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https://www.readbyqxmd.com/read/28108974/design-and-evaluation-of-topical-diclofenac-sodium-gel-using-hot-melt-extrusion-technology-as-a-continuous-manufacturing-process-with-kolliphor%C3%A2-p407
#1
Jaywant Pawar, Rajkiran Narkhede, Purnima Amin, Vaishali Tawde
The aim of the present context was to develop and evaluate a Kolliphor® P407-based transdermal gel formulation of diclofenac sodium by hot melt extrusion (HME) technology; central composite design was used to optimize the formulation process. In this study, we have explored first time ever HME as an industrially feasible and continuous manufacturing technology for the manufacturing of gel formulation using Kolliphor® P407 and Kollisolv® PEG400 as a gel base. Diclofenac sodium was used as a model drug. The HME parameters such as feeding rate, screw speed, and barrel temperature were crucial for the semisolid product development, and were optimized after preliminary trials...
January 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28108094/metabolic-profiling-identification-of-metabolites-formed-in-mediterranean-mussels-mytilus-galloprovincialis-after-diclofenac-exposure
#2
Bénilde Bonnefille, Lauren Arpin-Pont, Elena Gomez, Hélène Fenet, Frédérique Courant
Despite the growing concern on the presence of pharmaceutically active compounds in the environment, few studies have been conducted on their metabolism in marine organisms. In this study, a non-targeted strategy based on the generation of chemical profiles generated by liquid chromatography combined with high resolution mass spectrometry was used to highlight metabolite production by the Mediterranean mussel (Mytilus galloprovincialis) after diclofenac exposure. This method allowed revealing the production of 13 metabolites in mussel tissues...
January 17, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28107994/application-of-passive-sampling-devices-based-on-multi-walled-carbon-nanotubes-for-the-isolation-of-selected-pharmaceuticals-and-phenolic-compounds-in-water-samples-possibilities-and-limitations
#3
Aleksandra Jakubus, Magdalena Tyma, Piotr Stepnowski, Monika Paszkiewicz
Nowadays, carbon nanotubes, as commercially available materials, have attracted great attention because of their unique physicochemical properties, especially their strong adsorption abilities. This paper deals with the possibilities and limitations of the application of multi-walled carbon nanotubes as an alternative sorbent in passive sampling devices for the isolation of selected pharmaceuticals and phenolic compounds directly in water samples. Compounds with different properties, including sulfapyridine, sulfamethoxazole, carbamazepine, p-nitrophenol, 17-β-estradiol, 3,5-dichlorophenol and diclofenac were selected as model compounds...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28107717/diclofenac-can-exhibit-estrogenic-modes-of-action-in-male-xenopus-laevis-and-affects-the-hypothalamus-pituitary-gonad-axis-and-mating-vocalizations
#4
Norah Johanna Efosa, Wibke Kleiner, Werner Kloas, Frauke Hoffmann
Diclofenac (DCF) is a non-steroidal analgesic and antiphlogistic. Due to its tremendous use, DCF can be found in the environment, especially in sewage, but also surface waters, ground and drinking water. Previous studies indicated that DCF can modulate the reproductive physiology of fish by altering the expression of important key enzymes of the hypothalamus-pituitary-gonad-axis (HPG-axis) and might act as an estrogenic endocrine disrupting chemical (EDC). Other studies, however, demonstrated that DCF does not exhibit any estrogenicity...
January 6, 2017: Chemosphere
https://www.readbyqxmd.com/read/28107631/overcoming-the-heat-endurance-of-tumor-cells-by-interfering-the-anaerobic-glycolysis-metabolism-for-improved-photothermal-therapy
#5
Wei-Hai Chen, Guo-Feng Luo, Qi Lei, Sheng Hong, Wen-Xiu Qiu, Li-Han Liu, Si-Xue Cheng, Xian-Zheng Zhang
In this study, we developed a general method to decorate plasmonic gold nanorods (GNRs) with a CD44-targeting functional polymer, containing hyaluronic acid (HA) targeting moiety and a small molecule Glut1 inhibitor of diclofenac (DC), to obtain GNR/HA-DC. This nanosystem exhibited the superiority of selectively sensitizing tumor cells for photothermal therapy (PTT) by inhibiting the unique anaerobic glycolysis. Upon specifically targeting CD44, sequentially time-dependent DC release could be achieved by the trigger of hyaluronidase (HAase), which abundantly existed in tumor tissue...
January 20, 2017: ACS Nano
https://www.readbyqxmd.com/read/28106668/primidone-inhibits-trpm3-and-attenuates-thermal-nociception-in-vivo
#6
Ute Krügel, Isabelle Straub, Holger Beckmann, Michael Schaefer
The melastatin-related transient receptor potential channel TRPM3 is a nonselective cation channel expressed in nociceptive neurons and activated by heat. Since TRPM3-deficient mice show inflammatory thermal hyperalgesia, pharmacological inhibition of TRPM3 may exert antinociceptive properties. Fluorometric Ca influx assays and a compound library containing approved or clinically tested drugs were used to identify TRPM3 inhibitors. Biophysical properties of channel inhibition were assessed using electrophysiological methods...
January 12, 2017: Pain
https://www.readbyqxmd.com/read/28106285/inhibition-of-immune-responses-and-related-proteins-in-rhamdia-quelen-exposed-to-diclofenac
#7
João L C Ribas, James P Sherry, Aleksander R Zampronio, Helena C Silva de Assis, Denina B D Simmons
Non-steroidal anti-inflammatory drugs (NSAIDs) are among the most widely detected pharmaceuticals in surface water worldwide. The NSAID diclofenac is used to treat many types of pain and inflammation. Diclofenac's potential to cause adverse effects in exposed wildlife is a growing concern. To evaluate the effects of waterborne diclofenac on the immune response in Rhamdia quelen (South American Catfish), fish were exposed to three concentrations of diclofenac (0.2, 2.0, and 20.0 µg/L) for 14 days. Some of the exposed fish were also given an intraperitoneal injection on day 14 of 1 mg/kg of carrageenan to evaluate cell migration to the peritoneum...
January 20, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28102676/novel-antitumor-platinum-ii-conjugates-containing-the-nonsteroidal-anti-inflammatory-agent-diclofenac-synthesis-and-dual-mechanisms-of-antiproliferative-effects
#8
Francesco Paolo Intini, Juraj Zajac, Vojtech Novohradsky, Teresa Saltarella, Concetta Pacifico, Viktor Brabec, Giovanni Natile, Jana Kasparkova
One concept how to improve anticancer effects of conventional metallodrugs consists in conjugation of these compounds with other biologically (antitumor) active agents, acting by a different mechanism. Here, we present synthesis, biological effects, and mechanisms of action of new Pt(II) derivatives containing one or two nonsteroidal anti-inflammatory diclofenac (DCF) ligands also known for their antitumor effects. The antiproliferative properties of these metallic conjugates show that these compounds are potent and cancer cell selective cytotoxic agents exhibiting activity in cisplatin resistant and the COX-2 positive tumor cell lines...
January 19, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28102013/the-effect-of-potassium-diclofenac-and-dexamethasone-on-mmp-1-gene-transcript-levels-during-experimental-tooth-movement-in-rats
#9
G P Molina Da Silva, O M Tanaka, D F Campos Navarro, C E Repeke, G P Garlet, O Guariza-Filho, P C Trevilatto
OBJECTIVES: The aim of this study was to analyze MMP-1 transcript levels in periodontal tissues of rats that underwent orthodontic treatment using potassium diclofenac and dexamethasone at different stages of tooth movement. SETTING AND SAMPLE POPULATION: The sample comprised of ninety male Wistar rats. MATERIAL AND METHODS: A closed nickel-titanium coil spring was used to apply a force of 50 cN to move the maxillary right first molars mesially...
February 2017: Orthodontics & Craniofacial Research
https://www.readbyqxmd.com/read/28101901/cyto-genotoxicity-and-oxidative-stress-in-common-carp-cyprinus-carpio-exposed-to-a-mixture-of-ibuprofen-and-diclofenac
#10
Hariz Islas-Flores, Leobardo Manuel Gómez-Oliván, Marcela Galar-Martínez, Esmeralda Michelle Sánchez-Ocampo, Nely SanJuan-Reyes, Mariana Ortíz-Reynoso, Octavio Dublán-García
Thirty million people worldwide consume each day nonsteroidal anti-inflammatory drugs (NSAIDs), a heterogeneous group of pharmaceuticals used for its analgesic, antipyretic, and anti-inflammatory properties. Recent studies report high NSAID concentrations in wastewater treatment plant effluents, in surface, ground, and drinking water, and in sediments. NSAIDs are also known to induce toxicity on aquatic organisms. However, toxicity in natural ecosystems is not usually the result of exposure to a single substance but to a mixture of toxic agents, yet only a few studies have evaluated the toxicity of mixtures...
January 19, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28101466/characterization-of-the-effect-of-drug-drug-interaction-on-protein-binding-in-concurrent-administration-of-sulfamethoxazol-and-diclofenac-sodium-using-bovine-serum-albumin
#11
Md Kamal Hossain, Amina Khatun, Mahmudur Rahman, Md Nahid Akter, Sadia Afreen Chowdhury, Sm Mahbubul Alam
Purpose: This project was aimed to determine the effect of concurrent administration of sulfamethoxazole and diclofenac sodium. Methods: Equilibrium dialysis method was adopted to study different protein binding aspects of sulfamethoxazole and diclofenac sodium. Results: Sulfamethoxazole showed two types of association constants; high affinity constant 29.0±0.20×10(6) M(-1) with lower number of binding sites of 0.7±1 and low affinity constant 1.13±0.20×10(6) M(-1) with higher number of binding sites of 3...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28098428/the-self-sufficient-p450-rhf-expressed-in-a-whole-cell-system-selectively-catalyses-the-5-hydroxylation-of-diclofenac
#12
Jan M Klenk, Bernd A Nebel, Joanne L Porter, Justyna K Kulig, Shaneela A Hussain, Sven M Richter, Michele Tavanti, Nicholas J Turner, Martin A Hayes, Bernhard Hauer, Sabine L Flitsch
P450 monooxygenases are able to catalyse the highly regio- and stereoselective oxidations of many organic molecules. However, the scale-up of such bio-oxidations remains challenging due to the often-low activity, level of expression and stability of P450 biocatalysts. Despite these challenges they are increasingly desirable as recombinant biocatalysts, particularly for the production of drug metabolites. Diclofenac is a widely used anti-inflammatory drug that is persistent in the environment along with the 4'- and 5-hydroxy metabolites...
January 18, 2017: Biotechnology Journal
https://www.readbyqxmd.com/read/28098264/assessment-of-coulometric-array-electrochemical-detection-coupled-with-hplc-uv-for-the-absolute-quantitation-of-pharmaceuticals
#13
Michael B Hicks, Leah Salituro, Ian Mangion, Wes Schafer, Rong Xiang, Xiaoyi Gong, Christopher J Welch
The use of a coulometric array detector in tandem with HPLC-UV was evaluated for the absolute quantitation of pharmaceutical compounds without standards, an important capability gap in contemporary pharmaceutical research and development. The high-efficiency LC flow-through electrochemical detector system allows for the rapid evaluation of up to 16 different potentials, aiding in the identification and quantitation of electrochemically reactive species. By quantifying the number of electrons added or removed from an analyte during its passage through the detector, the number of moles of the analyte can be established...
January 18, 2017: Analyst
https://www.readbyqxmd.com/read/28097758/alpha-blockers-in-the-management-of-ureteric-lithiasis-a-meta-analysis
#14
Nicholas Raison, Kamran Ahmed, Oliver Brunckhorst, Prokar Dasgupta
INTRODUCTION: Effective medical expulsion for ureteric stones with α-blockers offers numerous advantages over surgical alternatives. However, its effectiveness remains uncertain and with the publication of new trial data, the available evidence requires reappraisal. OBJECTIVE: The aim of this study was to assess the efficacy of α-blockers the management of ureteric lithiasis. METHODS: A systematic review of the literature, with predefined search criteria, was conducted using PubMed and Embase...
January 2017: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/28096583/addition-of-clonidine-to-bupivacaine-in-transversus-abdominis-plane-block-prolongs-postoperative-analgesia-after-cesarean-section
#15
Ranju Singh, Nishant Kumar, Aruna Jain, Sudipta Joy
BACKGROUND AND AIMS: The aim was to compare duration of postoperative analgesia with addition of clonidine to bupivacaine in bilateral transversus abdominis plane (TAP) block after lower segment cesarean section (LSCS). MATERIAL AND METHODS: One hundred American Society of Anesthesiologists (ASA) grade I and II pregnant patients undergoing LSCS under spinal anesthesia were randomly divided to receive either 20 ml bupivacaine 0.25% (Group B; n = 50) or 20 ml bupivacaine+1ug/kg clonidine bilaterally (Group BC; n = 50) in TAP block in a double-blind fashion...
October 2016: Journal of Anaesthesiology, Clinical Pharmacology
https://www.readbyqxmd.com/read/28096578/the-effect-of-pregabalin-and-s-ketamine-in-total-knee-arthroplasty-patients-a-randomized-trial
#16
Lajla Kadic, Frank G van Haren, Oliver Wilder-Smith, Jorgen Bruhn, Jacques J Driessen, Maarten C de Waal Malefijt
BACKGROUND AND AIMS: Pain reduction is important for rehabilitation after total knee arthroplasty. Intra- and peri-articular infiltration with local anesthetics may be an alternative to commonly used locoregional techniques. Adding pregabalin orally and s-ketamine intravenously may further reduce postoperative pain. MATERIAL AND METHODS: This prospective, randomized, double-blind, placebo-controlled study compared two methods of perioperative analgesia. Control patients received a standardized multimodal postoperative analgesic regime of paracetamol, diclofenac, and piritramide-patient-controlled analgesia, including ropivacaine knee infiltration during surgery...
October 2016: Journal of Anaesthesiology, Clinical Pharmacology
https://www.readbyqxmd.com/read/28095993/evaluation-of-the-short-term-fate-and-transport-of-chemicals-of-emerging-concern-during-soil-aquifer-treatment-using-select-transformation-products-as-intrinsic-redox-sensitive-tracers
#17
Meriam Muntau, Manoj Schulz, Kevin S Jewell, Nina Hermes, Uwe Hübner, Thomas Ternes, Jörg E Drewes
In this study, known products from oxic transformation of the X-ray contrast medium iopromide were introduced for the first time as intrinsic tracer for in situ characterization of the transition zone between oxic and suboxic conditions during the initial phase of soil-aquifer treatment (SAT). Two wet-dry cycles of a full-scale infiltration basin were monitored to characterize hydraulic retention times, redox conditions, removal of bulk organic parameters and the fate of chemicals of emerging concern (CECs)...
January 14, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28092840/suppressive-effect-of-spirulina-fusiformis-on-diclofenac-induced-hepato-renal-injury-and-gastrointestinal-ulcer-in-wistar-albino-rats-a-biochemical-and-histological-approach
#18
Jerine Peter S, Kadar Basha S, R Giridharan, Udhaya Lavinya B, Evan Prince Sabina
CONTEXT: The non-steroidal anti-inflammatory drug (NSAID), diclofenac causes hepato-renal toxicity and gastric ulcer. The aim of this study was to investigate the protective effect of Spirulina fusiformis on Diclofenac-induced toxicity in Wistar albino rats. METHODS: Rats were treated as follows: normal control (group I); diclofenac (50mg/kgb.w., i.p.) treated rats (group II); diclofenac-induced (50mg/kgb.w., i.p.) rats treated with Spirulina fusiformis (400mg/kgb...
January 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28091717/bar-adsorptive-microextraction-technique-application-for-the-determination-of-pharmaceuticals-in-real-matrices
#19
Carlos Almeida, Samir M Ahmad, José Manuel F Nogueira
In the present work, bar adsorptive microextraction using miniaturized devices (7.5 × 3.0 mm) coated with suitable sorbent phases, combined with microliquid desorption (100 μL) followed by high-performance liquid chromatography with diode array detection (BAμE-μLD/HPLC-DAD), is proposed for the determination of trace level of six pharmaceuticals (furosemide, mebeverine, ketoprofen, naproxen, diclofenac and mefenamic acid) in environmental water and urine matrices. By comparing ten distinct sorbent materials (five polymeric and five activated carbons), the polymer P5 proved to be the most suitable to achieve the best selectivity and efficiency...
January 16, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28079297/the-effectiveness-of-diclofenac-sodium-in-the-treatment-of-mondor-s-disease-of-the-breast-the-topical-patch-compared-to-the-oral-capsules
#20
Bader Hamza Shirah, Hamza Assad Shirah, Wedad Salem Alonazie
Mondor's disease of the breast is a rare, benign sclerosing superficial thrombophlebitis of the subcutaneous veins of the anterior or lateral chest wall, which is treated conservatively. We aim in this study to evaluate the outcome and effectiveness of our treatment protocol using oral diclofenac sodium and topical diclofenac sodium patch in 172 patients. A retrospective database analysis of 172 female patients between January 2001 and December 2010 was done. The treatment protocol consisted of group 1: treatment by oral diclofenac sodium 100 mg once daily for 3 weeks...
January 12, 2017: Breast Journal
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