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Naproxcinod shows significant advantages over naproxen in the mdx model of Duchenne Muscular Dystrophy
Conclusion: In conclusion, this study shows that NO donation may have an important role, in addition to anti-inflammatory activity, in slowing down the progression of the disease in the mdx mouse model therefore positioning naproxcinod as a promising candidate for treatment of DMD. (Source: Orphanet Journal of Rare Diseases)
Source: Orphanet Journal of Rare Diseases - August 22, 2015 Category: Internal Medicine Authors: Daniela MigliettaClara De PalmaClara ScioratiBarbara VerganiViviana PisaAntonello VillaEnnio OnginiEmilio Clementi Source Type: research

Resistance exercise and naproxen sodium: effects on a stable PGF 2α metabolite and morphological adaptations of the upper body appendicular skeleton
Conclusion Despite acute inhibition of the PGF2α metabolite at early time points, naproxen sodium did not hinder positive morphological adaptations of the upper body in response to resistance training. (Source: Inflammopharmacology)
Source: Inflammopharmacology - August 19, 2015 Category: Drugs & Pharmacology Source Type: research

Identification of in vitro and in vivo disconnects using transcriptomic data
Conclusion: The results confirmed that there are important discrepancies between in vitro and in vivo toxicogenomic experiments. However, the contribution of this paper is to provide a tool to identify genes that are disconnected between the two systems. Pathway analysis of disconnected genes may improve our understanding of uncertainties in the mechanism of actions of drug candidates in humans, especially concerning the early detection of toxicity. (Source: BMC Genomics)
Source: BMC Genomics - August 18, 2015 Category: Genetics & Stem Cells Authors: Martin OtavaZiv ShkedyWillem TalloenGeert VerheyenAdetayo Kasim Source Type: research

Chondroprotective effect of three different classes of anti-inflammatory agents on human osteoarthritic chondrocytes exposed to IL-1β.
Abstract VA694, a promising cyclooxigenase-2 (COX-2)-inhibiting hybrid drug endowed with nitric oxide (NO) releasing properties (NO-COXIB), showed COX-2-selective inhibitory effects, associated with interesting anti-inflammatory and anti-nociceptive activities. Therefore, we studied the effects of VA694 on cartilage metabolism, in comparison with Naproxcinod, a COX inhibitor and NO donor (CINOD), and Naproxen, a traditional non-steroidal-anti-inflammatory drug (NSAID) on human osteoarthritic chondrocyte cultures. IL-1β-stimulated chondrocytes showed a significant decrease in cell viability (P<0.001). VA694, Nap...
Source: International Immunopharmacology - August 17, 2015 Category: Allergy & Immunology Authors: Cheleschi S, Pascarelli NA, Valacchi G, Di Capua A, Biava M, Belmonte G, Giordani A, Sticozzi C, Anzini M, Fioravanti A Tags: Int Immunopharmacol Source Type: research

Effects of the non-steroidal anti-inflammatory drug(NSAID) naproxen on gene expression of antioxidant enzymes in zebrafish (Danio rerio)
Publication date: September 2015 Source:Environmental Toxicology and Pharmacology, Volume 40, Issue 2 Author(s): V. Stancová, A. Ziková, Z. Svobodová, W. Kloas The aim of this study was to investigate the effects of naproxen on the gene expression of antioxidant enzymes in adult zebrafish. Surprisingly, after 2 weeks exposure no significant effect on the mRNA expression of the target genes was found in the liver. However, mRNA levels of three genes were altered significantly in the intestine. The expression of Ucp-2 decreased at the environmental concentration of 1μg/L while mRNA expression of GST p2 increased at...
Source: Environmental Toxicology and Pharmacology - August 16, 2015 Category: Environmental Health Source Type: research

Drop printing of pharmaceuticals: Effect of molecular weight on PEG coated‐naproxen/PEG 3350 solid dispersions
Solid dispersions have been used to enhance the bioavailability of poorly water‐soluble active pharmaceutical ingredients (APIs). However, the solid‐state phase, compositional uniformity, and scale‐up problems are issues that need to be addressed. To allow for highly controllable products, the drop printing (DP) technique can provide precise dosages and predictable compositional uniformity of APIs in two‐/three‐dimensional structures. DP was used to prepare naproxen (NAP)/polyethylene glycol 3350 (PEG 3350) solid dispersions with PEG coatings of different molecular weights (MWs). A comparison of moisture‐accele...
Source: AIChE Journal - August 14, 2015 Category: Science Authors: Hsin‐Yun Hsu, Michael T. Harris, Scott Toth, Garth J. Simpson Tags: Soft Matter: Synthesis, Processing and Products Source Type: research

Drop printing of pharmaceuticals: Effect of molecular weight on PEG coated‐naproxen/PEG3350 solid dispersions
This article is protected by copyright. All rights reserved. (Source: AIChE Journal)
Source: AIChE Journal - August 7, 2015 Category: Science Authors: Hsin‐Yun Hsu, Scott Toth, Garth J. Simpson, Michael T. Harris Tags: Soft Matter: Synthesis, Processing and Products Source Type: research

Structural modeling, in vitro antiproliferative activity, and the effect of substituents on the DNA fastening and scission actions of heteroleptic copper(II) complexes with terpyridines and naproxen
New J. Chem., 2015, Advance ArticleDOI: 10.1039/C5NJ01059D, PaperDharmasivam Mahendiran, Perumal Gurumoorthy, Krishnasamy Gunasekaran, Raju Senthil Kumar, Aziz Kalilur RahimanA new series of heteroleptic copper(II) complexes with terpyridines and naproxen are reported. The results of biological activity are laying a foundation for the design of new anticancer agents.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - August 6, 2015 Category: Chemistry Authors: Dharmasivam Mahendiran Source Type: research

Onset and durability of pain relief in knee osteoarthritis: pooled results from two placebo trials of naproxen/esomeprazole combination and celecoxib.
CONCLUSION: Naproxen/esomeprazole produced a significant absolute moderate early pain response, which was maintained for 12 weeks. RAPID3 was found to be highly correlated with the typical OA measure (WOMAC) and might be a useful clinical tool for measuring NSAID response. NCT00664560: https://clinicaltrials.gov/ct2/show/NCT00664560, NCT00665431: https://www.clinicaltrials.gov/ct2/show/NCT00665431. PMID: 26235613 [PubMed - as supplied by publisher] (Source: The Physician and Sportsmedicine Online)
Source: The Physician and Sportsmedicine Online - August 5, 2015 Category: Sports Medicine Tags: Phys Sportsmed Source Type: research

Diverse Ways of Perturbing the Human Arachidonic Acid Metabolic Network To Control Inflammation.
Abstract Inflammation and other common disorders including diabetes, cardiovascular disease, and cancer are often the result of several molecular abnormalities and are not likely to be resolved by a traditional single-target drug discovery approach. Though inflammation is a normal bodily reaction, uncontrolled and misdirected inflammation can cause inflammatory diseases such as rheumatoid arthritis and asthma. Nonsteroidal anti-inflammatory drugs including aspirin, ibuprofen, naproxen, or celecoxib are commonly used to relieve aches and pains, but often these drugs have undesirable and sometimes even fatal side eff...
Source: Cancer Control - August 3, 2015 Category: Cancer & Oncology Authors: Meng H, Liu Y, Lai L Tags: Acc Chem Res Source Type: research

Abstract 877: Aspirin and other nonsteroidal anti-inflammatory drugs, statins, and risk of non-Hodgkin lymphoma
Conclusions. We found a strong inverse association of low dose aspirin use with risk of NHL and the subtypes of DLBCL, FL, and MZL, but no association for regular/extra strength aspirin, other NSAIDs or statin use. While confirmation is needed, our findings for low dose aspirin but not use of other NSAIDs suggest that anti-platelet or other effects of low dose aspirin may be of etiologic significance in lymphomagenesis.Citation Format: James R. Cerhan, Megan M. O'Bryne, Grzegorz S. Nowakowski, Timothy G. Call, Carrie A. Thompson, Tait D. Shanafelt, William R. Macon, Neil E. Kay, Thomas M. Habermann, Susan L. Slager, Mark L...
Source: Cancer Research - August 2, 2015 Category: Cancer & Oncology Authors: Cerhan, J. R., O'Bryne, M. M., Nowakowski, G. S., Call, T. G., Thompson, C. A., Shanafelt, T. D., Macon, W. R., Kay, N. E., Habermann, T. M., Slager, S. L., Liebow, M. Tags: Epidemiology Source Type: research

Abstract 4502: Identification of an aspirin-derived small molecule as a potential therapeutic for colorectal cancer
In the US, colorectal cancer (CRC) remains the second leading cause of cancer-related death. The 5-year survival rate for patients with CRC is 64%, although for patients who present with distant metastases at diagnosis the 5 year survival is only 12%. Currently used standard care for CRC can only marginally extend the survival of patients and is associated with numerous adverse events. Hence, there remains an urgent need for more effective and less toxic treatments, which can increase CRC patient survival with better quality of life. Non-steroidal anti-inflammatory drugs (NSAIDs) (e.g. Aspirin, Ibuprofen, Naproxen), which ...
Source: Cancer Research - August 2, 2015 Category: Cancer & Oncology Authors: Karelia, D., Pandey, M., Plano, D., Narayan, S., Jani, J., Sharma, J., Amin, S., Sharma, A. K. Tags: Experimental and Molecular Therapeutics Source Type: research

Acute Migraine Treatment
This article provides a systematic, evidence-based approach to acute medication choices for the patient with migraine. Recent Findings:: Recent clinical trials, meta-analyses, and practice guidelines have confirmed that four nonsteroidal anti-inflammatory drugs (NSAIDs) with randomized controlled trial evidence for efficacy in migraine (ibuprofen, naproxen sodium, diclofenac potassium, and acetylsalicylic acid) and seven triptans (sumatriptan, rizatriptan, eletriptan, zolmitriptan, almotriptan, frovatriptan, and naratriptan) are appropriate medications for acute migraine treatment. Dihydroergotamine (DHE) is also suitable ...
Source: CONTINUUM - August 1, 2015 Category: Neurology Tags: Review Articles Source Type: research

Separation and On‐line Preconcentration of Nonsteroidal Anti‐inflammatory Drugs by Microemulsion Electrokinetic Chromatography
This article is protected by copyright. All rights reserved (Source: Electrophoresis)
Source: Electrophoresis - August 1, 2015 Category: Biochemistry Authors: Chia‐Wen Chang, Yu‐Cheng Chen, Chuen‐Ying Liu Tags: Research Paper Source Type: research

Functional food property of honey locust (Gleditsia triacanthos) flowers
Publication date: October 2015 Source:Journal of Functional Foods, Volume 18, Part A Author(s): Chuan-Rui Zhang, Amila A. Dissanayake, Muraleedharan G. Nair The use of honey locust in food prompted us to study its flowers for functional food constituents. Bioassay-guided purification of hexane, ethyl acetate and methanolic extracts of its flowers afforded three new betulinic acid esters (1–3), one new linalool carboxylic acid ester (4), known terpenoids (5–7) and known polyphenols (8–11), as elucidated by spectroscopic methods. The extracts and terpenoids 1–7 were tested for antiinflammatory and antioxidant ac...
Source: Journal of Functional Foods - July 31, 2015 Category: Nutrition Source Type: research

Interventions for pain with intrauterine device insertion.
CONCLUSIONS: Nearly all trials used modern IUC. Most effectiveness evidence was of moderate quality, having come from single trials. Lidocaine 2% gel, misoprostol, and most NSAIDs did not help reduce pain. Some lidocaine formulations, tramadol, and naproxen had some effect on reducing IUC insertion-related pain in specific groups. The ineffective interventions do not need further research. PMID: 26222246 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - July 29, 2015 Category: Journals (General) Authors: Lopez LM, Bernholc A, Zeng Y, Allen RH, Bartz D, O'Brien PA, Hubacher D Tags: Cochrane Database Syst Rev Source Type: research

Structural modeling, in vitro antiproliferative activity, and effect of substituents on dna fastening and scission actions of heteroleptic copper(ii) complexes with terpyridines and naproxen drug
New J. Chem., 2015, Accepted ManuscriptDOI: 10.1039/C5NJ01059D, PaperKalilur Rahiman, Dharmasivam Mahendiran, Perumal Gurumoorthy, Gunasekaran krishnasamy, Senthil kumar RajuA series of heteroleptic copper(II) complexes of the type [Cu(L1-6)(nap)Cl] (1-6) (L1-6 = 4'-(4-substituted)-2,2':6',2''-terpyridines, nap = naproxen drug) have been synthesized and characterized. The single crystal analysis of complexes 1...The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - July 24, 2015 Category: Chemistry Authors: Kalilur Rahiman Source Type: research

Non-steroidal anti-inflammatory drugs (NSAIDs) for axial spondyloarthritis (ankylosing spondylitis and non-radiographic axial spondyloarthritis).
CONCLUSIONS: High to moderate quality evidence indicates that both traditional and COX-2 NSAIDs are efficacious for treating axSpA, and moderate to low quality evidence indicates harms may not differ from placebo in the short term. Various NSAIDs are equally effective. Continuous NSAID use may reduce radiographic spinal progression, but this requires confirmation. PMID: 26186173 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - July 17, 2015 Category: Journals (General) Authors: Kroon FP, van der Burg LR, Ramiro S, Landewé RB, Buchbinder R, Falzon L, van der Heijde D Tags: Cochrane Database Syst Rev Source Type: research

A novel approach for predicting the dissolution profiles of pharmaceutical tablets.
Abstract In this paper, the intrinsic dissolution profiles of naproxen (NAP) at pH values of 1.5 and 3.0 and of trimethoprim (TMP) at pH values of 1.5, 3.0, 5.0, 6.5 and 7.2 were measured. Meanwhile, the dissolution profiles of NAP and TMP from cylindrical tablets were measured at different temperatures (298.15 K, 305.15 K, 301.15 K and 310.15 K) and stirring speeds (50 rpm, 100 rpm and 150 rpm) as well as at different pH values (1.5, 3.0, 5.0, 6.5 and 7.2). Additionally the pH-dependent solubilities of both APIs were measured and modeled. The chemical-potential-gradient model combined with the perturbed-chain stat...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 10, 2015 Category: Drugs & Pharmacology Authors: Paus R, Hart E, Ji Y Tags: Eur J Pharm Biopharm Source Type: research

Enteric protection of naproxen in a fixed-dose combination product produced by hot-melt co-extrusion
In this study hot-melt co-extrusion is used as processing technique to manufacture a fixed-dose combination product providing enteric protection to naproxen incorporated in the core and immediate release to esomeprazole magnesium embedded in the coat. The plasticizing effect of naproxen and triethyl citrate (TEC) was tested on the enteric polymers investigated (Eudragit® L100-55, HPMC-AS-LF and HPMCP-HP-50). Core matrix formulations containing HPMC-AS-LF, TEC and a naproxen load of 15, 30 and 50% were processed and characterized. The in vitro naproxen release in 0.1N HCl was prevented for 2h for all formulations. The phys...
Source: International Journal of Pharmaceutics - July 4, 2015 Category: Drugs & Pharmacology Source Type: research

Occurrence of pharmaceuticals in municipal wastewater, in the recipient water, and sedimented particles of northern Lake Päijänne.
Abstract The presence of five different pharmaceuticals, consisting of four anti-inflammatory and one antiepileptic drug, was determined in influent and effluent of a municipal wastewater treatment plant (WWTP) near the city of Jyväskylä, Finland, and in the receiving water, northern Lake Päijänne. In addition, samples of sedimented particles were collected among water samples from five locations near the discharge point of the treated wastewater. The solid phase extracts (SPEs) of water samples were analyzed by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) in the multiple reaction monito...
Source: Environmental Science and Pollution Research International - July 3, 2015 Category: Environmental Health Authors: Lindholm-Lehto PC, Ahkola HS, Knuutinen JS, Herve SH Tags: Environ Sci Pollut Res Int Source Type: research

A Novel Approach for Analyzing the Dissolution Mechanism of Solid Dispersions
Conclusions The chemical-potential-gradient model combined with PC-SAFT can be used to analyze the dissolution mechanism of solid dispersions and to describe and predict the dissolution profiles of API as function of stirring speed, temperature and pH value of the medium. This work helps to find appropriate ways to improve the dissolution rate of poorly-soluble APIs. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - July 2, 2015 Category: Drugs & Pharmacology Source Type: research

Semisynthetic hybrids of boswellic acids: a novel class of potential anti-inflammatory and anti-arthritic agents
Abstract A series of hybrid molecules 7–13 of boswellic acid (BA)/11-keto-β-boswellic acid (KBA) 1/2 with well-known anti-inflammatory drugs (i.e. aspirin, naproxen, ibuprofen and cinnamic acid) have been synthesized and evaluated for their anti-inflammatory and anti-arthritic activities. Two of hybrid compounds 8 and 11 bearing naproxen and BA/KBA unit have displayed promising anti-inflammatory and anti-arthritic activities than the standard drugs. (Source: Medicinal Chemistry Research)
Source: Medicinal Chemistry Research - July 1, 2015 Category: Chemistry Source Type: research

Nonsteroidal Anti-inflammatory Drugs in-vitro and in-vivo treatment and Multidrug Resistance Protein 4 expression in human platelets.
Abstract Platelet Multidrug Resistance Protein4 (MRP4)-overexpression has a role in reducing aspirin action in patients after by-pass surgery. Aspirin induces platelet MRP4 over-expression, through megakaryocytes genomic modulation. Aim of our work was to verify whether other Non-Steroidal Anti Inflammatory Drugs (NSAIDs) enhance platelet MRP4 expression and evaluate platelet function in patients who overexpressed MRP4. We evaluated MRP4-mRNA in a human megakacaryoblastic cell line(DAMI), treated with both COX-2 inhibitor (Celecoxib) and traditional NSAIDs (Diclofenac and Naproxen). Osteoarthritis patients, who rep...
Source: Vascular Pharmacology - June 30, 2015 Category: Drugs & Pharmacology Authors: Temperilli F, Di Franco M, Massimi I, Guarino ML, Guzzo MP, Valesini G, Frati L, Pulcinelli FM Tags: Vascul Pharmacol Source Type: research

Toxicity and antinociceptive effects of Hamelia patens
Abstract Many medicinal herbs are used in folk medicine without taking into account their toxicity. Hamelia patens Jacq. (Rubiaceae), a Mexican endemic species, is used for the empirical treatment of pain. The aim of this work was to evaluate the toxicity and antinociceptive effects of ethanolic extracts of H. patens leaves. The toxicity of H. patens leaves (500–5000 mg/kg) was evaluated in acute (14 days) and subacute (28 days) assays. In the subacute assay, a blood analysis (both hematology and chemistry) was carried out. The antinociceptive effects of H. patens leaves (50–200 mg/kg) were evaluated using thermal-indu...
Source: Revista Brasileira de Farmacognosia - June 27, 2015 Category: Drugs & Pharmacology Source Type: research

Roles of functional groups of naproxen in its sorption to kaolinite.
In this study, batch experiments of naproxen (NPX, anti-inflammatory drug) and two kinds of competitors to kaolinite were studied. The Kd of naproxen to kaolinite is 1.30-1.62Lkg(-1). The n-π electron donor-acceptor (n-π EDA) interaction between diaromatic ring of naproxen (π-electron acceptors) and the siloxane oxygens (n-donors) of kaolinite is the dominant sorption mechanism. The carboxyl group of naproxen can contribute to the overall sorption. A conception model was put forward to elucidate to sorption mechanisms, in which the contribution of n-π EDA and hydrogen bond to overall sorption was quantified. These sorp...
Source: Chemosphere - June 27, 2015 Category: Chemistry Authors: Yu C, Bi E Tags: Chemosphere Source Type: research

P-305 * A Phase Ib Biomarker Trial of Naproxen in Patients at Risk for DNA Mismatch Repair Deficient Colorectal Cancer
(Source: Annals of Oncology)
Source: Annals of Oncology - June 24, 2015 Category: Cancer & Oncology Authors: Vilar, E., Stoffel, E., Lim, R., Lynch, P., You, Y. N., Lipkin, S., Vornik, L., Lee, J., Perloff, M., Brown, P. Tags: posters Source Type: research

Selective inhibition by aspirin and naproxen of mainstream cigarette smoke-induced genotoxicity and lung tumors in female mice.
Abstract The role of nonsteroidal anti-inflammatory drugs (NSAIDs) in smoke-related lung carcinogenesis is still controversial. We have developed and validated a murine model for evaluating the tumorigenicity of mainstream cigarette smoke (MCS) and its modulation by chemopreventive agents. In the present study, the protective effects of the nonselective cyclooxygenase inhibitors aspirin and naproxen were investigated by using a total of 277 Swiss H neonatal mice of both genders. Groups of mice were exposed whole-body to MCS during the first 4 months of life, followed by an additional 3.5 months in filtered air in...
Source: Archives of Toxicology - June 24, 2015 Category: Toxicology Authors: Balansky R, Ganchev G, Iltcheva M, Micale RT, La Maestra S, D'Oria C, Steele VE, De Flora S Tags: Arch Toxicol Source Type: research

Influence of humidity on the phase behavior of API/polymer formulations.
Abstract Amorphous formulations of APIs in polymers tend to absorb water from the atmosphere. This absorption of water can induce API recrystallization, leading to reduced long-term stability during storage. In this work, the phase behavior of different formulations was investigated as a function of relative humidity. Indomethacin and naproxen were chosen as model APIs and poly(vinyl pyrrolidone) (PVP) and poly(vinyl pyrrolidone-co-vinyl acetate) (PVPVA64) as excipients. The formulations were prepared by spray drying. The water sorption in pure polymers and in formulations was measured at 25°C and at different val...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 24, 2015 Category: Drugs & Pharmacology Authors: Prudic A, Ji Y, Luebbert C, Sadowski G Tags: Eur J Pharm Biopharm Source Type: research

Cyclosporin A‐sensitive cytotoxicity of flurbiprofen non‐stereoselectively mediated by cytochrome P450 metabolism in three‐dimensional cultured rat hepatocytes
ConclusionThe reactive acyl‐CoA thioesters and acyl‐glucuronides were not associated with liver damage, denying one of the leading hypotheses. CYP metabolism of FLP non‐stereoselectively participated in Cys A‐sensitive cytotoxicity, suggesting mitochondrial injury. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - June 23, 2015 Category: Drugs & Pharmacology Authors: Tadatoshi Tanino, Yoshinori Funakami, Noriaki Nagai, Yoshihisa Kato Tags: Research Paper Source Type: research

Effects of over-the-counter analgesic use on reproductive hormones and ovulation in healthy, premenopausal women
STUDY QUESTION Does use of commonly used over-the-counter (OTC) pain medication affect reproductive hormones and ovulatory function in premenopausal women? SUMMARY ANSWER Few associations were found between analgesic medication use and reproductive hormones, but use during the follicular phase was associated with decreased odds of sporadic anovulation after adjusting for potential confounders. WHAT IS KNOWN ALREADY Analgesic medications are the most commonly used OTC drugs among women, but their potential effects on reproductive function are unclear. STUDY DESIGN, SIZE, DURATION The BioCycle Study was a prospective, obs...
Source: Human Reproduction - June 18, 2015 Category: Reproduction Medicine Authors: Matyas, R. A., Mumford, S. L., Schliep, K. C., Ahrens, K. A., Sjaarda, L. A., Perkins, N. J., Filiberto, A. C., Mattison, D., Zarek, S. M., Wactawski-Wende, J., Schisterman, E. F. Tags: Reproductive epidemiology Source Type: research

Molecules, Vol. 20, Pages 11219-11235: Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs
The aim of the study was to assess changes in the activity of anti-inflammatory terpenes from Chilean medicinal plants after the formation of derivatives incorporating synthetic anti-inflammatory agents. Ten new hybrid molecules were synthesized combining terpenes (ferruginol (1), imbricatolic acid (2) and oleanolic acid (3)) with ibuprofen (4) or naproxen (5). The topical anti-inflammatory activity of the compounds was assessed in mice by the arachidonic acid (AA) and 12-O-tetradecanoyl phorbol 13-acetate (TPA) induced ear edema assays. Basal cytotoxicity was determined towards human lung fibroblasts, gastric epithelial c...
Source: Molecules - June 18, 2015 Category: Chemistry Authors: Cristina TheodulozCarla DelporteGabriela Valenzuela-BarraXimena SilvaSolange CádizFernanda BustamanteMariano PertinoGuillermo Schmeda-Hirschmann Tags: Article Source Type: research

Removal of emerging pollutants through Granular Activated Carbon
The objective of this study was to evaluate the efficiency of adsorption at Granular Activated Carbon (GAC) columns on the removal of selected Emerging Contaminants (ECs) from water at concentrations found in the aquatic environment (from ng/L to few μg/L) and to obtain breakthrough curves for each substance. For this scope several fixed bed column experiments have been conducted in a pilot-scale GAC column system. The ECs examined were the Endocrine Disrupting Compounds (EDCs) Bisphenol-A (BPA) and Triclosan (TCS) and the Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Ibuprofen (IBU), Naproxen (NPX) and Ketoprofen (KFN)....
Source: Chemical Engineering Journal - June 17, 2015 Category: Chemistry Source Type: research

Combined use of L‐Alanine Tert Butyl Ester Lactate and Trimethyl‐β‐Cyclodextrin for the enantiomeric separations of 2‐arylpropionic acids non‐steroidal anti‐inflammatory drugs
This article is protected by copyright. All rights reserved (Source: Electrophoresis)
Source: Electrophoresis - June 17, 2015 Category: Biochemistry Authors: Maria C. Mavroudi, Constantina P. Kapnissi‐Christodoulou Tags: Research Paper Source Type: research

High gastrointestinal permeability and local metabolism of naringenin: influence of antibiotic treatment on absorption and metabolism.
Abstract The present study aims to determine the permeability of naringenin in the stomach, small intestine and colon, to evaluate intestinal and hepatic first-pass metabolism, and to study the influence of the microbiota on the absorption and disposition of naringenin (3·5 μg/ml). A single-pass intestinal perfusion model in mice (n 4-6) was used. Perfusate (every 10 min), blood (at 60 min) and bile samples were taken and analysed to evaluate the presence of naringenin and its metabolites by an HPLC-MS/MS method. To study the influence of the microbiota on the bioavailability of naringenin, a group of animals ...
Source: The British Journal of Nutrition - June 17, 2015 Category: Nutrition Authors: Orrego-Lagarón N, Martínez-Huélamo M, Vallverdú-Queralt A, Lamuela-Raventos RM, Escribano-Ferrer E Tags: Br J Nutr Source Type: research

Controlled release of acidic drugs in compendial and physiological hydrogen carbonate buffer from polymer blend-coated oral solid dosage forms.
The objective of this study was to investigate the suitability of "Eudragit® RL/Eudragit® L55" (RL/L55) blend coatings for a pH-independent release of acidic drugs. A coating for ketoprofen and naproxen mini tablets was developed showing constant drug release rate under pharmacopeial two-stage test conditions for at least 300min. To simulate drug release from the mini tablets coated with RL/L55 blends in the gastrointestinal (GI) tract, drug release profiles in Hanks buffer pH 6.8 were recorded and compared with drug release profiles in compendial media. RL/L55 blend coatings showed increased drug permeability in Hanks b...
Source: European Journal of Pharmaceutical Sciences - June 17, 2015 Category: Drugs & Pharmacology Authors: Wulff R, Rappen GM, Koziolek M, Garbacz G, Leopold CS Tags: Eur J Pharm Sci Source Type: research

Deciphering the pathogenesis of NSAID enteropathy using proton pump inhibitors and a hydrogen sulfide-releasing NSAID
The small intestine is a significant site of ulceration and bleeding induced by nonsteroidal anti-inflammatory drugs (NSAIDs). The pathogenesis is poorly understood. The present study explored the roles of bile, bacteria, and enterohepatic circulation to NSAID enteropathy, using both a conventional NSAID (naproxen) and a gastrointestinal-safe naproxen derivative (ATB-346), as well as proton pump inhibitors (PPIs). Rats were treated orally with naproxen or equimolar doses of ATB-346 over a 5-day period, with or without PPI administration, and intestinal damage was quantified. The cytotoxicity of bile from the rats was evalu...
Source: AJP: Gastrointestinal and Liver Physiology - June 15, 2015 Category: Gastroenterology Authors: Blackler, R. W., De Palma, G., Manko, A., Da Silva, G. J., Flannigan, K. L., Bercik, P., Surette, M. G., Buret, A. G., Wallace, J. L. Tags: INFLAMMATION/IMMUNITY/MEDIATORS Source Type: research

Thermodynamic insights into drug–surfactant interactions: Study of the interactions of naporxen, diclofenac sodium, neomycin, and lincomycin with hexadecytrimethylammonium bromide by using isothermal titration calorimetry
Publication date: 1 August 2015 Source:Colloids and Surfaces B: Biointerfaces, Volume 132 Author(s): Sinjan Choudhary , Paurnima Talele , Nand Kishore The success of drug delivery depends on the efficiency of the route of administration, which in turn relies on properties of the drug and its transport vehicle. A quantitative knowledge of association of drugs with transport vehicles is lacking when the latter are in the category of self assembled structures. The work reported in this manuscript addresses the mechanism of partitioning of naproxen, diclofenac sodium, neomycin and lincomycin in the micelles of hexadecytrimet...
Source: Colloids and Surfaces B: Biointerfaces - June 10, 2015 Category: Biochemistry Source Type: research

In Vivo Effects of Naproxen, Salicylic Acid, and Valproic Acid on the Pharmacokinetics of Trichloroethylene and Metabolites in Rats
(Source: Journal of Toxicology and Environmental Health Part A)
Source: Journal of Toxicology and Environmental Health Part A - June 8, 2015 Category: Environmental Health Authors: RouhouCharest-TardifHaddad Source Type: research

New insight into the mechanisms of gastroduodenal injury induced by nonsteroidal anti-inflammatory drugs: practical implications.
In conclusion, new derivatives of NSAIDs releasing vasoactive gaseous mediators NO or H₂S are associated with fewer gastrointestinal adverse effects, suggesting that, in the future, they may be used as a safer alternative in everyday clinical practice and antithrombotic therapy. PMID: 25666703 [PubMed - in process] (Source: Polskie Archiwum Medycyny Wewnetrznej)
Source: Polskie Archiwum Medycyny Wewnetrznej - June 3, 2015 Category: Internal Medicine Tags: Pol Arch Med Wewn Source Type: research

Assessment of naproxen adsorption on bone char in aqueous solutions using batch and fixed-bed processes
This study highlights the relevance of performing an integrated analysis of adsorbent effectiveness in batch and dynamic conditions to establish the best process configuration for the removal of emerging water pollutants such as pharmaceuticals. (Source: Journal of Molecular Liquids)
Source: Journal of Molecular Liquids - May 31, 2015 Category: Molecular Biology Source Type: research

Comparison of Oral Oxycodone and Naproxen in Soft Tissue Injury Pain Control: A Double Blind Randomized Clinical Trial
This randomized clinical trial compares the efficacy and safety of oral oxycodone (an oral opioid) with naproxen (a non-steroidal anti-inflammatory drug) in acute pain control in patients with soft tissue injury. It also evaluates the need for additional doses of analgesics in the first 24 hours of discharge from emergency department (ED). (Source: The American Journal of Emergency Medicine)
Source: The American Journal of Emergency Medicine - May 29, 2015 Category: Emergency Medicine Authors: Marzieh Fathi, Mohammad Amin Zare, Hamid Reza Bahmani, Shahriar Zehtabchi Source Type: research

Comparison of oral oxycodone and naproxen in soft tissue injury pain control: a double-blind randomized clinical trial
This randomized clinical trial compares the efficacy and safety of oral oxycodone (an oral opioid) with naproxen (a nonsteroidal anti-inflammatory drug) in acute pain control in patients with soft tissue injury. It also evaluates the need for additional doses of analgesics in the first 24 hours of discharge from emergency department (ED). (Source: The American Journal of Emergency Medicine)
Source: The American Journal of Emergency Medicine - May 29, 2015 Category: Emergency Medicine Authors: Marzieh Fathi, Mohammad Amin Zare, Hamid Reza Bahmani, Shahriar Zehtabchi Tags: Original Contribution Source Type: research

Selective adsorption mechanisms of antilipidemic and non-steroidal anti-inflammatory drug residues on functionalized silica-based porous materials in a mixed solute.
Abstract The selective adsorption mechanisms of naproxen (NAP), acetaminophen (ACT), and clofibric acid (CFA) on silica-based porous materials were examined by single and mixed-batch adsorption. Effects of the types and densities of surface functional groups on adsorption capacities were determined, including the role of hydrophobic and hydrophilic dissolved organic matters (DOMs). Hexagonal mesoporous silica (HMS), superparamagnetic HMS (HMS-SP) and SBA-15 were functionalized and applied as adsorbents. Compared with powdered activated carbon (PAC), amine-functionalized HMS had a better adsorption capacity for CFA,...
Source: Chemosphere - May 26, 2015 Category: Chemistry Authors: Suriyanon N, Permrungruang J, Kaosaiphun J, Wongrueng A, Ngamcharussrivichai C, Punyapalakul P Tags: Chemosphere Source Type: research

Thermodynamic insights into drug-surfactant interactions: Study of the interactions of naporxen, diclofenac sodium, neomycin, and lincomycin with hexadecytrimethylammonium bromide by using isothermal titration calorimetry.
Abstract The success of drug delivery depends on the efficiency of the route of administration, which in turn relies on properties of the drug and its transport vehicle. A quantitative knowledge of association of drugs with transport vehicles is lacking when the latter are in the category of self assembled structures. The work reported in this manuscript addresses the mechanism of partitioning of naproxen, diclofenac sodium, neomycin and lincomycin in the micelles of hexadecytrimethylammonium bromide and that is quantitatively based on the measurement of thermodynamic parameters of interactions by using isothermal ...
Source: Colloids and Surfaces - May 23, 2015 Category: Biotechnology Authors: Choudhary S, Talele P, Kishore N Tags: Colloids Surf B Biointerfaces Source Type: research

Self-assembly of amphiphilic anionic calix[4]arenes and encapsulation of poorly soluble naproxen and flurbiprofen
Org. Biomol. Chem., 2015, Advance ArticleDOI: 10.1039/C5OB00703H, CommunicationLucia Barbera, Giuseppe Gattuso, Franz H. Kohnke, Anna Notti, Sebastiano Pappalardo, Melchiorre F. Parisi, Ilenia Pisagatti, Salvatore Patane, Norberto Micali, Valentina VillariThe ability of an anionic calix[4]arene amphiphile to aggregate and to solubilize, as a result, the poorly water-soluble drugs naproxen and flurbiprofen is described.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Organic Biomolecular Chemistry)
Source: RSC - Organic Biomolecular Chemistry - May 22, 2015 Category: Molecular Biology Authors: Lucia Barbera Source Type: research

Efficacy and safety of nonsteroidal anti‐inflammatory drugs in Asian patients with knee osteoarthritis: summary of a randomized, placebo‐controlled study
ConclusionCelecoxib and naproxen were comparable in their effects to reduce the signs and symptoms of knee OA in Asian patients. Celecoxib was shown to be safe and well tolerated in this patient population. (Source: APLAR Journal of Rheumatology)
Source: APLAR Journal of Rheumatology - May 20, 2015 Category: Rheumatology Authors: Margaret N. Essex, Michael A. O'Connell, Regina Behar, Weihang Bao Tags: Original Article Source Type: research

pH-responsive ABC type miktoarm star terpolymers: Synthesis via combination of click reaction and SET-LRP, characterization, self-assembly, and controlled drug release
We report on the one-pot synthesis of well-defined ABC miktoarm star terpolymers consisting of poly(ethyleneglycol)-b-poly(tert-butylacrylate)-b-polycaprolactone, (mPEG-b-PtBA-b-PCL), by using combination of click reaction and single electron transfer living radical polymerization (SET-LRP). Mono-epoxide functionalized mPEG (mPEG-EP) was synthesized and reacted with sodium azide in the presence of NH4Cl to afford mPEG-N3(-OH). Then, a difunctional molecule bearing azide and bromine moieties, mPEG-N3(-Br), was synthesized via the nucleophilic reaction of mPEG-N3(-OH) with 2-bromoisobutyryl bromide. Propargyl-terminated poly...
Source: Polymer - May 19, 2015 Category: Chemistry Source Type: research

Design, Synthesis and QSAR Studies on a Series of 2, 5-Disubstituted-1,3,4-oxadiazole Derivatives of Diclofenac and Naproxen For Analgesic and Anti-inflammatory activity.
Abstract A series of twenty molecules belonging to 2,5-disubstituted-1,3,4-oxadiazole derivatives of Diclofenac and Naproxen were designed, synthesized and their structures were confirmed by spectroscopy. The target compounds were evaluated for anti-inflammatory and analgesic activity. The result indicates that the compounds 12, 4, 6, 7 and 15 were found to have good analgesic and anti-inflammatory activities, while the compounds 12 and 14 were found to have good analgesic and the compound 22 were found to have good anti-inflammatory activities. HQSAR and Topomer QSAR studies were performed to get insights in the s...
Source: Medicinal Chemistry - May 19, 2015 Category: Chemistry Authors: Ilango K, Valentina P, Kumar G, Dixit D, Nilewar S, Kathiravan MK Tags: Med Chem Source Type: research

Insights into the Entrance/Exit Route of COX-2 [Lipids]
Cyclooxygenase enzymes (COX-1 and COX-2) catalyze the conversion of arachidonic acid to prostaglandin G2. The inhibitory activity of rapid, reversible COX inhibitors (ibuprofen, naproxen, mefenamic acid, and lumiracoxib) demonstrated a significant increase in potency and time dependence of inhibition against double tryptophan murine COX-2 mutants at the 89/90 and 89/119 positions. In contrast, the slow, time-dependent COX inhibitors (diclofenac, indomethacin, and flurbiprofen) were unaffected by those mutations. Further mutagenesis studies suggested that mutation at position 89 was principally responsible for the changes i...
Source: Journal of Biological Chemistry - May 14, 2015 Category: Chemistry Authors: Blobaum, A. L., Xu, S., Rowlinson, S. W., Duggan, K. C., Banerjee, S., Kudalkar, S. N., Birmingham, W. R., Ghebreselasie, K., Marnett, L. J. Tags: Enzymology Source Type: research