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Etodolac

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https://www.readbyqxmd.com/read/27687548/nsaids-diclofenac-indomethacin-and-meloxicam-highly-upregulate-expression-of-icam-1-and-cox-2-induced-by-x-irradiation-in-human-endothelial-cells
#1
Yoshihiko Uehara, Yasuhiko Murata, Soichiro Shiga, Yoshio Hosoi
BACKGROUND: It is well known that radiation exposure to the heart and the use of non-steroidal anti-inflammatory drugs (NSAIDs) increase the risk of myocardial infarction (MI). Some NSAIDs are also known to act synergistically with ionizing radiation and have radio-sensitizing effects in radiotherapy. These evidences suggest that NSAIDs may affect the risk of MI after radiation exposure to the heart. In the present study, we investigated effects of NSAIDs on radiation-induced expression of cell adhesion molecules and COX-2, which are associated with inflammation and an increased risk of MI, in human endothelial cells...
October 28, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27593184/self-assembling-organogels-based-on-pluronic-and-lethicin-for-sustained-release-of-etodolac-in-vitro-and-in-vivo-correlation
#2
Ahmed M Mohammed, W Faisal, Khaled I Saleh, Shaaban K Osman
Etodolac, a member of non steroidal anti-inflammatory drugs (NSAIDs), has a poor aqueous solubility. Long term administration of etodolac causes severe gastrointestinal disturbances such as peptic ulcer and bleeding. These disturbances could be overcome by alternative routes such as a topical administration. In the present study, pluronic lecithin organogels (PLOs) were prepared by simple mixing of pluronic solution with lecithin solution. Etodolac was loaded into the prepared gels or added during the gel formation...
September 2, 2016: Current Drug Delivery
https://www.readbyqxmd.com/read/27578406/interactions-of-helquats-with-chiral-acidic-aromatic-analytes-investigated-by-partial-filling-affinity-capillary-electrophoresis
#3
Martin Růžička, Dušan Koval, Jan Vávra, Paul E Reyes-Gutiérrez, Filip Teplý, Václav Kašička
Noncovalent molecular interactions between helquats, a new class of dicationic helical extended diquats, and several chiral acidic aromatic drugs and catalysts have been investigated using partial-filling affinity capillary electrophoresis (PF-ACE). Helquats dissolved at 1mM concentration in the aqueous background electrolyte (40mM Tris, 20mM acetic acid, pH 8.1) were introduced as ligand zones of variable length (0-130mm) into the hydroxypropylcellulose coated fused silica capillary whereas 0.1mM solutions of negatively charged chiral drugs or catalysts (warfarin, ibuprofen, mandelic acid, etodolac, binaphthyl phosphate and 11 other acidic aromatic compounds) were applied as a short analyte zone at the injection capillary end...
October 7, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/27480443/development-and-characterization-of-multifunctional-directly-compressible-co-processed-excipient-by-spray-drying-method
#4
Sohil I Chauhan, Sandeep V Nathwani, Moinuddin M Soniwala, Jayant R Chavda
The present investigation was carried out to develop and characterize a multifunctional co-processed excipient for improving the compressibility of poorly compressible drugs. Etodolac was used as a model drug. Microcrystalline cellulose (MCC), lactose monohydrate (lactose), and StarCap 1500 (StarCap) were selected as components of the co-processed excipient. The spray drying method was used for co-processing of excipients. D-optimal mixture design was applied to optimize the proportion of component excipients...
August 1, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27478643/etodolac-containing-topical-niosomal-gel-formulation-development-and-evaluation
#5
Gyati Shilakari Asthana, Abhay Asthana, Davinder Singh, Parveen Kumar Sharma
The present study aimed to investigate the delivery potential of Etodolac (ETD) containing topical niosomal gel. Niosomal formulations were prepared by thin film hydration method at various ratios of cholesterol and Span 60 and were evaluated with respect to particle size, shape, entrapment efficiency, and in vitro characteristics. Dicetyl phosphate (DCP) was also added in the niosomal formulation. Mean particle size of niosomal formulation was found to be in the range of 2 μm to 4 μm. Niosomal formulation N2 (1 : 1) ratio of cholesterol and surfactant displayed good entrapment efficiency (96...
2016: Journal of Drug Delivery
https://www.readbyqxmd.com/read/27253735/-missing-tooth-multidomain-peptide-nanofibers-for-delivery-of-small-molecule-drugs
#6
I-Che Li, Amanda N Moore, Jeffrey D Hartgerink
The clinical administration of many small molecule hydrophobic drugs is challenged by the insolubility of these drugs under physiological conditions. Because of this, the development of biocompatible scaffolds capable of effectively delivering hydrophobic drug molecules is of particular interest. Multidomain peptides (MDPs) provide biocompatible hydrogel scaffolds that are injectable and space-conforming, allowing for in situ delivery of a variety of drugs. Here we demonstrate that through manipulation of peptide primary sequence, a molecular cavity can be incorporated into the hydrophobic core of these peptide nanofibers allowing for encapsulation and delivery of small molecule drugs with poor water solubility...
June 13, 2016: Biomacromolecules
https://www.readbyqxmd.com/read/27235931/reducing-liver-metastases-of-colon-cancer-in-the-context-of-extensive-and-minor-surgeries-through-%C3%AE-adrenoceptors-blockade-and-cox2-inhibition
#7
Liat Sorski, Rivka Melamed, Pini Matzner, Hagar Lavon, Lee Shaashua, Ella Rosenne, Shamgar Ben-Eliyahu
Liver metastases are a major cause of colorectal cancer death, and the perioperative period is believed to critically affect the metastatic process. Here we tested whether blocking excess release of catecholamines and prostaglandins during surgical procedures of different extent can reduce experimental liver metastasis of the syngeneic CT26 colon cancer in female and male BALB/c mice. Animals were either treated with the beta-blocker, propranolol, the COX-2 inhibitor, etodolac, both drugs, or vehicle. The role of NK cells in controlling CT26 hepatic metastasis and in mediating the effect of the drugs was assessed by in vivo depletion or stimulation of NK cells, using anti-asialo GM1 or CpG-C, respectively...
May 25, 2016: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/27160363/comparative-assessment-of-the-effect-of-ibuprofen-and-etodolac-on-edema-trismus-and-pain-in-lower-third-molar-surgery-a-randomized-clinical-trial
#8
Júlio César Silva de Oliveira, Gustavo Augusto Grossi de Oliveira, Ana Paula Farnezi Bassi
PURPOSE: To compare the efficacy of ibuprofen (IBU) and etodolac (ETO) for controlling pain, edema, and trismus after extraction of lower third molars. MATERIALS AND METHODS: Twenty adolescents and adults with 2 impacted mandibular-third molars (in similar positions) were selected for the study. Patients were randomly assigned either to the IBU group (600 mg of IBU 3 times a day for 3 days) or to the ETO group (300 mg of ETO 3 times a day for 3 days). Drugs were administered immediately after dental extraction...
August 2016: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/27105592/hplc-enantioseparation-of-racemic-bupropion-baclofen-and-etodolac-modification-of-conventional-ligand-exchange-approach-by-pre-column-formation-of-chiral-ligand-exchange-complexes
#9
Manisha Singh, Ravi Bhushan
Separation of racemic mixture of (RS)-Bupropion, (RS)-Baclofen and (RS)-Etodolac, commonly marketed racemic drugs, has been achieved by modifying the conventional ligand exchange approach. The Cu(II) complexes were first prepared with a few L-amino acids, namely, L-proline, L-histidine, L-phenylalanine, and L-tryptophan and to these was introduced mixture of enantiomer pair of (RS)-bupropion, or (RS)-baclofen or (RS)-etodolac. As a result, formation of a pair of diastereomeric complexes occurred by 'chiral ligand exchange' via the competition between the chelating L-amino acid and each of the two enantiomers from a given pair...
April 23, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/26945484/lidocaine-self-sacrificially-improves-the-skin-permeation-of-the-acidic-and-poorly-water-soluble-drug-etodolac-via-its-transformation-into-an-ionic-liquid
#10
Yasushi Miwa, Hidetoshi Hamamoto, Tatsuhiro Ishida
Poor transdermal penetration of active pharmaceutical ingredients (APIs) impairs both bioavailability and therapeutic benefits and is a major challenge in the development of transdermal drug delivery systems. Here, we transformed a poorly water-soluble drug, etodolac, into an ionic liquid in order to improve its hydrophobicity, hydrophilicity and skin permeability. The ionic liquid was prepared by mixing etodolac with lidocaine (1:1, mol/mol). Both the free drug and the transformed ionic liquid were characterized by differential scanning colorimetry (DSC), infrared spectroscopy (IR), and saturation concentration measurements...
May 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/26944000/stress-impairs-the-efficacy-of-immune-stimulation-by-cpg-c-potential-neuroendocrine-mediating-mechanisms-and-significance-to-tumor-metastasis-and-the-perioperative-period
#11
B Levi, P Matzner, Y Goldfarb, L Sorski, L Shaashua, R Melamed, E Rosenne, G G Page, S Ben-Eliyahu
We recently reported that immune stimulation can be compromised if animals are simultaneously subjected to stressful conditions. To test the generalizability of these findings, and to elucidate neuroendocrine mediating mechanisms, we herein employed CpG-C, a novel TLR-9 immune-stimulating agent. Animals were subjected to ongoing stress (20-h of wet cage exposure) during CpG-C treatment, and antagonists to glucocorticoids, β-adrenoceptor, COX2, or opioids were employed (RU486, nadolol, etodolac, naltrexone)...
August 2016: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/26902001/predictive-factors-for-nsaids-related-gastrointestinal-toxicity-can-cox-2-selective-inhibtor-prevent-it
#12
Yuko Kanbayashi, Hideyuki Konishi
BACKGROUND/AIMS: To identify predictive factors for NSAIDs-related GI toxicity and to clarify whether cox-2 selective inhibitors can prevent it or not. METHODOLOGY: We have surveyed all patients received esophagogastroduodenoscopy examined at our hospital between January 2008 and September 2011. We performed the following retrospective analyses of the clinical records of the 253 patients prescribed NSAIDs. The severity of gastro duodenal mucosal lesions was evaluated using the modified gastro duodenal LANZA score...
June 2015: Hepato-gastroenterology
https://www.readbyqxmd.com/read/26846538/improving-the-performance-of-an-aerobic-membrane-bioreactor-mbr-treating-pharmaceutical-wastewater-with-powdered-activated-carbon-pac-addition
#13
Yasemin Kaya, A Murat Bacaksiz, Ugur Golebatmaz, Ilda Vergili, Z Beril Gönder, Gulsum Yilmaz
In this study, the effects of organic loading rate (OLR) and the addition of powdered activated carbon (PAC) on the performance and membrane fouling of MBR were conducted to treat real pharmaceutical process wastewater. Over 145 days of operation, the MBR system was operated at OLRs ranging from 1 to 2 kg COD m(-3) day(-1) without sludge wasting. The addition of PAC provided an improvement in the flux, despite an increase in the OLR:PAC ratio. The results demonstrated that the hybrid PAC-MBR system maintained a reduced amount of membrane fouling and steadily increased the removal performance of etodolac...
April 2016: Bioprocess and Biosystems Engineering
https://www.readbyqxmd.com/read/26723001/enantioselective-analysis-of-etodolac-in-human-plasma-by-lc-ms-ms-application-to-clinical-pharmacokinetics
#14
Carolina de Miranda Silva, Adriana Rocha, Eduardo Tozatto, Lucienir Maria da Silva, Eduardo Antônio Donadi, Vera Lucia Lanchote
Etodolac is a non-steroidal anti-inflammatory drug with preferential inhibition of cyclooxigenase-2 and is widely used in the management of pain in patients with inflammatory arthritis. Etodolac is available as a racemic mixture of (-)-(R)-Etodolac and (+)-(S)-Etodolac; cyclooxigenases inhibition is attributed to (+)-(S)-Etodolac. According to our knowledge, this is the first method for determination of etodolac enantiomers in plasma using LC-MS/MS. Plasma extraction were performed with 25μL of plasma and 1mL of n-hexane:ethyl acetate (95:5); racemic ibuprofen was used as internal standard...
February 20, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/26695395/selective-cox-2-inhibitors-significantly-reduce-the-occurrence-of-heterotopic-ossification-after-hip-arthroscopic-surgery
#15
Ehud Rath, Yaniv Warschawski, Eran Maman, Oleg Dolkart, Zachary T Sharfman, Moshe Salai, Eyal Amar
BACKGROUND: Heterotopic ossification (HO) after hip arthroscopic surgery is a common complication and may be associated with clinical sequelae such as pain, impingement, and decreased range of motion. Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used medications for reducing or preventing HO. HYPOTHESIS/PURPOSE: The purpose of this study was to evaluate the effectiveness of short-term selective cyclooxygenase-2 (COX-2) inhibitors used for HO prophylaxis after hip arthroscopic surgery...
March 2016: American Journal of Sports Medicine
https://www.readbyqxmd.com/read/26664057/anodic-oxidation-of-etodolac-and-its-linear-sweep-square-wave-and-differential-pulse-voltammetric-determination-in-pharmaceuticals
#16
B Yilmaz, S Kaban, B K Akcay
In this study, simple, fast and reliable cyclic voltammetry, linear sweep voltammetry, square wave voltammetry and differential pulse voltammetry methods were developed and validated for determination of etodolac in pharmaceutical preparations. The proposed methods were based on electrochemical oxidation of etodolac at platinum electrode in acetonitrile solution containing 0.1 M lithium perchlorate. The well-defined oxidation peak was observed at 1.03 V. The calibration curves were linear for etodolac at the concentration range of 2...
July 2015: Indian Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/26456294/an-ionic-liquid-in-water-microemulsion-as-a-potential-carrier-for-topical-delivery-of-poorly-water-soluble-drug-development-ex-vivo-and-in-vivo-evaluation
#17
Shishu Goindi, Ramanpreet Kaur, Randeep Kaur
In this paper, we report an ionic liquid-in-water (IL/w) microemulsion (ME) formulation which is able to solubilize etodolac (ETO), a poorly water soluble drug for topical delivery using BMIMPF6 (1-butyl-3-methylimidazolium hexafluorophosphate) as IL, Tween 80 as surfactant and ethanol as co-surfactant. The prepared ME was characterized for physicochemical parameters, subjected to ex-vivo permeation studies as well as in-vivo pharmacodynamic evaluation. The ex-vivo drug permeation studies through rat skin was performed using Franz-diffusion cell and the IL/w based ME showed maximum mean cumulative percent permeation of 99...
November 30, 2015: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/26448006/network-meta-analysis-comparing-relatively-selective-cox-2-inhibitors-versus-coxibs-for-the-prevention-of-nsaid-induced-gastrointestinal-injury
#18
COMPARATIVE STUDY
Man Yang, Hong-Tao Wang, Miao Zhao, Wen-Bo Meng, Jin-Qing Ou, Jun-Hui He, Bing Zou, Ping-Guang Lei
Currently 2 difference classes of cyclooxygenase (COX)-2 inhibitors, coxibs and relatively selective COX-2 inhibitors, are available for patients requiring nonsteroidal anti-inflammatory drug (NSAID) therapy; their gastroprotective effect is hardly directly compared. The aim of this study was to compare the gastroprotective effect of relatively selective COX-2 inhibitors with coxibs. MEDLINE, EMBASE, and the Cochrane Library (from their inception to March 2015) were searched for potential eligible studies. We included randomized controlled trials comparing coxibs (celecoxib, etoricoxib, parecoxib, and lumiracoxib), relatively selective COX-2 inhibitors (nabumetone, meloxicam, and etodolac), and nonselective NSAIDs with a study duration ≥ 4 weeks...
October 2015: Medicine (Baltimore)
https://www.readbyqxmd.com/read/26275572/a-window-of-opportunity-biomarker-study-of-etodolac-in-resectable-breast-cancer
#19
Richard B Schwab, Shumei Kato, Brian Crain, Minya Pu, Karen Messer, Noel Weidner, Sarah L Blair, Anne M Wallace, Dennis A Carson, Barbara A Parker
Observational data show that nonsteroidal anti-inflammatory drug (NSAID) use is associated with a lower rate of breast cancer. We evaluated the effect of etodolac, an FDA-approved NSAID reported to inhibit cyclooxygenase (COX) enzymes and the retinoid X receptor alpha (RXR), on rationally identified potential biomarkers in breast cancer. Patients with resectable breast cancer planned for initial management with surgical resection were enrolled and took 400 mg of etodolac twice daily prior to surgery. Protein and gene expression levels for genes related to COX-2 and RXRα were evaluated in tumor samples from before and after etodolac exposure...
October 2015: Cancer Medicine
https://www.readbyqxmd.com/read/25929857/effect-of-etodolac-hydrazone-a-new-compound-synthesised-from-etodolac-on-spermatozoon-quality-testicular-lipid-peroxidation-apoptosis-and-spermatozoon-dna-integrity
#20
S Sarıözkan, G Türk, P Çıkla-Süzgün, M Güvenç, A Yüce, A H Yay, F Cantürk, Ş G Küçükgüzel
The aim of this study was to investigate the effect of etodolac hydrazone (EH), a new compound synthesised from etodolac, on spermatozoon quality, testicular lipid peroxidation, apoptosis and spermatozoon DNA integrity in rats. Group 1 (n = 8) received 1 ml dimethyl sulfoxide (DMSO) daily (Control); group 2 (n = 8) was treated with 5 mg kg(-1)  day(-1) EH, dissolved in 1 ml DMSO (EH-5); and group 3 (n = 8) was treated with 10 mg kg(-1)  day(-1) EH, dissolved in 1 ml DMSO (EH-10). All administrations were performed by gavage and maintained for 8 weeks...
March 2016: Andrologia
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