Read by QxMD icon Read

"solid dispersion"

Ahmad Bani-Jaber, Iyad Alshawabkeh, Samaa Abdullah, Imad Hamdan, Adel Ardakani, Maha Habash
Due to its unique properties, such as biodegradability, biocompatibility, high amphiphilic property, and micelle formation, casein (CS) has been increasingly studied for drug delivery. We used CS as a drug carrier in solid dispersions (SDs) and evaluated the effect of its degradation by trypsin on drug dissolution from the dispersions. SDs of CS and mefenamic acid (MA) were prepared by physical mixing, kneading, and coprecipitation methods. In comparison to pure MA, the dispersions were evaluated for drug-protein interaction, loss of drug crystalinity, and drug morphology by differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectroscopy, and scanning electron microscopy...
October 17, 2016: AAPS PharmSciTech
Na Zhu, Jian-Chun Li, Jin-Xiu Zhu, Xiu Wang, Jin Zhang
BACKGROUND With the gradually accumulating research on pharmacological activity of wogonin, the in vitro analysis research on wogonin has become more and more popular, but there are very few reports about in vivo detection, and there are no solid dispersions (SDs) of Wogonin. The aim of this study was to explore the formation of solid dispersions (SDs) of wogonin. The reasons for the low bioavailability were studied through different routes of administration. MATERIAL AND METHODS SDs was formulated using the solvent evaporation method via polyvinylpyrrolidone K30 (PVP)...
October 16, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Katsuhiko Yamamoto, Taro Kojima, Masatoshi Karashima, Yukihiro Ikeda
To judge the developability and analyze functional mechanism of co-amorphouses, we investigated the physicochemical properties of co-amorphouses and compare the properties with the co-crystals having the same drug and counters. Co-amorphous compounds are a novel approach to improve the physicochemical properties of drugs. A co-amorphous is in an amorphous solid state allowing non-ionic interactions between drug molecules and counter molecules. The co-amorphous compounds composed of itraconazole (ITZ) with the organic carboxyl acid, fumaric acid (FA) or L-tartaric acid (TA), were prepared by mechanical grinding...
October 12, 2016: Chemical & Pharmaceutical Bulletin
Peeush Singhal, Rajneesh Dutt Kaushik, Vijay Jyoti Kumar, Anurag Verma, Pranav Gupta
In this Research, an effort has been done for the development of effervescent controlled release floating tablet (ECRFT) from solid dispersions (SDs) of diclofenac sodium (DS) for upsurge the solubility and dissolution rate. ECRFT of DS was prepared by using SDs of DS and its SDs prepared with PEG as carrier using thermal method (Simple fusion). SDs of DS were formulated in many ratio (1:1, 1:2, 1:3 and 1:4). Prepared SDs was optimized for its solubility, % drug content and % dissolution studies. Tablets were formulated by using optimized SDs products and all formulation was evaluated for various parameters...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Laura C Luciani-Giacobbe, María V Ramírez-Rigo, Yamila Garro-Linck, Gustavo A Monti, Ruben H Manzo, María E Olivera
One of the main obstacles to the successful treatment of tuberculosis is the poor and variable oral bioavailability of rifampicin (RIF), which is mainly due to its low hydrophilicity and dissolution rate. The aim of this work was to obtain a hydrophilic new material that allows a very fast dissolution rate of RIF and therefore is potentially useful in the development of oral solid dosage forms. The acid form of carboxymethylcellulose (CMC) was co-processed with RIF by solvent impregnation to obtain CMC-RIF powder, which was characterized by polarized optical microscopy, powder x-ray diffraction, DSC-TGA, hot stage microscopy, (13)C and (15)N solid-state NMR and FT-IR spectroscopy...
October 6, 2016: European Journal of Pharmaceutical Sciences
Justine Thiry, Pierre Lebrun, Chloe Vinassa, Marine Adam, Lauranne Netchacovitch, Eric Ziemons, Philippe Hubert, Fabrice Krier, Brigitte Evrard
The purpose of this work was to increase the solubility and the dissolution rate of itraconazole, which was chosen as the model drug, by obtaining an amorphous solid dispersion by hot melt extrusion. Therefore, an initial preformulation study was conducted using differential scanning calorimetry, thermogravimetric analysis and Hansen's solubility parameters in order to find polymers which would have the ability to form amorphous solid dispersions with itraconazole. Afterwards, the four polymers namely Kollidon(®) VA64, Kollidon(®) 12PF, Affinisol(®) HPMC and Soluplus(®), that met the set criteria were used in hot melt extrusion along with 25wt...
October 5, 2016: International Journal of Pharmaceutics
Camila Fabiano de Freitas, Diogo Silva Pellosi, Bianca Martins Estevão, Italo Rodrigo Calori, Tayana Mazin Tsubone, Mário José Politi, Wilker Caetano, Noboru Hioka
It was evaluated the properties of the xanthene dyes Erythrosin B, Eosin Y and theirs Methyl, Butyl and Decyl ester derivatives as possible photosensitizers (PS) for photodynamic treatments. The more hydrophobic dyes self-aggregate in water/ethanol solutions above 70% water (v/v) in the mixture. In buffered water these PS were encapsulated in Pluronic polymeric surfactants of P-123 and F-127 by two methodologies: direct addition and the thin-film solid dispersion methods. The thin solid method provided formulations with higher stabilities besides effective encapsulation of the PS as monomers...
September 26, 2016: Photochemistry and Photobiology
Gayatri C Patel, Megha Kasarwala
BACKGROUND: The purpose of this study was to investigate the application of a controlled porosity osmotic tablet (CPOT) utilizing solid dispersion (SD) of poorly soluble drug. The patents on Cyclobenzaprine HCl (US4968507 A) and Venlafaxine salts (EP 2085078 A1) helped in selection of drug and polymers. METHOD: The SDs having different ratio of drug to carrier (PVP K 30) were prepared by kneading method and optimized. Effect of three independent variables, total amount of osmogen (mannitol& potassium chloride), total amount of polymer (polyethylene oxide WSR 301, hydroxy propyl methyl cellulose K100 M), and polymer1: polymer 2 ratio was investigated using Box Behnken design...
October 4, 2016: Recent Patents on Drug Delivery & Formulation
Bin Tian, Xing Tang, Lynne S Taylor
The purpose of this study was to investigate the feasibility of using a fluorescence-based technique to evaluate drug-polymer miscibility and to probe the correlation between miscibility and physical stability of amorphous solid dispersions (ASDs). Indomethacin-hydroxypropyl methylcellulose (IDM-HPMC), indomethacin-hydroxypropyl methylcellulose acetate succinate (IDM-HPMCAS) and indomethacin-polyvinylpyrrolidone (IDM-PVP) were used as model systems. The miscibility of the IDM-polymer systems was evaluated by fluorescence spectroscopy, fluorescence imaging, differential scanning calorimetry (DSC) and infrared (IR) spectroscopy...
October 4, 2016: Molecular Pharmaceutics
Hisham Al-Obaidi, M Jayne Lawrence, Graham Buckton
OBJECTIVES: To understand the impact of ionic and non-ionic surfactants on the dissolution and stability properties of amorphous polymeric dispersions using griseofulvin (GF) as a model for poorly soluble drugs. METHODS: Solid dispersions of the poorly water-soluble drug, griseofulvin (GF) and the polymers, poly(vinylpyrrolidone) (PVP) and poly(2-hydroxypropyl methacrylate) (PHPMA), have been prepared by spray drying and bead milling and the effect of the ionic and non-ionic surfactants, namely sodium dodecyl sulphate (SDS) and Tween-80, on the physico-chemical properties of the solid dispersions studied...
October 2, 2016: Journal of Pharmacy and Pharmacology
Siyuan Huang, Chen Mao, Robert O Williams, Chia-Yi Yang
The solubility of a drug is ultimately governed by its chemical potential as it is present in the undissolved solute. For a pharmaceutical amorphous solid dispersion (ASD), its solubility depends on the state and composition of the undissolved solute when the ASD is equilibrated with water. Concerning the undissolved solute phase that can contain up to 3 components (drug, polymer, and water), we developed a complete thermodynamic model to calculate the chemical potential of a drug in the multicomponent, amorphous system...
September 28, 2016: Journal of Pharmaceutical Sciences
Justine Thiry, Fabrice Krier, Shenelka Ratwatte, Jean-Michel Thomassin, Christine Jerome, Brigitte Evrard
The aim of this study was to evaluate hot-melt extrusion (HME) as a continuous process to form cyclodextrin (CD) inclusion complexes in order to increase the solubility and dissolution rate of itraconazole (ITZ), a class II model drug molecule of the Biopharmaceutics Classification System. Different CD derivatives were tested in a 1:1 (CD:ITZ) molar ratio to obtain CD ternary inclusion complexes in the presence of a polymer, namely Soluplus(®) (SOL). The CD used in this series of experiments were β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD) with degrees of substitution of 0...
September 26, 2016: European Journal of Pharmaceutical Sciences
K Wlodarski, L Tajber, W Sawicki
The aim of this research was to develop immediate release tablets comprising solid dispersion (IRSDTs) of tadalafil (Td) in a vinylpyrrolidone and vinyl acetate block copolymer (PVP-VA), characterized by improved dissolution profiles. The solid dispersion of Td in PVP-VA (Td/PVP-VA) in a weight ratio of 1:1 (w/w) was prepared using two different processes i.e. spray drying and ball milling. While the former process has been well established in the formulation of IRSDTs the latter has not been exploited in these systems yet...
September 19, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Sherry J Morgan, Lauren M Besenhofer, Wayne Buck, Helga Lorenz, James W Rhodes, Yi Yang
A cutaneous response (localized swelling and/or erythema of the skin) has been noted in dog toxicology studies in which multiple, unrelated compounds were administered orally with copovidone as a vehicle. The response has been noted in studies with 6 different test items that are structurally unrelated and span several different therapeutic indications spanning an approximate 6-year period (2009-2015). A factor common among the studies is the formulation-a copovidone amorphous solid dispersion (ASD). Cutaneous responses have not been observed in dogs administered non-ASD formulations of the same test items but have occasionally been noted in placebo (copovidone control) dogs...
September 20, 2016: Toxicologic Pathology
Julien P Maincent, Laura K Najvar, William R Kirkpatrick, Siyuan Huang, Thomas F Patterson, Nathan P Wiederhold, Jay I Peters, Robert O Williams
Previously, modified release itraconazole in the form of a melt-extruded amorphous solid dispersion based on a pH dependent enteric polymer combined with hydrophilic additives (HME-ITZ), exhibited improved in vitro dissolution properties. These properties agreed with pharmacokinetic results in rats showing high and sustained itraconazole (ITZ) systemic levels. The objective of the present study was to better understand the best choice of rodent model for evaluating the pharmacokinetic and efficacy of this orally administered modified release ITZ dosage form against invasive Aspergillus fumigatus...
October 5, 2016: Drug Development and Industrial Pharmacy
Yue Cao, Li-Li Shi, Qing-Ri Cao, Mingshi Yang, Jing-Hao Cui
Poorly water-soluble drugs often suffer from limited or irreproducible clinical response due to their low solubility and dissolution rate. In this study, organic solvent-free solid dispersions (OSF-SDs) containing telmisartan (TEL) were prepared using polyvinylpyrrolidone K30 (PVP K30) and polyethylene glycol 6000 (PEG 6000) as hydrophilic polymers, sodium hydroxide (NaOH) as an alkalizer, and poloxamer 188 as a surfactant by a lyophilization method. In-vitro dissolution rate and physicochemical properties of the OSF-SDs were characterized using the USP I basket method, differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and fourier transform-infrared (FT-IR) spectroscopy...
2016: Iranian Journal of Pharmaceutical Research: IJPR
Hiroki Suzuki, Kodai Ueno, Takahiro Mizumoto, Yoshiki Seto, Hideyuki Sato, Satomi Onoue
The present study aimed to develop an inhalable self-micellizing solid dispersion of cyclosporine A (SMSD/CsA) for the direct delivery to the respiratory system with improved therapeutic efficacy and minimized systemic exposure. SMSD/CsA was obtained by wet-milling, and then jet-milled SMSD/CsA was blended with lactose carrier, producing a respirable powder of SMSD/CsA (SMSD/CsA-RP). The physicochemical, pharmacological, and pharmacokinetic properties of SMSD/CsA-RP were characterized, and the hepatotoxic and nephrotoxic potentials were investigated by biomarker analysis...
September 12, 2016: European Journal of Pharmaceutical Sciences
Sheng-Wei Chiu, Derek R Sturm, Justin D Moser, Ronald P Danner
A modification of a GC was developed to investigate both infinitely dilute and finite concentrations of solvents in polymers. Thermodynamic properties of hypromellose acetate succinate (HPMCAS-L)-acetone-water systems are important for the optimization of spray-drying processes used in pharmaceutical manufacturing of solid dispersion formulations. These properties, at temperatures below the glass transition temperature, were investigated using capillary column inverse gas chromatography (CCIGC). Water was much less soluble in the HPMCAS-L than acetone...
September 30, 2016: Journal of Chromatography. A
Anna Krupa, Marc Descamps, Jean-Francois Willart, Beata Strach, Elżbieta Wyska, Renata Jachowicz, Florence Danède
In this study, the suitability of high-energy ball milling was invesitaged with the aim to vitrify tadalafil (TD) and improve its bioavailability. To achieve this goal, pure TD as well as binary mixtures composed of the drug and Soluplus® (SL) were co-processed by high-energy ball milling. Modulated differential scanning calorimetry (MDSC) and X-ray powder diffraction (XRD) demonstrated that after such co-processing, the crystalline form of TD was transformed into an amorphous form. The presence of a single glass transition (Tg) for all the co-milled formulations indicated that TD was dispersed into SL at the molecular level, forming amorphous molecular alloys, regardless of the drug concentration...
September 12, 2016: Molecular Pharmaceutics
Soraya Hengsawas Surasarang, Justin M Keen, Siyuan Huang, Feng Zhang, James W McGinity, Robert O Williams Iii
The purpose of this study was to enhance the dissolution properties of albendazole (ABZ) by the use of amorphous solid dispersions. Phase diagrams of ABZ-polymer binary mixtures generated from Flory-Huggins theory were used to assess miscibility and processability. Forced degradation studies showed that ABZ degraded upon exposure to hydrogen peroxide and 1 N NaOH at 80°C for 5 min, and the degradants were albendazole sulfoxide (ABZSX), and ABZ impurity A, respectively. ABZ was chemically stable following exposure to 1 N HCl at 80°C for one hour...
September 12, 2016: Drug Development and Industrial Pharmacy
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"