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"solid dispersion"

Liana Stanislavovna Usmanova, Marat Akhmedovich Ziganshin, Valery Vilenovich Gorbatchuk, Sufia Askhatovna Ziganshina, Dmitry Anatolevich Bizyaev, Anastas Akhmetovich Bukharaev, Timur Anvarovich Mukhametzyanov, Alexander Vladimirovich Gerasimov
A lot of pharmaceutical substances have a poor solubility that limits their absorption and distribution to the targeted sites to elicit the desired action without causing untoward effects on healthy cells or tissues. For such drugs, new modes of delivery have to be developed for efficient and effective delivery of the drug to the target site. Formation of magnetically active solid dispersion of such drugs could be a useful approach to addressing this problem because they combine targeted delivery and good solubility...
January 2017: Journal of Advanced Pharmaceutical Technology & Research
Hyun-Jong Cho, Jun-Pil Jee, Ji-Ye Kang, Dong-Yeop Shin, Han-Gon Choi, Han-Joo Maeng, Kwan Hyung Cho
The aim of this work was to develop cefdinir solid dispersions (CSDs) prepared using hydrophilic polymers with enhanced dissolution/solubility and in vivo oral bioavailability. CSDs were prepared with hydrophilic polymers such as hydroxypropyl-methylcellulose (HPMC; CSD1), carboxymethylcellulose-Na (CMC-Na; CSD2), polyvinyl pyrrolidone K30 (PVP K30; CSD3) at the weight ratio of 1:1 (drug:polymer) using a spray-drying method. The prepared CSDs were characterized by aqueous solubility, differential scanning calorimetry (DSC), powder X-ray diffraction (p-XRD), scanning electron microscopy (SEM), aqueous viscosity, and dissolution test in various media...
February 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Qi Zhang, Yiqiong Pu, Bing Wang, Yuqin Wang, Tina Tingxia Dong, Tao Guo, Tong Zhang, Zhenzhen Cai
In this study, we prepared solid dispersions (SDs) of 20(S)-protopanaxadiol (PPD) using a melting-solvent method with different polymers, in order to improve the solubility and dissolution performance of drugs with poor water solubility. The SDs were characterized via differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), and molecular docking and dynamics study. DSC and PXRD results indicated that PPD crystallinity in SDs was significantly reduced, and that the majority of PPD is amorphous...
February 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Avital Beig, Noa Fine-Shamir, David Lindley, Jonathan M Miller, Arik Dahan
Rifaximin is a BCS class IV (low-solubility, low-permeability) drug and also a P-gp substrate. The aims of this work were to assess the efficiency of different rifaximin amorphous solid dispersion (ASDs) formulations in achieving and maintaining supersaturation and to investigate the consequent solubility-permeability interplay. Spray-dried rifaximin ASDs were prepared with different hydrophilic polymers and their ability to achieve and maintain supersaturation was assessed. Then, rifaximin's apparent intestinal permeability was investigated as a function of increasing supersaturation both in vitro using the parallel artificial membrane permeability assay (PAMPA) and in vivo using the single-pass rat intestinal perfusion (SPIP) model...
February 15, 2017: AAPS Journal
Zhi-Hong Liu, Xue-Jing Li, Ai-Wen Huang, Jing Zhang, Hong-Tao Song
PURPOSE: This study aimed to develop a synchronized and sustained-release silymarin dropping pill, and to evaluate its pharmacokinetic characteristics. METHODS: Polyoxyethylene stearate, glyceryl monostearate, and stearic acid were used to prepare the dropping pills. X-ray powder diffraction, differential scanning calorimetry, and release were used to evaluate its physicochemical properties. The plasma concentration of silybin in beagle dogs after oral administration of silymarin dropping pills and silymarin capsule was determined by RP-HPLC...
February 13, 2017: Current Drug Delivery
Koji Takeda, Yuto Gotoda, Daichi Hirota, Fumihiro Hidaka, Tomo Sato, Tsutashi Matsuura, Hiroyuki Imanaka, Naoyuki Ishida, Koreyoshi Imamura
The technique for homogeneously dispersing hydrophobic drugs in a water-soluble solid matrix (solid dispersion) is a subject that has been extensively investigated in the pharmaceutical industry. Herein, a novel technique for dispersing a solid, without the need to use a surfactant, is reported. A freeze-dried amorphous sugar sample was dissolved in an organic solvent, that contained a soluble model hydrophobic component. The suspension of the sugar and the model hydrophobic component was vacuum foam dried to give a solid powder...
February 13, 2017: Molecular Pharmaceutics
Qiong Wu, Michael T Kennedy, Karthik Nagapudi, Y-H Kiang
Poloxamer 188, a commonly used emulsifying and solubilizing agent, was found to be the cause of crystallization of an investigational drug, AMG 579, from its amorphous solid dispersion at accelerated storage conditions. Investigation of this physical stability issue included thorough characterization of poloxamer 188 at non-ambient conditions. At 40°C, poloxamer 188 becomes deliquescent above relative humidity of 75%. Upon returning to ambient conditions, the deliquescent poloxamer 188 loses water and re-solidifies...
February 2, 2017: International Journal of Pharmaceutics
Thanu Thongnopkoon, Satit Puttipipatkhachorn
This study was aimed to examine the nanoparticle formation from redispersion of binary and ternary solid dispersions. Binary systems composed of various ratios of glibenclamide (GBM) and polyvinylpyrrolidone K30 (PVP-K30), whereas a constant amount at 2.5%w/w of a surfactant, sodium lauryl sulfate (SLS) or Gelucire44/14 (GLC), was added to create ternary systems. GBM nanoparticles were collected after the systems were dispersed in water for 15 minutes. The obtained nanoparticles were characterized for size distribution, crystallinity, thermal behavior, molecular structure, and dissolution properties...
February 6, 2017: Drug Development and Industrial Pharmacy
YanXin Yu, Shan Xu, Hong You, YinJie Zhang, Bo Yang, XiaoYang Sun, LingLin Yang, Yue Chen, ShaoZhi Fu, JingBo Wu
In this study, our purpose was to explore the synergistic anti-tumor effect and mechanism of paclitaxel nanoparticles (PTX-NPs) combined with radiotherapy (RT) on human cervical carcinoma (HeLa). PTX-NPs were prepared by a solid dispersion method using methoxy poly(ethylene glycol)-poly(ɛ-caprolactone) (MPEG-PCL), which combined with RT exerted a potent and high efficient effect against cervical cancer. In vivo antitumor activity of PTX-NPs combined with RT, was estimated using nude mice carrying Hela cell xenograft tumor...
November 2017: Drug Delivery
Manoela K Riekes, Aswin Dereymaker, Philippe Berben, Patrick Augustijns, Hellen K Stulzer, Guy Van den Mooter
Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus(®), top-coated with an enteric layer. The impact of different bead size, enteric polymers (Eudragit L100(®) and Eudragit L100-55(®)) and coating time was investigated. Samples were evaluated by X-ray diffraction, scanning electron microscopy, laser diffraction and in vitro studies in 0...
January 30, 2017: International Journal of Pharmaceutics
Wenjun Huang, Taraknath Mandal, Ronald G Larson
We present coarse-grained (CG) force fields for Hydroxypropyl-Methylcellulose Acetate Succinate (HPMCAS) polymers and the drug molecule phenytoin using a bead/stiff spring model, with each bead representing a HPMCAS monomer or monomer side group (hydroxypropyl acetate, acetate, or succinate), or a single phenytoin ring. We obtain the bonded and non-bonded interaction parameters in our CG model using the RDFs from atomistic simulations of short HPMCAS model oligomers (20-mer) and atomistic simulations of phenytoin molecules...
January 31, 2017: Molecular Pharmaceutics
Xu Liu, Lin Zhou, Feng Zhang
The purpose of this study was to investigate the reaction between naproxen (NPX) and meglumine (MEG) at elevated temperature and to study the effect of this reaction on the physical stabilities and in vitro drug-release properties of melt-extruded naproxen amorphous solid dispersions (ASDs). Differential scanning calorimetry, hot-stage polarized light microscopy, Fourier transform infrared spectroscopy, and X-ray photoelectron spectroscopy analyses demonstrated that in situ salt formation with proton transfer between NPX and MEG occurred at elevated temperature during the melt extrusion process...
January 30, 2017: Molecular Pharmaceutics
Hideyuki Sato, Mizuki Ogino, Keisuke Yakushiji, Hiroki Suzuki, Ken-Ichi Shiokawa, Hiroshi Kikuchi, Yoshiki Seto, Satomi Onoue
The aim of this study is to enhance the antihypothermic action of ginger extract (GE) employing a solid dispersion (SD) approach. The prepared SD of GE (GE/SD) was characterized in terms of physicochemical and pharmacokinetic properties. The antihypothermic action of GE samples was evaluated in a rat model of hypothermia. GE/SD exhibited improved dissolution behavior of the major active ingredients in GE, 6-gingerol (6G) and 8-gingerol (8G), with levels of dissolution 12- and 31-fold higher than that of GE, respectively...
February 13, 2017: Journal of Agricultural and Food Chemistry
Mark T Davis, Catherine B Potter, Maryam Mohammadpour, Ahmad B Albadarin, Gavin M Walker
A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40°C/75% RH. A number of solid state analytical techniques including PXRD, DSC, small angle X-ray scattering, FTIR and solid state NMR were used to characterise the physicochemical properties of the ASDs following processing and storage and to assess any interactions between components...
January 25, 2017: International Journal of Pharmaceutics
Mai Khanfar, Suhair Al-Nimry
Lovastatin (LOV), an antihyperlipidimic agent, is characterized by low solubility/poor dissolution and, thus, low bioavailability (<5%). A beneficial effect on its bioavailability could result from improving its dissolution. One of the most common methods used to enhance dissolution is the preparation of solid dispersions. Solid dispersions of LOV and silica with different surface areas were prepared. The effects of the type of silica, ratio of drug/silica, incubation period with silica, and the effect of surface area were all studied...
January 26, 2017: AAPS PharmSciTech
Hideto Minami, Akihiro Kojima, Toyoko Suzuki
Flattened cross-linked hollow poly(divinylbenzene) (PDVB) particles with encapsulated n-hexadecane (HD) were successfully prepared through suspension polymerization using the self-assembling of phase-separated polymer (SaPSeP) method, in which the solid dispersion medium was gelled by gellan gum and compressed. The solid phase induced by gellan gum can be easily changed to a liquid state by heating, allowing the obtained particles to be easily recovered after polymerization. When the polymerization was conducted in the solid dispersion medium without compression, spherical hollow PDVB/HD composite particles were obtained...
February 3, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
Krishnamoorthy Venkateskumar, Subramani Parasuraman, Raju Gunasunderi, Krishnan Sureshkumar, M Muralidhar Nayak, Syed Adnan Ali Shah, Khoo Kassen, Heng Wei Kai
OBJECTIVE: The objective of this study is to provide a mechanistic insight into solubility enhancement and dissolution of acyclovir (ACY) by polyethylene glycol20000 (PEG20000). MATERIALS AND METHODS: Solid dispersions with differing ratios of drug (ACY) and carrier (PEG20000) were prepared and evaluated by phase solubility, in vitro release studies, kinetic analysis, in situ perfusion, and in vitro permeation studies. Solid state characterization was also done by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared spectroscopy (FT-IR) analysis and surface morphology was assessed by Polarizing Microscopic Image (PMI) analysis, Scanning Electron Microscopy (SEM), Atomic Force Microscopy (AFM), and Nuclear Magnetic Resonance (NMR) analysis...
October 2016: International Journal of Pharmaceutical Investigation
M Maniruzzaman, S A Ross, M T Islam, N Scoutaris, A Nair, Dennis Douroumis
The purpose of this study was to evaluate the performance of Neusilin® (NEU) a synthetic magnesium aluminometasilicate as inorganic drug carrier co-processed with the hydrophilic surfactants Labrasol and Labrafil to develop Tranilast (TLT) based solid dispersions using continuous melt extrusion (HME) processing. Twin - screw extrusion was optimized to develop various TLT/excipient/surfactant formulations followed by continuous capsule filling in the absence of any downstream equipment. Physicochemical characterisation showed the existence of TLT in partially crystalline state in the porous network of inorganic NEU for all extruded formulations...
January 26, 2017: Drug Development and Industrial Pharmacy
Raid Alany
No abstract text is available yet for this article.
February 2017: Pharmaceutical Development and Technology
Maria Doreth, Murtadha Abdul Hussein, Petra A Priemel, Holger Grohganz, René Holm, Heidi Lopez de Diego, Thomas Rades, Korbinian Löbmann
In situ amorphization is a concept that allows to amorphize a given drug in its final dosage form right before administration. Hence, this approach can potentially be used to circumvent recrystallization issues that other amorphous formulation approaches are facing during storage. In this study, the feasibility of microwave irradiation to prepare amorphous solid dispersions (glass solutions) in situ was investigated. Indomethacin (IND) and polyvinylpyrrolidone K12 (PVP) were tableted at a 1:2 (w/w) ratio. In order to study the influence of moisture content and energy input on the degree of amorphization, tablet formulations were stored at different relative humidity (32, 43 and 54% RH) and subsequently microwaved using nine different power-time combinations up to a maximum energy input of 90kJ...
January 20, 2017: International Journal of Pharmaceutics
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