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https://www.readbyqxmd.com/read/28642203/developments-of-polysorbate-tween-based-microemulsions-preclinical-drug-delivery-toxicity-and-antimicrobial-applications
#1
REVIEW
Gurpreet Kaur, S K Mehta
The present review deals with the progress of Polysorbates (Tween) based microemulsions in drug delivery. PEGylated Sorbitan Fatty Acid Esters (Tweens/Polysorbates) are one of the most used non-ionic surfactants. Particularly Polysorbates based microemulsion has been widely used for enhancing solubilization of poorly soluble drugs. This article deals with underlying the preclinical factors which affect the solubilization efficacy of Tween formulations, implication of pharmaceutically accepted vectors in terms of absorption, bioavailability, biological fate and potential toxicity...
June 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28639467/ethanol-induced-symptoms-in-patients-receiving-gemcitabine-diluted-from-a-concentrate-for-solution-for-infusion-containing-ethanol
#2
Raúl Diez-Fernández, Rocío Vázquez-Sánchez, Laura López-Esteban, Santos Enrech-Frances, Ana María Sánchez-Peña, Laura Díaz-Paniagua, Miguel Soria-Tristán, José Miguel Martín Martínez, Teresa Molina-García
Purpose Ethanol as an excipient is used to enhance the solubility of gemcitabine, but, sometimes, the dose of ethanol a patient may be given is much higher than the dose considered to be toxic. We aimed to assess ethanol-related symptoms and signs in patients receiving two formulations of gemcitabine, with and without ethanol. Methods A randomized double blind cross-over study was conducted. All patients being treated with gemcitabine received two consecutive doses of the drug, one diluted from a concentrate for solution for infusion (CSI) containing ethanol and the other from a lyophilized powder, without ethanol, which was used as control group...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28633064/an-innovative-approach-to-bioremediation-of-mercury-contaminated-soils-from-industrial-mining-operations
#3
Damien McCarthy, Grant C Edwards, Mae S Gustin, Andrew Care, Matthieu B Miller, Anwar Sunna
Soils contaminated with mercury (Hg) have proved expensive and logistically difficult to remediate. Research continues into finding suitable environmentally-friendly and efficient ways of achieving this end. Bioremediation is an option, which employs the strategies microorganisms have evolved to deal with Hg. One microbial strategy involves uptake and intracellular volatilisation of mercuric ions, which passively diffuse from the cell and back into the atmosphere. In this work, Pseudomonas veronii cells grown to stationary phase were immobilised in a xanthan gum-based biopolymer via encapsulation...
June 14, 2017: Chemosphere
https://www.readbyqxmd.com/read/28629984/the-contribution-of-the-in-vivo-fate-of-an-oil-depot-to-drug-absorption
#4
R W Kalicharan, C Oussoren, P Schot, E de Rijk, H Vromans
Sustained release of lipophilic compounds can be achieved with oil depots. These parenteral formulations are generally injected in the vastus lateralis and deltoid muscle. It is known that the absorption rate differs between these two muscles. The reason for this is not fully understood. The aim of the current study was to investigate the fate of an oil depot in different tissues to elucidate whether the disappearance rate of oil is the cause of observed differences in absorption rate. A study with healthy volunteers was conducted to determine 1...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28628923/cremophor-el-alters-the-plasma-protein-binding-and-pharmacokinetic-profile-of-valspodar-in-rats
#5
Ziyad Binkhathlan
Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray(®)) contains cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28627457/analysis-of-the-origins-of-content-non-uniformity-in-high-shear-wet-granulation
#6
Sarang Oka, David Smrčka, Anjali Kataria, Heather Emady, Fernando Muzzio, František Štěpánek, Rohit Ramachandran
In this study, the origins of granule content non-uniformity in the high-shear wet granulation of a model two-component pharmaceutical blend were investigated. Using acetaminophen as the active pharmaceutical ingredient (API) and microcrystalline cellulose as the excipient, the distribution of the API across the granule size classes was measured for a range of conditions that differed in the duration of the initial dry mixing stage, the overall composition of the blend and the wet massing time. The coarse granule fractions were found to be systematically sub-potent, while the fines were enriched in the API...
June 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28625149/stability-indicating-reverse-phase-hplc-method-for-estimation-of-rifampicin-and-piperine-in-pharmaceutical-dosage-form
#7
Umang H Shah, Shraddha Patel, Manan Raval
BACKGROUND: High performance liquid chromatography is an integral analytical tool in assessing drug product stability. HPLC methods should be able to separate, detect, and quantify the various drug-related degradants that can form on storage or manufacturing, plus detect and any drug-related impurities that may be introduced during synthesis. OBJECTIVE: A simple, economic, selective, precise, and stability-indicating HPLC method has been developed and validated for analysis of Rifampicin (RIFA) and Piperine (PIPE) in bulk drug and in the formulation...
June 18, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28624420/biophysical-characterization-and-thermal-stability-of-pneumococcal-histidine-triad-protein-d-phtd-in-the-presence-of-zinc-and-manganese
#8
Salvador F Ausar, Kavisha Jayasundara, Lamees Akawi, Cristopher Roque, Anthony Sheung, Jian Hu, Marina Kirkitadze, Nausheen Rahman
The Pneumococcal Histidine Triad Protein D (PhtD) is believed to play a central role in pneumococcal metal ion homeostasis and has been proposed as a promising vaccine candidate against pneumococcal disease. To investigate for potential stabilizers, a panel of physiologically relevant metals was screened using the thermal shift assay and it was found that only Zn(2+) and Mn(2+) were able to increase PhtD melting temperature. Differential Scanning Calorimetry (DSC) analysis revealed a sequential unfolding of PhtD and the presence of at least 3 independent folding domains that can be stabilized by Zn(2+) and Mn(2+)...
June 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28620763/anticancer-efficacy-of-self-nanoemulsifying-drug-delivery-system-of-sunitinib-malate
#9
Saad M Alshahrani, Abdullah S Alshetaili, Ahmed Alalaiwe, Bader B Alsulays, Md Khalid Anwer, Ramadan Al-Shdefat, Faisal Imam, Faiyaz Shakeel
Sunitinib malate (SM) is reported as a weakly soluble drug in water due to its poor dissolution rate and oral bioavailability. Hence, in the current study, various "self-nanoemulsifying drug delivery systems (SNEDDS)" of SM were prepared, characterized and evaluated for the enhancement of its in vitro dissolution rate and anticancer efficacy. On the basis of solubilization potential of SM in various excipients, "Lauroglycol-90 (oil), Triton-X100 (surfactant) and Transcutol-P (cosurfactant)" were selected for the preparation of SM SNEDDS...
June 15, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28619620/development-of-a-solid-dosage-platform-for-the-oral-delivery-of-bilayer-vesicles
#10
Jitinder S Wilkhu, Sarah E Mcneil, David E Anderson, Marc Kirchmeier, Yvonne Perrie
Within this work, we develop vesicles incorporating sub-unit antigens as solid dosage forms suitable for the oral delivery of vaccines. Using a combination of trehalose, dextran and mannitol, freeze-dried oral disintegrating tablets were formed which upon rehydration release bilayer vesicles incorporating antigen. Initial studies focused on the optimisation of the freeze-dry cycle and subsequently excipient content was optimised by testing tablet hardness, disintegration time and moisture content. The use of 10% mannitol and 10% dextran produced durable tablets which offered strong resistance to mechanical damage yet appropriate disintegration times and dispersed to release niosomes-entrapping antigen...
June 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28619610/forecasting-gastrointestinal-precipitation-and-oral-pharmacokinetics-of-dantrolene-in-dogs-using-an-in-vitro-precipitation-testing-coupled-with-in-silico-modeling-and-simulation
#11
Atsushi Kambayashi, Jennifer B Dressman
The aim of the current research was to determine the precipitation kinetics of dantrolene sodium using canine biorelevant in vitro testing and to model the precipitation kinetics by appropriately coupling the data with an in silico tool adapted for dogs. The precipitation profiles of dantrolene sodium solutions were obtained with the in vitro paddle apparatus at a revolution rate of 50 rpm. The in silico prediction tool was designed using STELLA software and the predicted plasma concentration profiles of dantrolene using the in vitro precipitation data were compared with the observed in vivo pharmacokinetics in beagle dogs...
June 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28618348/ultrasound-sensitive-nanoparticle-aggregates-for-targeted-drug-delivery
#12
Anne-Laure Papa, Netanel Korin, Mathumai Kanapathipillai, Akiko Mammoto, Tadanori Mammoto, Amanda Jiang, Robert Mannix, Oktay Uzun, Christopher Johnson, Deen Bhatta, Garry Cuneo, Donald E Ingber
Here we describe injectable, ultrasound (US)-responsive, nanoparticle aggregates (NPAs) that disintegrate into slow-release, nanoscale, drug delivery systems, which can be targeted to selective sites by applying low-energy US locally. We show that, unlike microbubble based drug carriers which may suffer from stability problems, the properties of mechanical activated NPAs, composed of polymer nanoparticles, can be tuned by properly adjusting the polymer molecular weight, the size of the nanoparticle precursors as well as the percentage of excipient utilized to hold the NPA together...
September 2017: Biomaterials
https://www.readbyqxmd.com/read/28612663/development-of-multiple-unit-pellet-system-tablets-by-employing-the-sedem-expert-diagram-system-i-pellets-with-different-sizes
#13
Hannlie Hamman, Josias Hamman, Anita Wessels, Jacques Scholtz, Jan Steenekamp
Multiple-unit pellet systems (MUPS) provide several pharmacokinetic and pharmacodynamic advantages over single-unit dosage forms, however, compression of pellets into MUPS tablets present certain challenges. Although the SeDeM Expert Diagram System (SeDeM EDS) was originally developed to provide information about the most appropriate excipient and the minimum amount thereof that is required for producing direct compressible tablets, this study investigated the possibility to apply the SeDeM EDS in the production of MUPS tablets...
June 14, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28610740/toxicity-and-biodistribution-of-orally-administered-casein-nanoparticles
#14
Ana Gloria Gil, Juan Manuel Irache, Iván Peñuelas, Carlos Javier González Navarro, Adela López de Cerain
In the last years, casein nanoparticles have been proposed as carriers for the oral delivery of biologically active compounds. However, till now, no information about their possible specific hazards in vivo was available. The aim of this work was to assess the safety of casein nanoparticles when administered orally to animals through a 90 days dose-repeated toxicity study (OECD guideline 408), that was performed in Wistar rats under GLP conditions. After 90 days, no evidences of significant alterations in animals treated daily with 50, 150 or 500 mg/kg bw of nanoparticles were found...
June 10, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28609454/an-investigation-into-the-effects-of-excipient-particle-size-blending-techniques-and-processing-parameters-on-the-homogeneity-and-content-uniformity-of-a-blend-containing-low-dose-model-drug
#15
Hamad Alyami, Eman Dahmash, James Bowen, Afzal R Mohammed
Powder blend homogeneity is a critical attribute in formulation development of low dose and potent active pharmaceutical ingredients (API) yet a complex process with multiple contributing factors. Excipient characteristics play key role in efficient blending process and final product quality. In this work the effect of excipient type and properties, blending technique and processing time on content uniformity was investigated. Powder characteristics for three commonly used excipients (starch, pregelatinised starch and microcrystalline cellulose) were initially explored using laser diffraction particle size analyser, angle of repose for flowability, followed by thorough evaluations of surface topography employing scanning electron microscopy and interferometry...
2017: PloS One
https://www.readbyqxmd.com/read/28608238/the-impact-of-disintegrant-type-surfactant-and-api-properties-on-the-processability-and-performance-of-roller-compacted-formulations-of-acetaminophen-and-aspirin
#16
Junshu Zhao, Otilia Koo, Duohai Pan, Yongmei Wu, Dinesh Morkhade, Sandeep Rana, Partha Saha, Arturo Marin
In formulation development, certain excipients, even though used in small quantities, can have a significant impact on the processability and performance of the dosage form. In this study, three common disintegrants, croscarmellose sodium (CCS), crospovidone (xPVP), and sodium starch glycolate (SSG) as well as the surfactant sodium lauryl sulfate (SLS) were evaluated for their impact on the processability and performance of a typical dry granulation formulation. Two model compounds, the mechanically brittle and chemically inert acetaminophen and the mechanically ductile carboxylic acid aspirin, were used for the evaluation...
June 12, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28606335/atr-ftir-characterization-of-generic-brand-named-and-counterfeit-sildenafil-and-tadalafil-based-tablets-found-on-the-brazilian-market
#17
José Coelho Neto, Fernanda L C Lisboa
Viagra and Cialis are among the most counterfeited medicines in many parts of the world, including Brazil. Despite the many studies that have been made regarding discrimination between genuine and counterfeit samples, most published works do not contemplate generic and similar versions of these medicines and also do not explore excipients/adjuvants contributions when characterizing genuine and suspected samples. In this study, we present our findings in exploring ATR-FTIR spectral profiles for characterizing both genuine and questioned samples of several generic and brand-name sildenafil- and tadalafil-based tablets available on the Brazilian market, including Viagra and Cialis...
July 2017: Science & Justice: Journal of the Forensic Science Society
https://www.readbyqxmd.com/read/28600606/performance-and-tolerability-of-the-moisturizers-cetaphil-%C3%A2-and-excipial-%C3%A2-in-atopic-dermatitis-what-is-the-evidence-based-on-randomized-trials
#18
REVIEW
Esther J van Zuuren, Zbys Fedorowicz, Bernd W M Arents
INTRODUCTION: Moisturizers play a prominent role in the management of atopic dermatitis by improving the impaired skin barrier function and enhancing skin hydration. Their efficacy was evaluated in a recently published Cochrane Review 'Emollients and moisturizers for eczema'. OBJECTIVE: In the present review, we summarize the performance and safety of Cetaphil(®) and Excipial(®) moisturizing products. METHODS: This review was carried out in compliance with standard Cochrane methodological procedures, which means independent study selection, data extraction, assessment of risk of bias, and analyses by two review authors...
June 9, 2017: Dermatology and Therapy
https://www.readbyqxmd.com/read/28600185/paclitaxel-encapsulated-in-halloysite-clay-nanotubes-for-intestinal-and-intracellular-delivery
#19
R Yendluri, Y Lvov, M DeVilliers, V Vinokurov, E Naumenko, E Tarasova, R Fakhrullin
Naturally formed halloysite tubules have a length of 1 μm length and lumens with a diameter of 12-15 nm which can be loaded with drugs. Halloysite's biocompatibility allows for its safe delivering to cells at a concentration of up to 0.5 mg/mL. We encapsulated the anti-cancer drug paclitaxel in halloysite and evaluated the drug release kinetics in simulated gastric and intestinal conditions. To facilitate maximum drug release in intestinal tract, halloysite tubes were coated with the pH-responsive polymer poly(methacrylic acid-co-methyl methacrylate)...
June 6, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28596139/effects-of-cyclodextrins-on-the-chemical-stability-of-drugs
#20
Agnieszka Popielec, Thorsteinn Loftsson
Cyclodextrins (CDs) are enabling pharmaceutical excipients that can enhance both solubility and stability of wide variety of drugs in aqueous solutions through formation of drug/CD inclusion complexes where apolar moieties of the drug molecules are located inside the CD cavity. In properly designed pharmaceutical formulations CDs will improve physiochemical properties of lipophilic drugs without affecting their intrinsic ability to permeate biological membranes. Here the effect of CD complexes on the chemical stability of drugs is reviewed...
June 5, 2017: International Journal of Pharmaceutics
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