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https://www.readbyqxmd.com/read/28425971/%C3%AF-%C3%A2-cells-feature-de-ubiquitination-of-slc-transporters-and-increased-levels-and-fluxes-of-amino-acids
#1
André Bordinassi Medina, Marcin Banaszczak, Yang Ni, Ina Aretz, David Meierhofer
Solute carrier (SLC) transporters are a diverse group of membrane transporter proteins that regulate the cellular flux and distribution of endogenous and xenobiotic compounds. Post-translational modifications (PTMs), such as ubiquitination, have recently emerged as one of the major regulatory mechanisms in protein function and localization. Previously, we showed that SLC amino acid transporters were on average 6-fold de-ubiquitinated and increased amino acid levels were detected in ρ⁰ cells (lacking mitochondrial DNA, mtDNA) compared to parental cells...
April 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28415922/host-pharmacokinetics-and-drug-accumulation-of-anthelmintics-within-target-helminth-parasites-of-ruminants
#2
A Lifschitz, C Lanusse, L Alvarez
Anthelmintic drugs require effective concentrations to be attained at the site of parasite location for a certain period to assure their efficacy. The processes of absorption, distribution, metabolism and excretion (pharmacokinetic phase) directly influence drug concentrations attained at the site of action and the resultant pharmacological effect. The aim of the current review article was to provide an overview of the relationship between the pharmacokinetic features of different anthelmintic drugs, their availability in host tissues, accumulation within target helminths and resulting therapeutic efficacy...
April 17, 2017: New Zealand Veterinary Journal
https://www.readbyqxmd.com/read/28412483/effect-of-micro-environment-modification-and-polymer-type-on-the-in-vitro-dissolution-behavior-and-in-vivo-performance-of-amorphous-solid-dispersions
#3
Weiwei Sun, Baoliang Pan
This study investigates the effects of micro-environment modification and polymer type on the in-vitro dissolution behavior and in-vivo performance of micro-environment pH modifying solid dispersions (pHM-SD) for the poorly water-soluble model drug Toltrazuril (TOL). Various pHM-SDs were prepared using Ca(OH)2 as a pH-modifier in hydrophilic polymers, including polyethylene glycol 6000 (PEG6000), polyvinylpyrrolidone k30 (PVPk30) and hydroxypropyl methylcellulose (HPMC). Based on the results of physicochemical characterizations and in-vitro dissolution testing, the representative ternary (Ca(OH)2:TOL:PEG6000/HPMC/PVPk30=1:8:24, w/w/w) and binary (TOL:PVPk30=1:3, w/w) solid dispersions were selected and optimized to perform in-vivo pharmacokinetic study...
April 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28412404/development-of-human-biotransformation-qsars-and-application-for-pbt-assessment-refinement
#4
Ester Papa, Alessandro Sangion, Jon A Arnot, Paola Gramatica
Toxicokinetics heavily influence chemical toxicity as the result of Absorption, Distribution, Metabolism (Biotransformation) and Elimination (ADME) processes. Biotransformation (metabolism) reactions can lead to detoxification or, in some cases, bioactivation of parent compounds to more toxic chemicals. Moreover, biotransformation has been recognized as a key process determining chemical half-life in an organism and is thus a key determinant for bioaccumulation assessment for many chemicals. This study addresses the development of QSAR models for the prediction of in vivo whole body human biotransformation (metabolism) half-lives measured or empirically-derived for over 1000 chemicals, mainly represented by pharmaceuticals...
April 13, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28408188/investigation-and-risk-evaluation-of-the-occurrence-of-carbamazepine-oxcarbazepine-their-human-metabolites-and-transformation-products-in-the-urban-water-cycle
#5
Elena Brezina, Carsten Prasse, Johannes Meyer, Harald Mückter, Thomas A Ternes
Trace organic contaminants such as pharmaceuticals, personal care products and industrial chemicals are frequently detected in the urban water cycle, including wastewater, surface water and groundwater, as well as drinking water. These also include human metabolites (HMs), which are formed in the human body and then excreted via urine or feces, as well as transformation products (TPs) formed in engineered treatment systems and the aquatic environment. In the current study, the occurrence of HMs as well as their TPs of the anticonvulsants carbamazepine (CBZ) and oxcarbazepine (OXC) were investigated using LC tandem MS in effluents of wastewater treatment plants (WWTPs), surface water and groundwater...
April 10, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28405577/a-comprehensive-physicochemical-thermal-and-spectroscopic-characterization-of-zinc-ii-chloride-using-x-ray-diffraction-particle-size-distribution-differential-scanning-calorimetry-thermogravimetric-analysis-differential-thermogravimetric-analysis-ultraviolet
#6
Mahendra Kumar Trivedi, Kalyan Kumar Sethi, Parthasarathi Panda, Snehasis Jana
OBJECTIVE: Zinc chloride is an important inorganic compound used as a source of zinc and has other numerous industrial applications. Unfortunately, it lacks reliable and accurate physicochemical, thermal, and spectral characterization information altogether. Hence, the authors tried to explore in-depth characterization of zinc chloride using the modern analytical technique. MATERIALS AND METHODS: The analysis of zinc chloride was performed using powder X-ray diffraction (PXRD), particle size distribution, differential scanning calorimetry (DSC), thermogravimetric analysis/differential thermogravimetric analysis (TGA/DTG), ultraviolet-visible spectroscopy (UV-vis), and Fourier transform-infrared (FT-IR) analytical techniques...
January 2017: International Journal of Pharmaceutical Investigation
https://www.readbyqxmd.com/read/28403898/health-risks-associated-with-the-pharmaceuticals-in-wastewater
#7
EDITORIAL
Nasser Nassiri Koopaei, Mohammad Abdollahi
The overwhelming population growth in recent decades and water crisis along with limited and uneven geographical distribution of fresh water resources is a growing challenge for the economic and human development. Wastewater reclamation and use could be an alternative for intact water sources and a promising solution to water scarcity and unequal distribution. However, wastewater is a double-edged resource both as an accessible water source for food production and human usage and concurrently may carry uncharacterized content with unknown toxicological profile causing acute or long-term health risks...
April 12, 2017: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
https://www.readbyqxmd.com/read/28402570/prescription-opioid-access-patterns-and-factors-associated-with-increasing-number-of-prescribers-pharmacies-and-dispensings-an-observational-study-using-pharmaceutical-claims
#8
Bianca Blanch, Louisa Degenhardt, Nicholas A Buckley, Natasa Gisev, Timothy Dobbins, Emily A Karanges, Briony Larance, Sarah Larney, Sallie-Anne Pearson
Objective. : To examine associations between patient factors and increasing opioid access measured by three metrics: number of unique prescribers, pharmacies, and dispensings in 12 months. Methods. : We used pharmaceutical claims for a random 10% sample of Australians age 18 years or older initiating or reinitiating strong opioid treatment (≥90 days of no strong opioid dispensing) between July 2010 and December 2012. We report the distribution of opioid access by metric...
April 10, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28402142/development-of-separation-technology-for-the-removal-of-radium-223-from-targeted-thorium-conjugate-formulations-part-ii-purification-of-targeted-thorium-conjugates-on-cation-exchange-columns
#9
Janne Olsen Frenvik, Knut Dyrstad, Solveig Kristensen, Olav B Ryan
Tumour targeting pharmaceuticals will play a crucial role in future pharma pipelines. The Targeted Thorium Conjugate (TTC) therapeutic platform could provide real benefit to patients, whereby targeting moieties like monoclonal antibodies are radiolabelled with the alpha-emitting radionuclide thorium-227 ((227)Th, t1/2=18.7 days). A potential problem could be the accumulation of the long-lived daughter nuclide radium-223 ((223)Ra, t1/2=11.4 days) in the drug product during manufacture and distribution. Therefore, the level of (223)Ra must be standardised before administration to the patient...
April 12, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28398095/influence-of-drug-load-on-dissolution-behavior-of-tablets-containing-a-poorly-water-soluble-drug-estimation-of-the-percolation-threshold
#10
Tim Wenzel, Cordula Stillhart, Peter Kleinebudde, Anikó Szepes
Drug load plays an important role in the development of solid dosage forms, since it can significantly influence both processability and final product properties. The percolation threshold of the active pharmaceutical ingredient (API) corresponds to a critical concentration, above which an abrupt change in drug product characteristics can occur. The objective of this study was to identify the percolation threshold of a poorly water-soluble drug with regard to the dissolution behavior from immediate release tablets...
April 19, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28396636/enhancing-drug-efficacy-and-therapeutic-index-through-cheminformatics-based-selection-of-small-molecule-binary-weapons-that-improve-transporter-mediated-targeting-a-cytotoxicity-system-based-on-gemcitabine
#11
Justine M Grixti, Steve O'Hagan, Philip J Day, Douglas B Kell
The transport of drug molecules is mainly determined by the distribution of influx and efflux transporters for which they are substrates. To enable tissue targeting, we sought to develop the idea that we might affect the transporter-mediated disposition of small-molecule drugs via the addition of a second small molecule that of itself had no inhibitory pharmacological effect but that influenced the expression of transporters for the primary drug. We refer to this as a "binary weapon" strategy. The experimental system tested the ability of a molecule that on its own had no cytotoxic effect to increase the toxicity of the nucleoside analog gemcitabine to Panc1 pancreatic cancer cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28395830/sweet-cherries-from-fund%C3%A3-o-possess-antidiabetic-potential-and-protect-human-erythrocytes-against-oxidative-damage
#12
Ana C Gonçalves, Catarina Bento, Branca M Silva, Luís R Silva
Cherries are one of the most appreciated summer fruits due to their attractive colour, sweet taste, high water content, low level of calories and composition in bioactive compounds which, in turn, are important to prevent some pathologies like diabetes, cardiovascular diseases and cancer. In this work we evaluated the phenolic profile and biological potential of 5 varieties of sweet cherries from Fundão region (Portugal) (Saco, Sweetheart, Satin, Maring and Hedelfinger). A total of 23 phenolic compounds were identified by LC-DAD and distributed by the several classes: 6 anthocyanins, 1 hydroxybenzoic acid, 8 hydroxycinnamic acids, 3 flavan-3-ols and 5 flavonols...
May 2017: Food Research International
https://www.readbyqxmd.com/read/28392910/drug-shortages-in-israel-regulatory-perspectives-challenges-and-solutions
#13
Eyal Schwartzberg, Denize Ainbinder, Alla Vishkauzan, Ronni Gamzu
BACKGROUND: Pharmaceutical drug shortages (DSs) are a global problem which presents challenges to countries around the world. Shortages of pharmaceutical products may have a direct detrimental impact on public health and patients' wellbeing by causing delayed, or even lack of, treatment. Moreover, DSs may force both patients and caregivers to use unfamiliar drugs, which could lead to medication errors. The objective of our study was to analyze DSs in Israel during the years 2013-2015, assessing their etiology and exploring the steps taken for their mitigation and prevention...
2017: Israel Journal of Health Policy Research
https://www.readbyqxmd.com/read/28392414/micro-flow-imaging-as-a-quantitative-tool-to-assess-size-and-agglomeration-of-plga-microparticles
#14
Miranda M C van Beers, Cees Slooten, Jelte Meulenaar, Ahmad S Sediq, Ruud Verrijk, Wim Jiskoot
The purpose of this study was to explore the potential of flow imaging microscopy to measure particle size and agglomeration of poly(D,L-lactic-co-glycolic acid) (PLGA) microparticles. The particle size distribution of pharmaceutical PLGA microparticle products is routinely determined with laser diffraction. In our study, we performed a unique side-by-side comparison between MFI 5100 (flow imaging microscopy) and Mastersizer 2000 (laser diffraction) for the particle size analysis of two commercial PLGA microparticle products, i...
April 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28392011/rationing-hepatitis-c-treatment-in-the-context-of-austerity-policies-in-france-and-cameroon-a-transnational-perspective-on-the-pharmaceuticalization-of-healthcare-systems
#15
Fanny Chabrol, Pierre-Marie David, Gaëlle Krikorian
New powerful drugs against hepatitis C can cure the disease, but they are not widely distributed because their exorbitant prices are destabilizing healthcare systems in both African and European countries. This article takes access to hepatitis C treatments since 2013 in France and in Cameroon as a lens to analyze the rationing of pharmaceutical treatments in relation to recent transformations of health systems. Access to these treatments is analyzed thanks to ethnographic observation and interviews lead in Paris and Yaoundé, with patients, associations, health professionals and public health experts...
March 28, 2017: Social Science & Medicine
https://www.readbyqxmd.com/read/28388648/trends-in-medicines-procurement-by-the-brazilian-federal-government-from-2006-to-2013
#16
Tatiana Chama Borges Luz, Claudia Garcia Serpa Osorio-de-Castro, Rachel Magarinos-Torres, Bjorn Wettermark
The costs of medicines pose a growing burden on healthcare systems worldwide. A comprehensive understanding of current procurement processes provides strong support for the development of effective policies. This study examined Brazilian Federal Government pharmaceutical procurement data provided by the Integrated System for the Administration of General Services (SIASG) database, from 2006 to 2013. Medicine purchases were aggregated by volume and expenditure for each year. Data on expenditure were adjusted for inflation using the Extended National Consumer Price Index (IPCA) for December 31, 2013...
2017: PloS One
https://www.readbyqxmd.com/read/28385248/ultrasound-assisted-extraction-and-structural-characterization-by-nmr-of-alginates-and-carrageenans-from-seaweeds
#17
Latufa Youssouf, Laura Lallemand, Pierre Giraud, Faiza Soulé, Archana Bhaw-Luximon, Olivier Meilhac, Christian Lefèbvre D'Hellencourt, Dhanjay Jhurry, Joël Couprie
Polysaccharides from seaweeds are interesting materials for food and pharmaceutical applications such as drug delivery due to their biocompatibility and biodegradability. Extraction of these biopolymers is usually performed during several hours to obtain a significant extraction yield. In this paper, we report on a new process to extract alginates from brown seaweeds (Sargassum binderi and Turbinaria ornata) and carrageenans from red seaweeds (Kappaphycus alvarezii and Euchema denticulatum) with the assistance of ultrasound...
June 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28380390/dropwise-additive-manufacturing-of-pharmaceutical-products-for-amorphous-and-self-emulsifying-drug-delivery-systems
#18
Elçin Içten, Hitesh S Purohit, Chelsey Wallace, Arun Giridhar, Lynne S Taylor, Zoltan K Nagy, Gintaras V Reklaitis
The improvements in healthcare systems and the advent of the precision medicine initiative have created the need to develop more innovative manufacturing methods for the delivery and production of individualized dosing and personalized treatments. In accordance with the changes observed in healthcare systems towards more innovative therapies, this paper presents dropwise additive manufacturing of pharmaceutical products (DAMPP) for small scale, distributed manufacturing of individualized dosing as an alternative to conventional manufacturing methods A dropwise additive manufacturing process for amorphous and self-emulsifying drug delivery systems is reported, which utilizes drop-on-demand printing technology for automated and controlled deposition of melt-based formulations onto inert tablets...
April 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28376825/antiretroviral-therapy-supply-chain-quality-control-and-assurance-in-improving-people-living-with-hiv-therapeutic-outcomes-in-cameroon
#19
M P Ngogang Djobet, David Singhe, Julienne Lohoue, Christopher Kuaban, Jeanne Ngogang, Ernest Tambo
BACKGROUND: Evaluation of medication efficacy and safety is an essential guarantee to successful therapeutic outcome in public health practices. However, larger distribution chain supply in developing countries such as Cameroon is often challenged by counterfeit drugs, poor manufacturing, storage and degradation leading to health and patient adverse consequences. Yet, access to supply chain management in strengthening ARVs quality assurance and outcomes remains poorly documented. More than 53,000 patients have been enrolled on free ARVs medications, but little is documented on quality assurance and validity of safety for affected populations along the supply chain management since 2008...
April 4, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28371770/occurrence-of-antibiotic-resistance-genes-and-mobile-genetic-elements-in-enterococci-and-genomic-dna-during-anaerobic-digestion-of-pharmaceutical-waste-sludge-with-different-pretreatments
#20
Juan Tong, XueTing Lu, JunYa Zhang, Qianwen Sui, Rui Wang, Meixue Chen, Yuansong Wei
Pharmaceutical waste sludge harbors large amounts of antibiotic resistance genes (ARGs) and mobile genetic elements (MGEs), and it is necessary to study the reduction of ARGs and MGEs during sludge treatment. Therefore, the antibiotic resistance phenotypes and genotypes of enterococci, and the ARGs and MGEs in genomic DNA were investigated during anaerobic digestion (AD) with microwave (MW), thermal hydrolysis (TH) and ozone pretreatment. Results showed that sludge pretreatment increased the occurrence of the resistance phenotypes and genotypes of enterococci...
March 22, 2017: Bioresource Technology
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