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https://www.readbyqxmd.com/read/28528850/overview-of-solidification-techniques-for-self-emulsifying-drug-delivery-systems-from-industrial-perspective
#1
J Mandić, A Zvonar Pobirk, F Vrečer, M Gašperlin
Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different solidification techniques selfemulsifying powders, granules, pellets and tablets can be produced...
May 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28523632/co-spray-drying-with-hpmc-as-a-platform-to-improve-direct-compaction-properties-of-various-tablet-fillers
#2
JinZhi Li, LiJie Zhao, Xiao Lin, Lan Shen, Yi Feng
Many commonly used tablet fillers are not suitable for direct compaction process due to insufficient properties, mainly of flowability and compactability. This work therefore aimed to use co-spray drying with HPMC as a platform to improve direct compaction properties of various tablet fillers. Starch, calcium hydrogen phosphate dihydrate (DCPD), and mannitol were chosen as a representative of three types of commonly used fillers (i.e. organic macromolecules, water-insoluble inorganic salts, and water-soluble small molecular carbohydrates), respectively...
May 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28523384/the-need-for-restructuring-the-disordered-science-of-amorphous-drug-formulations
#3
REVIEW
Khadijah Edueng, Denny Mahlin, Christel A S Bergström
The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago...
May 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28522002/freeze-dried-cylinders-carrying-chitosan-nanoparticles-for-vaginal-peptide-delivery
#4
Marzia Marciello, Silvia Rossi, Carla Caramella, Carmen Remuñán-López
Recently nanoparticle-based vaginal drug delivery formulations have been acquiring great attention for the administration of peptide based-vaccines or microbicides to prevent or treat sexually transmitted diseases. In this work, a straightforward and efficient strategy for the vaginal application and release of peptide-loaded mucoadhesive nanoparticles was developed. This essentially consists of chitosan nanoparticles encapsulated in suitable hydrophilic freeze-dried cylinders. Chitosan nanoparticles are responsible for carrying the peptide drug and allowing adhesion to the vaginal mucosal epithelium...
August 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28521373/paediatric-medicines-regulatory-and-scientific-issues
#5
Chrysa Daousani, Vangelis D Karalis
In the past, dosage regimens authorized for adults were extrapolated to children relying mainly on empirical dosage adjustments. However, children are not small adults, but a distinct and heterogeneous group in terms of physiology, disease occurrence, pharmacokinetics, pharmacodynamics and also psychological, cognitive, and behavioral aspects. Even though it would be helpful to know the physiological changes and the special drug treatment needs in children, this task could not be performed due to ethical reasons...
May 18, 2017: Drug Research
https://www.readbyqxmd.com/read/28512054/synthesis-and-characterization-of-psyllium-seed-mucilage-grafted-with-n-n-methylene-bisacrylamide
#6
Monica R P Rao, Laxmi Babrekar, Vaishali S Kharpude, Jagruti Chaudhari
Psyllium seed polysaccharide was modified to investigate its use as multifunctional pharmaceutical excipient. The objective of this study was isolation of psyllium seed polysaccharide and crosslinking with acrylic acid using N,N-methylene bisacrylamide and its characterization. Acrylic acid was used as monomer and ammonium persulfate as initiator. A full factorial design was employed to optimize the crosslinking. The modified polysaccharide was characterized by FTIR, DSC, PXRD, loss on drying, pH, viscosity, micromeritics properties and swelling studies in 0...
May 13, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28511881/-what-medication-should-be-prescribed-to-a-patient-with-coeliac-disease
#7
C Pérez-Diez, S Guillén-Lorente, P Palomo-Palomo
Coeliac disease is a permanent intolerance to gluten proteins from wheat, rye, barley and triticale. Although strict adherence is complicated, the only effective treatment is a gluten-free diet throughout life. Some drugs contain starch as an excipient, and there is a risk related to the gluten content, which must be avoided in these patients. Current legislation requires the analysis of the protein content of wheat starch, or the absence of starches from another source where rice, maize, or potato starches are used as excipients...
May 13, 2017: Semergen
https://www.readbyqxmd.com/read/28508349/the-contemporary-role-of-stents-and-angioplasty-for-the-treatment-of-infrapopliteal-disease-in-critical-limb-ischemia
#8
REVIEW
Tarek A Hammad, Anand Prasad
PURPOSE OF REVIEW: Critical limb ischemia (CLI) is associated with significant morbidity, mortality, and increased health care expenses. Revascularization has a central role in the treatment of CLI. Following publication of BASIL (bypass versus angioplasty in severe ischemia of the leg) trial a decade ago, an "endovascular first" approach had gained momentum and the technologies available for endovascular therapy have exponentially increased. Both the development of technology and technique, highlighted in this review, have allowed operators to treat complex infrapopliteal lesions which are central to CLI pathology...
July 2017: Current Cardiology Reports
https://www.readbyqxmd.com/read/28507936/thermal-stability-and-kinetic-study-of-fluvoxamine-stability-in-binary-samples-with-lactose
#9
Faranak Ghaderi, Mahboob Nemati, Mohammad Reza Siahi-Shadbad, Hadi Valizadeh, Farnaz Monajjemzadeh
Purpose: In the present study the incompatibility of FLM (fluvoxamine) with lactose in solid state mixtures was investigated. The compatibility was evaluated using different physicochemical methods such as differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR) spectroscopy and mass spectrometry. Methods: Non-Isothermally stressed physical mixtures were used to calculate the solid-state kinetic parameters. Different thermal models such as Friedman, Flynn-Wall-Ozawa (FWO) and Kissinger-Akahira-Sunose (KAS) were used for the characterization of the drug-excipient interaction...
April 2017: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28506515/combined-semi-empirical-screening-and-design-of-experiments-doe-approach-to-identify-candidate-formulations-of-a-lyophilized-live-attenuated-tetravalent-viral-vaccine-candidate
#10
Ashaben Patel, Steven M Erb, Linda Strange, Ravi S Shukla, Ozan Kumru, Lee Smith, Paul Nelson, Sangeeta B Joshi, Jill A Livengood, David B Volkin
A combination experimental approach, utilizing semi-empirical excipient screening followed by statistical modeling using design of experiments (DOE), was undertaken to identify stabilizing candidate formulations for a lyophilized live attenuated Flavivirus vaccine candidate. Various potential pharmaceutical compounds used in either marketed or investigative live attenuated viral vaccine formulations were first identified. The ability of additives from different categories of excipients, either alone or in combination, were then evaluated for their ability to stabilize virus against freeze-thaw, freeze-drying, and accelerated storage (25°C) stresses by measuring infectious virus titer...
May 12, 2017: Vaccine
https://www.readbyqxmd.com/read/28502898/development-of-modified-release-3d-printed-tablets-printlets-with-pharmaceutical-excipients-using-additive-manufacturing
#11
Alvaro Goyanes, Fabrizio Fina, Annalisa Martorana, Daniel Sedough, Simon Gaisford, Abdul W Basit
The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into enteric printlets incorporating up to 50% drug loading with two different infill percentages (20 and 100%)...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502896/a-quality-by-design-qbd-twin-screw-extrusion-wet-granulation-approach-for-processing-water-insoluble-drugs
#12
Mohammed Maniruzzaman, Steven A Ross, Tumpa Dey, Arun Nair, Martin J Snowden, Dennis Douroumis
In this study, a Quality by Design (QbD) approach was used to identify the effect of formulation parameters in a twin screw wet extrusion granulation process for the manufacturing of ibuprofen (IBU) granules with increased dissolution rates. A fractional factorial Design of Experiment (DoE) was used to investigate the effect of the excipient composition, binder amount and liquid to solid (L/S) ratio (independent variables) on drug dissolution rates, median particle size diameter and specific surface area (dependent variables)...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502177/leveraging-colloidal-aggregation-for-drug-rich-nanoparticle-formulations
#13
Ahil N Ganesh, Jennifer Logie, Christopher K McLaughlin, Benjamin L Barthel, Tad H Koch, Brian K Shoichet, Molly S Shoichet
While limited drug loading continues to be problematic for chemotherapeutics formulated in nanoparticles, we found that we could take advantage of colloidal drug aggregation to achieve high loading when combined with polymeric excipients. We demonstrate this approach with two drugs, fulvestrant and pentyl-PABC doxazolidine (PPD; a prodrug of doxazolidine, which is a DNA cross-linking anthracycline), and two polymers, polysorbate 80 (UP80) and poly(d,l-lactide-co-2-methyl-2-carboxytrimethylene carbonate)-graft-poly(ethylene glycol) (PLAC-PEG; a custom-synthesized, self-assembling amphiphilic polymer)...
May 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28501673/chemotherapeutic-drug-photothermal-agent-co-self-assembling-nanoparticles-for-near-infrared-fluorescence-and-photoacoustic-dual-modal-imaging-guided-chemo-photothermal-synergistic-therapy
#14
Yang Li, Guihua Liu, Jinyuan Ma, Jinyan Lin, Huirong Lin, Guanghao Su, Dengyue Chen, Shefang Ye, Xiaoyuan Chen, Xuan Zhu, Zhenqing Hou
Multimodal imaging-guided synergistic combination therapy has shown great potential for cancer treatment. However, the nanocarrier-based theranostic systems suffer from batch-to-batch variation, complexity of multicomponent, poor drug loading, and carrier-related toxicity issues. To address these issues, herein we developed a novel carrier-free theranostic system with nanoscale characteristics for near-infrared fluorescence (NIRF) and photoacoustic (PA) dual-modal imaging-guided synergistic chemo-photothermal therapy (PTT)...
May 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28501440/classification-of-microcrystalline-celluloses-via-structures-of-individual-particles-measured-by-synchrotron-radiation-x-ray-micro-computed-tomography
#15
Longwei Fang, Xianzhen Yin, Li Wu, Yaping He, Yuanzhi He, Wei Qin, Fanyue Meng, Peter York, Xu Xu, Jiwen Zhang
Microcrystalline cellulose (MCC) is one of the most important excipients due to its outstanding binding and tableting properties. Owing to the absence of high resolution characterization techniques at the single particle scale, 3D (three dimension) microstructure of MCC and its effects on formulation performance remain unexamined. The aim of this work was to establish a methodology for single particles of MCC type 102 based on synchrotron radiation X-ray micro computed tomography (SR-μCT), principal component analysis (PCA) and partial least square discriminant analysis (PLSDA)...
May 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28500485/hydroxyurea-lactose-interaction-study-in-silico-and-in-vitro-evaluation
#16
Kunal B Bachchhao, R R Patil, C R Patil, Dipak D Patil
The Maillard reaction between hydroxyurea (a primary amine-containing drug) and lactose (used as an excipient) was explored. The adduct of these compounds was synthesized by heating hydroxyurea with lactose monohydrate at 60 °C in borate buffer (pH 9.2) for 12 h. Synthesis of the adduct was confirmed using UV-visible spectroscopy and Fourier transform infrared, differential scanning calorimetry, high-pressure liquid chromatography, and liquid chromatography-mass spectrometry studies. An in silico investigation of how the adduct formation affected the interactions of hydroxyurea with its biological target oxyhemoglobin, to which it binds to generate nitric oxide and regulates fetal hemoglobin synthesis, was carried out...
May 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28499879/developing-a-flexible-pediatric-dosage-form-for-antiretroviral-therapy-a-fast-dissolving-tablet
#17
Manjari Lal, Manshun Lai, Marcus Estrada, Changcheng Zhu
Current presentations of the anti-HIV drugs lopinavir and ritonavir make appropriate dosing for children difficult. We conducted a feasibility study to develop a formulation for these drugs with child-safe excipients in a flexible dosage form for children across the pediatric age spectrum. The freeze-drying-in-blister approach was used to produce fast-dissolving tablets (FDTs), as these can be dispersed in fluids for easy administration, even to infants, and appropriate portions of the dispersion can be given for different ages/weights...
May 9, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28499202/novel-dual-ves-phospholipid-self-assembled-liposomes-with-an-extremely-high-drug-loading-efficiency
#18
Yongpeng Hou, Chen Yao, Longbing Ling, Yawei Du, Ruiyu He, Muhammad Ismail, Ying Zhang, Zhenglin Fu, Xinsong Li
Vitamin E succinate (VES), a unique selective anti-cancer drug, has attracted much attention for its ability to induce apoptosis in various cancer cells. Importantly, it has been reported that VES is largely non-toxic to normal cells. However, poor aqueous solubility and bioavailability extensively restricted its clinical utility. In this report, dual VES phospholipid conjugate (di-VES-GPC) prodrug based liposomes were prepared in order to develop an efficient delivery system for VES. Di-VES-GPC was first synthesized by conjugating VES with l-α-glycerophosphorylcholine (GPC) using N,N'-dicyclohexylcarbodiimide (DCC) as a coupling agent...
May 2, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28496466/validated-spectrophtometric-method-for-simultaneous-determination-of-buprenorphine-and-naloxone-in-pharmaceutical-dosage-forms
#19
Effat Souri, Farzaneh Sadat Ahmadi, Maliheh Barazandeh Tehrani, Majid Mohammad Hosseini, Sedigheh Fadaye Vatan
Buprenorphine is a partial mu agonist and kappa antagonist which is used for the treatment of pain and opioid addiction. A mixture of buprenorphine hydrochloride and naloxone hydrochloride has been approved for the treatment of opioid dependence. In this study a third order derivative spectrophotometric method based on zero-crossing technique has been used for the simultaneous determination of buprenorphine hydrochloride and naloxone hydrochloride in tablets. The measurements were carried out at wavelengths of 257...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28495581/dipicolinic-acid-as-a-novel-spore-inspired-excipient-for-antibody-formulation
#20
Iris L Batalha, Peng Ke, Esther Tejeda-Montes, Shahid Uddin, Christopher F van der Walle, Graham Christie
Ionic excipients are commonly used in aqueous therapeutic monoclonal antibody (mAb) formulations. Novel excipients are of industrial interest, with a recent focus on Arg salt forms and their application as viscosity reducing and stabilizing additives. Here, we report that the calcium salt of dipicolinic acid (DPA, pyridine-2,6-dicarboxylic acid), uniquely present in nature in the core of certain bacterial spores, reduces the viscosity of a mAb formulated at 150mg/mL, below that achieved by Arg hydrochloride at the same concentration (10mM)...
May 8, 2017: International Journal of Pharmaceutics
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