bonding formation in the drug-polymer binary system, which was critical for ASDs stabilization...
February 15, 2018: Journal of Pharmaceutical Sciences
Leslie Raphael de Moura Ferraz, Alinne Élida Gonçalves Alves, Débora Dolores Souza da Silva Nascimento, Isabela Araújo E Amariz, Aline Silva Ferreira, Salvana Priscylla Manso Costa, Larissa Araújo Rolim, Ádley Antonini Neves de Lima, Pedro José Rolim Neto
Caused by Trypanosoma cruzi, Chagas disease is responsible for public health problems greater in magnitude than those attributed to malaria, schistosomiasis, or leishmaniasis. A factor in the socioeconomic development of poor countries, Chagas disease can cause death due to a high parasitic burden during its acute phase due and irreversible damage in organs such as the heart, esophagus, and colon during its chronic phase, even when the number of parasites is minimal. For treating Chagas disease, benznidazole (BNZ) remains the drug of choice and, in Latin America, the only drug on the market for treating the disease...
February 13, 2018: Acta Tropica
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