Evaluation of anti-inflammatory and ulcerogenic potential of zinc –ibuprofen and zinc–naproxen complexes in rats
AbstractBecause of numerous indications and high availability, non-steroidal anti-inflammatory drugs (NSAIDs) are among the most commonly prescribed and used medicines in the world. However, long-term therapy with and improper use of NSAIDs may lead to gastrointestinal damage. Therefore, improving the therapeutic index of the existing drugs has become a priority over the past decades. Considerable attention in the field has been concentrated on metal complexes of non-steroidal anti-inflammatory drugs. The aim of this study is to evaluate the effect of complexation with zinc on the anti-inflammatory and ulcerogenic effects ...
Source: Inflammopharmacology - May 23, 2017 Category: Drugs & Pharmacology Source Type: research
Celecoxib for osteoarthritis.
CONCLUSIONS: We are highly reserved about results due to pharmaceutical industry involvement and limited data. We were unable to obtain data from three studies, which included 15,539 participants, and classified as awaiting assessment. Current evidence indicates that celecoxib is slightly better than placebo and some tNSAIDs in reducing pain and improving physical function. We are uncertain if harms differ among celecoxib and placebo or tNSAIDs due to risk of bias, low quality evidence for many outcomes, and that some study authors and Pfizer declined to provide data from completed studies with large numbers of participant...
Source: Cochrane Database of Systematic Reviews - May 22, 2017 Category: General Medicine Authors: Puljak L, Marin A, Vrdoljak D, Markotic F, Utrobicic A, Tugwell P Tags: Cochrane Database Syst Rev Source Type: research
Enzymes Involved in Naproxen Degradation by Planococcus sp. S5.
Authors: Wojcieszyńska D, Domaradzka D, Hupert-Kocurek K, Guzik U Abstract Naproxen is a one of the most popular non-steroidal anti-inflammatory drugs (NSAIDs) entering the environment as a result of high consumption. For this reason, there is an emerging need to recognize mechanisms of its degradation and enzymes engaged in this process. Planococcus sp. S5 is a gram positive strain able to degrade naproxen in monosubstrate culture (27%). However, naproxen is not a sufficient growth substrate for this strain. In the presence of benzoate, 4-hydroxybenzoic acid, 3,4-dihydroxybenzoic acid or vanillic acid as growth s...
Source: Polish Journal of Microbiology - May 20, 2017 Category: Microbiology Tags: Pol J Microbiol Source Type: research
Second-Order Peer Reviews of Clinically Relevant Articles for the Physiatrist: Naproxen with Cyclobenzaprine, Oxycodone/Acetaminophen, or Placebo to Treating Acute Low Back Pain: A Randomized Clinical Trial
No abstract available (Source: American Journal of Physical Medicine and Rehabilitation)
Source: American Journal of Physical Medicine and Rehabilitation - May 19, 2017 Category: Rehabilitation Tags: Physiatry Reviews for Evidence in Practice Source Type: research
Pharmaceutical substances in ambient particulates: A preliminary assessment.
Abstract Till now, no attention has been paid to pharmaceuticals (PCs) in the air, though they are known to affect waters, soils, foods and biota. This paper describes the first attempt to characterize the PC occurrence in the air. Airborne particulates (PM10 or PM2.5 fractions, from Amsterdam, Netherland, Rome and Rende, Italy) were sampled on quartz fiber filter by means of pumping systems operating at medium-volume conditions (16 or 38.5 L min(-1)). The samples were solvent extracted through sonication with a dichloromethane:acetone:methanol mixture and reduced close to dryness; three fractions of the...
Source: Chemosphere - May 18, 2017 Category: Chemistry Authors: Cecinato A, Romagnoli P, Perilli M, Balducci C Tags: Chemosphere Source Type: research
Photochemically Controlled Drug Dosing from a Polymeric Scaffold
ConclusionThis study demonstrates the first application of photochemically controlled drug release from a biomaterial coating and the feasibility of using pMEA as a scaffold for housing the photoactive drug-DMB conjugates. (Source: Pharmaceutical Research)
Source: Pharmaceutical Research - May 15, 2017 Category: Drugs & Pharmacology Source Type: research
One-step synthesis of gold colloids using amidoaminocalixresorcinarenes as reducing and stabilizing agents. Investigation of naproxen binding
Publication date: 20 August 2017 Source:Colloids and Surfaces A: Physicochemical and Engineering Aspects, Volume 527 Author(s): Ya. V. Shalaeva, Ju. E. Morozova, A.M. Ermakova, I.R. Nizameev, M.K. Kadirov, E.Kh. Kazakova, A.I. Konovalov Amido(dimethylamino) calixresorcinarenes with different substituents on the lower rim (-CH3 (С1), −C5H11 (C5), −C11H23 (C11)) both as reducing and stabilizing agent in an aqueous solution were used for the fabrication of stable gold colloids. Gold colloids are characterized by spectrophotometry, FTIR − spectroscopy, transmission electron microscopy, dynamic light scat...
Source: Colloids and Surfaces A: Physicochemical and Engineering Aspects - May 12, 2017 Category: Chemistry Source Type: research
Heteroleptic silver(I) complexes with 2,2':6',2 ″-terpyridines and naproxen: DNA interaction, EGFR/VEGFR2 kinase, growth inhibition and cell cycle arrest studies.
Heteroleptic silver(I) complexes with 2,2':6',2″-terpyridines and naproxen: DNA interaction, EGFR/VEGFR2 kinase, growth inhibition and cell cycle arrest studies. Mater Sci Eng C Mater Biol Appl. 2017 Jul 01;76:601-615 Authors: Mahendiran D, Kumar RS, Rahiman AK Abstract A series of heteroleptic silver(I) complexes of the type [Ag(L(1-3))(nap)] (1-3), where L(1-3)=4'-(4-substituted)-2,2':6',2″-terpyridines and nap=naproxen have been synthesized and characterized by elemental analysis and spectroscopic methods. The geometric parameters of the complexes were determined using UV-Vis and DFT ca...
Source: Appl Human Sci - May 11, 2017 Category: Physiology Authors: Mahendiran D, Kumar RS, Rahiman AK Tags: Mater Sci Eng C Mater Biol Appl Source Type: research
Molecules, Vol. 22, Pages 783: Inclusion Complexes of a New Family of Non-Ionic Amphiphilic Dendrocalixarene and Poorly Water-Soluble Drugs Naproxen and Ibuprofen
The inclusion complexes of a new family of nonionic amphiphilic calixarenes with the anti-inflammatory hydrophobic drugs naproxen (NAP) and ibuprofen (IBP) were investigated. The effects of the alkyl chain ’s length and the inner core of calixarenes on the interaction of the two drugs with the calixarenes were explored. The inclusion complexes of Amphiphiles 1a–c with NAP and IBP increased the solubility of these drugs in aqueous media. The interaction of 1a–c with the drugs in aqueous med ia was investigated through fluorescence, molecular modeling, and 1H-NMR analysis. TEM studies further suppo...
Source: Molecules - May 11, 2017 Category: Chemistry Authors: Khalid Khan Syed Badshah Nasir Ahmad Haroon Rashid Yahia Mabkhot Tags: Article Source Type: research
NSAID heart attack risk apparent in first week of use
Analysis of data from nearly 450,000 patients reveals that celecoxib, diclofenac, ibuprofen, naproxen and rofecoxib all increased heart attack risk, with the greater risk of heart attack becoming apparent in the first week of treatment. (Source: The Pharmaceutical Journal)
Source: The Pharmaceutical Journal - May 10, 2017 Category: Drugs & Pharmacology Source Type: research
Naproxen Inhibits UVB ‐induced Basal Cell and Squamous Cell Carcinoma Development in Ptch1+/−/SKH‐1 hairless mice
Abstract Naproxen possesses anti‐proliferative and pro‐apoptotic effects besides its known anti‐inflammatory functions. Here, we demonstrate the anticancer effects of naproxen against UVB‐induced basal cell carcinoma (BCCs) and squamous cell carcinoma (SCCs) in a highly susceptible murine model of UVB carcinogenesis. Naproxen significantly inhibited UVB‐induced BCCs and SCCs in this model. Tumor number and volume were significantly decreased (P
Source: Photochemistry and Photobiology - May 9, 2017 Category: Science Authors: Sandeep C. Chaudhary, Mohammad Waseem, Mehtab Rana, Hui Xu, Levy Kopelovich, Craig A. Elmets, Mohammad Athar Tags: Special Issue Research Article Source Type: research
Behaviour of the main nonsteroidal anti-inflammatory drugs in a membrane bioreactor treating urban wastewater at high hydraulic- and sludge-retention time
Publication date: 15 August 2017 Source:Journal of Hazardous Materials, Volume 336 Author(s): D.M. González-Pérez, J.I. Pérez, M.A. Gómez The behaviour and removal efficiency of ibuprofen (IBU), diclofenac (DCF), ketoprofen (KPF), and naproxen (NPX) during the real urban wastewater treatment by an experimental full-scale MBR working at high sludge and hydraulic retention time (SRT, HRT) were determined. The MBR worked in denitrification/nitrification conformation at 35.4h of HRT (Q=0.45m3/h), 37 d of SRT and a recirculation flow rate of 4Q. The experiments were made under steady-state condition...
Source: Journal of Hazardous Materials - May 7, 2017 Category: Environmental Health Source Type: research
Improvement of the physicochemical properties of Co-amorphous naproxen-indomethacin by naproxen-sodium
In conclusion, the physical stability as well as the dissolution rate was significantly improved if partial or full exchange of naproxen by its sodium salt was performed, which may present a general optimization method to improve co-amorphous systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 5, 2017 Category: Drugs & Pharmacology Source Type: research
Efficacy of CR4056, a first-in-class imidazoline-2 analgesic drug, in comparison with naproxen in two rat models of osteoarthritis
(Source: Journal of Pain Research)
Source: Journal of Pain Research - May 4, 2017 Category: Anesthesiology Tags: Journal of Pain Research Source Type: research
Nickel(II)-naproxen mixed-ligand complexes: Synthesis, structure, antioxidant activity and interaction with albumins and calf-thymus DNA
New J. Chem., 2017, Accepted Manuscript DOI: 10.1039/C7NJ00257B, PaperXanthippi Totta, Antonios Hatzidimitriou, Athanasios Papadopoulos, George L Psomas The nickel(II) complexes with the non-steroidal anti-inflammatory drug naproxen (Hnap) were prepared in the absence or presence of the nitrogen-donor heterocyclic ligands 2,2'-bipyridine (bipy), 1,10-phenanthroline (phen), 2,2'-bipyridylamine (bipyam), 2,2'-dipyridylketone oxime... 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 - May 3, 2017 Category: Chemistry Authors: Xanthippi Totta Source Type: research
Different analgesics prior to intrauterine device insertion: is there any evidence of efficacy?
CONCLUSION: Despite finding that none of the study drugs seemed effective prior to IUD insertion, insertion did not cause severe pain. The negative findings indicate the need for future research into new strategies to decrease pain during IUD placement. PMID: 28463028 [PubMed - as supplied by publisher] (Source: The European Journal of Contraception and Reproductive Health Care)
Source: The European Journal of Contraception and Reproductive Health Care - May 2, 2017 Category: Reproduction Medicine Authors: Elkhouly NI, Maher MA Tags: Eur J Contracept Reprod Health Care Source Type: research
Interpreting the effect of confined cyclodextrin media on the FRET efficacy between Naproxen and a bio-active 3-pyrazolyl-2-pyrazoline derivative on the light of spectroscopic investigation appended by TD-DFT simulations and molecular docking analysis
Publication date: 15 June 2017 Source:Journal of Photochemistry and Photobiology A: Chemistry, Volume 343 Author(s): Arindam Sarkar, Soumyadipta Rakshit, Subhash Chandra Bhattacharya Significant Fluorescence Resonance Energy Transfer (FRET) process was observed between Naproxen (NPX) and a pharmaceutically important 3-pyrazolyl-2-pyrazoline derivative (PYZ) in bulk aqueous and heterogeneous cyclodextrin medium. The FRET efficacy of NPX-PYZ pair varied considerably in different cyclodextrin environments. Variation in the FRET efficacy mainly occurs due to a change in microenvironment of the fluorophores from bulk to a conf...
Source: Journal of Photochemistry and Photobiology A: Chemistry - April 27, 2017 Category: Chemistry Source Type: research
Gait analysis and weight bearing in pre-clinical joint pain research
Conclusions Objective and reproducible effects, with an endpoint showing face validity compared to pain while walking in patients with joint pain, are achieved by a new way of calculating dynamic weight bearing in monoarthritic rats. (Source: Journal of Neuroscience Methods)
Source: Journal of Neuroscience Methods - April 27, 2017 Category: Neuroscience Source Type: research
Gait analysis and weight bearing in pre-clinical joint pain research.
Conclusions Objective and reproducible effects, with an endpoint showing face validity compared to pain while walking in patients with joint pain, are achieved by a new way of calculating dynamic weight bearing in monoarthritic rats. (Source: Journal of Neuroscience Methods)
Source: Journal of Neuroscience Methods - April 25, 2017 Category: Neuroscience Source Type: research
[Confusion caused by dietary supplement lithium orotate].
Abstract A 38-year-old woman was referred to our hospital with pelvic inflammatory disease. She had been diagnosed as having a tubo-ovarian abscess, for which antibiotic therapy with metronidazole and levofloxacin was indicated. Because the patient was already taking lithium she was prescribed clindamycin instead of metronidazole, a drug that interacts with lithium. For the same reason, naproxen could not be prescribed to reduce pain. However, the lithium taken by the patient turned out to be a dietary supplement containing lithium orotate which she had obtained via the Internet. Because the serum lithium level pr...
Source: Tijdschrift voor Psychiatrie - April 22, 2017 Category: Psychiatry Authors: van Weringh G, Uitvlugt EB, Ponjee GHM, M Jalink G Tags: Tijdschr Psychiatr Source Type: research
Inhibition of pro-inflammatory enzymes by medicinal plants from the Argentinean highlands (Puna)
Conclusions Six out of the 13 species investigated showed a moderate to strong effect towards the enzyme sPLA2 (>40% inhibition at 200µg/mL) while three species presented strong activity against LOX with IC50< 250µg/mL and three were very active against hyaluronidase. Most of the crude drug extracts were able to stabilize the red blood cells membrane preventing their lysis. The compounds identified in the extracts can explain, at least in part, the activity found in the samples. The effect observed for the most active species support their traditional use as anti-inflammatory agents. However, more...
Source: Journal of Ethnopharmacology - April 20, 2017 Category: Drugs & Pharmacology Source Type: research
Enantioselective synthesis of (S)-naproxen using immobilized lipase on chitosan beads.
Abstract S-naproxen by enantioselective hydrolysis of racemic naproxen methyl ester was produced using immobilized lipase. The lipase enzyme was immobilized on chitosan beads, activated chitosan beads by glutaraldehyde, and Amberlite XAD7. In order to find an appropriate support for the hydrolysis reaction of racemic naproxen methyl ester, the conversion and enantioselectivity for all carriers were compared. In addition, effects of the volumetric ratio of two phases in different organic solvents, addition of cosolvent and surfactant, optimum pH and temperature, reusability, and inhibitory effect of methanol were i...
Source: Chirality - April 19, 2017 Category: Molecular Biology Authors: Gilani SL, Najafpour GD, Heydarzadeh HD, Moghadamnia A Tags: Chirality Source Type: research
Adsorption of pharmaceuticals and personal care products over metal-organic frameworks functionalized with hydroxyl groups: Quantitative analyses of H-bonding in adsorption
Publication date: 15 August 2017 Source:Chemical Engineering Journal, Volume 322 Author(s): Ji Yoon Song, Sung Hwa Jhung The removal of pharmaceuticals and personal care products (PPCPs) from water is important for ensuring a clean aquatic environment. In this work, the adsorptive removal of five PPCPs such as p-chloro-m-xylenol, bisphenol-A, triclosan, ketoprofen, and naproxen was carried out using metal-organic framework (MOF, here MIL-101) with or without modifications, i.e., introduction of hydroxyl groups. Quantitative investigations were conducted in order to understand the major mechanisms for adsorption. H-bonding...
Source: Chemical Engineering Journal - April 18, 2017 Category: Chemistry Source Type: research
NSAIDs for high-risk patients: none, celecoxib, or naproxen?
Publication date: Available online 11 April 2017 Source:The Lancet Author(s): Patricia McGettigan, Anne-Marie Schjerning Olsen (Source: The Lancet)
Source: The Lancet - April 13, 2017 Category: Journals (General) Source Type: research
Gastrointestinal safety of celecoxib versus naproxen in patients with cardiothrombotic diseases and arthritis after upper gastrointestinal bleeding (CONCERN): an industry-independent, double-blind, double-dummy, randomised trial
This study was registered with ClinicalTrials.gov, number NCT00153660. Findings Between May 24, 2005, and Nov 28, 2012, we enrolled 514 patients, assigning 257 patients to each study group, all of whom were included in the intention-to-treat population. Recurrent upper gastrointestinal bleeding occurred in 14 patients in the celecoxib group (nine gastric ulcers and five duodenal ulcers) and 31 patients in the naproxen group (25 gastric ulcers, three duodenal ulcers, one gastric ulcer and duodenal ulcer, and two bleeding erosions). The cumulative incidence of recurrent bleeding in 18 months was 5·6% (95% CI 3·...
Source: The Lancet - April 13, 2017 Category: Journals (General) Source Type: research
Pharmacokinetic Variability of Drugs Used for Prophylactic Treatment of Migraine
AbstractIn this review, we evaluate the variability in the pharmacokinetics of 11 drugs with established prophylactic effects in migraine to facilitate ‘personalized medicine’ with these drugs. PubMed was searched for ‘single-dose’ and ‘steady-state’ pharmacokinetic studies of these 11 drugs. The maximum plasma concentration was reported in 248 single-dose and 115 steady-state pharmacokinetic studies, and the area under the plasma conce ntration-time curve was reported in 299 single-dose studies and 112 steady-state pharmacokinetic studies. For each study, the coefficient of variation wa...
Source: CNS Drugs - April 12, 2017 Category: Neurology Source Type: research
Biodegradation of naproxen by freshwater algae Cymbella sp. and Scenedesmus quadricauda and the comparative toxicity.
In this study, both Cymbella sp. and Scenedesmus quadricauda showed complete growth inhibition (100%) at 100mgL(-1) within 24h. Biochemical characteristics including chlorophyll a, carotenoid contents and enzyme activities for these two microalgae were affected by NPX at relatively high concentrations after 4d of exposure. Degradation of naproxen was accelerated by both algae species. Cymbella sp. showed a more satisfactive effect in the bioremediation of NPX with higher removal efficiency. A total of 12 metabolites were identified by LC-MS/MS and the degradation pathways of naproxen in two algae were proposed. Hydroxylati...
Source: Bioresource Technology - April 8, 2017 Category: Biotechnology Authors: Ding T, Lin K, Yang B, Yang M, Li J, Li W, Gan J Tags: Bioresour Technol Source Type: research
Cardiovascular Safety of Celecoxib, Naproxen, or Ibuprofen for Arthritis
New England Journal of Medicine,Volume 376, Issue 14, Page 1389-1390, April 2017. (Source: New England Journal of Medicine)
Source: New England Journal of Medicine - April 5, 2017 Category: Internal Medicine Source Type: research
Structural and physicochemical characterization of pyridine derivative salts of anti-inflammatory drugs
Publication date: 5 August 2017 Source:Journal of Molecular Structure, Volume 1141 Author(s): Sunil Kumar Nechipadappu, Darshak R. Trivedi Salts of common anti-inflammatory drugs mefenamic acid (MFA), tolfenamic acid (TFA) and naproxen (NPX) with various pyridine derivatives (4-amino pyridine (4AP), 4-dimethylaminopyridine (DMAP) and 2-amino pyridine (2AP)) were synthesized by crystal engineering approach based on the pKa values of API's and the salt former. All the salts were characterized systematically by various spectroscopic methods including FT-IR and 1H NMR and the crystal structure was determined by single-crystal...
Source: Journal of Molecular Structure - March 30, 2017 Category: Molecular Biology Source Type: research
Coxibs Refocus Attention on the Cardiovascular Risks of Non-Aspirin NSAIDs
This article explains how coxibs refocused attention on the cardiovascular safety of NSAIDs and the general implications of that. COX-2 activity/specificity is one factor associated with increased cardiovascular risks; however, these risks cannot be attributed to coxibs alone. The traditional NSAIDs (i.e., meloxicam, etodolac, and nabumetone) have significant COX-2 specificity, but naproxen and ibuprofen have less specificity. All NSAIDs, whether traditional or a coxib, pose some cardiovascular risks. It is possible that clinicians continue to focus more on decreasing the immediate gastric risks than preventing the later c...
Source: American Journal of Cardiovascular Drugs - March 28, 2017 Category: Cardiology Source Type: research
Oral nonsteroidal anti-inflammatory drugs for fibromyalgia in adults.
CONCLUSIONS: There is only a modest amount of very low-quality evidence about the use of NSAIDs in fibromyalgia, and that comes from small, largely inadequate studies with potential risk of bias. That bias would normally be to increase the apparent benefits of NSAIDs, but no such benefits were seen. Consequently, NSAIDs cannot be regarded as useful for treating fibromyalgia. PMID: 28349517 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - March 27, 2017 Category: Journals (General) Authors: Derry S, Wiffen PJ, Häuser W, Mücke M, Tölle TR, Bell RF, Moore RA Tags: Cochrane Database Syst Rev Source Type: research
Can wastewater-based epidemiology be used to evaluate the health impact of temperature? - An exploratory study in an Australian population.
This study was to provide the first evaluation to see if WBE can be used to assess the impact of temperature exposure to a population in South East Queensland, Australia using selected pharmaceuticals and personal care products (PPCPs) as biomarkers. Daily loads of eight PPCPs in wastewater collected from a wastewater treatment plant were measured from February 2011 to June 2012. Corresponding daily weather data were obtained from the closest weather station. Missing data of PPCPs were handled using the multiple imputation (MI) method, then we used a one-way between-groups analysis of variance to examine the seasonal effec...
Source: Environmental Research - March 22, 2017 Category: Environmental Health Authors: Phung D, Mueller J, Lai FY, O'Brien J, Dang N, Morawska L, Thai PK Tags: Environ Res Source Type: research
Investigation of naproxen drug using mass spectrometry, thermal analyses and semi-empirical molecular orbital calculation
Publication date: March 2017 Source:Arabian Journal of Chemistry, Volume 10, Issue 3 Author(s): M.A. Zayed, M.F. Hawash, M. El-Desawy, Ali M.M. El-Gizouli Naproxen (C14H14O3) is a non-steroidal anti-inflammatory drug (NSAID). It is important to investigate its structure to know the active groups and weak bonds responsible for medical activity. In the present study, naproxen was investigated by mass spectrometry (MS), thermal analysis (TA) measurements (TG/DTG and DTA) and confirmed by semi empirical molecular orbital (MO) calculation, using PM3 procedure. These calculations included, bond length, bond order, bond strain, ...
Source: Arabian Journal of Chemistry - March 12, 2017 Category: Chemistry Source Type: research
Non-steroidal anti-inflammatory drugs and blood pressure control in patients treated for hypertension: results from the Swedish primary care cardiovascular database.
Authors: Ljungman C, Kahan T, Schiöler L, Wettermark B, Boström KB, Hasselström J, Hjerpe P, Manhem K Abstract PURPOSE: The aim of this observational cohort study was to investigate blood pressure level and the possibility to reach target blood pressure during concomitant use of NSAID in hypertensive patients. MATERIALS AND METHODS: From the Swedish primary care cardiovascular database (SPCCD) a cohort of 5463 patients (2007 to 2008) with at least one prescription of NSAID dispensed 6 months prior to the last blood pressure measurement were included. Clinical data were extracted from computerized...
Source: Blood Pressure - March 11, 2017 Category: Hematology Tags: Blood Press Source Type: research
pH-Dependent behavior of novel gellan beads loaded with naproxen.
Abstract We have designed, formulated and characterized low-acyl gellan gum (GG) macrobeads to be applied as potential carriers for the delivery of naproxen (NPX) to the distal parts of the gastrointestinal tract. The beads were obtained by ionotropic gelation technique. CaCl2 solution (1%, 9.0×10-2 M) was used as a cross-linking medium. Nine different polymer, drug and surfactant (Tween®80) mixtures were used for beads production. The surface and morphology of the dried beads were analyzed by SEM. Raman spectra of NPX powder and the beads confirmed that NPX did not undergo structural changes during prod...
Source: Current Drug Delivery - March 2, 2017 Category: Drugs & Pharmacology Authors: Szybowicz M, Hyla K, Białas M, Milanowski B, Froelich A, Osmałek T Tags: Curr Drug Deliv Source Type: research
Predictions of bisphenol A hepatic clearance in the isolated perfused rat liver (IPRL): impact of albumin binding and of co-administration with naproxen.
This study aimed (i) to characterise hepatic clearance (CL) of bisphenol A (BPA) and naproxen (NAP) administered alone or in binary mixtures to highlight the influence of a binding to albumin (ALB) using an isolated perfused rat liver (IPRL) system; and (ii) to compare results of prediction algorithms with measured clearance rates. 2. The IPRL system and liver microsomes were used to determine the metabolic constants of BPA and NAP either in the presence or absence of ALB. In this study, the IPRL was used as proxy for the in vivo situation. Accordingly, diverse in vitro-to-in vivo and in vivo-to-in vivo extrapolations (IVI...
Source: Xenobiotica - March 2, 2017 Category: Research Authors: Bounakta S, Bteich M, Mantha M, Poulin P, Haddad S Tags: Xenobiotica Source Type: research
Naproxen Inhibits UVB ‐induced Basal Cell and Squamous Cell Carcinoma Development in Ptch1+/‐/SKH‐1 hairless mice
Abstract Naproxen possesses anti‐proliferative and pro‐apoptotic effects besides its known anti‐inflammatory functions. Here, we demonstrate the anti‐cancer effects of naproxen against UVB‐induced BCCs and SCCs in a highly susceptible murine model of UVB carcinogenesis. Naproxen significantly inhibited UVB‐induced BCCs and SCCs in this model. Tumor number and volume were significantly decreased (p
Source: Photochemistry and Photobiology - March 1, 2017 Category: Science Authors: Sandeep C. Chaudhary, Mohammad Waseem, Mehtab Rana, Hui Xu, Levy Kopelovich, Craig A. Elmets, Mohammad Athar Tags: Special Issue Research Article Source Type: research
Melt extrusion vs. spray drying: The effect of processing methods on crystalline content of naproxen-povidone formulations.
This study demonstrated the unique advantages of melt extrusion over spray drying for the preparation of amorphous solid dispersions of naproxen at high drug level. PMID: 28259831 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - February 28, 2017 Category: Drugs & Pharmacology Authors: Haser A, Cao T, Lubach J, Listro T, Acquarulo L, Zhang F Tags: Eur J Pharm Sci Source Type: research
Hand Ground Nanoscale Zn(II)-Coordination Polymers Derived from NSAIDs: Cell Migration Inhibition of Human Breast Cancer Cells.
Abstract Increased level of intracellular prostaglandin E2 (PGE2) has been linked with the unregulated cancer cell migration that often leads to metastasis. Non-steroidal-anti-inflammatory-drugs (NSAIDs) are known inhibitors of cyclooxygenase (COX) enzymes responsible for increased PGE2 concentration in inflammated as well as cancer cells. In this article, we demonstrated that NSAID derived Zn(II)-coordination polymers were able to inhibit cell migration of human breast cancer cells. Various NSAIDs were anchored to a series of 1D Zn(II)-coordination polymers via carboxylate-Zn coordination and fully characterized ...
Source: Chemistry - February 24, 2017 Category: Chemistry Authors: Dastidar P, Paul M, Sarkar K, Deb J Tags: Chemistry Source Type: research
Anti-inflammatory choline based ionic liquids: Insights into their lipophilicity, solubility and toxicity parameters
Publication date: April 2017 Source:Journal of Molecular Liquids, Volume 232 Author(s): Ana M.O. Azevedo, Susana P.F. Costa, Ana F.V. Dias, Alexandre H.O. Marques, Paula C.A.G. Pinto, Katharina Bica, Anna K. Ressmann, Marieta L.C. Passos, André R.T.S. Araújo, Salette Reis, M. Lúcia M.F.S. Saraiva The impact on in vivo efficacy and safety of two novel ionic liquids based on the association of choline with non-steroidal anti-inflammatory drugs, ketoprofen and naproxen forming IL-APIs, was evaluated. Their lipophilicity, solubility and toxicity were assessed aiming the illustration of the pharmaceutical ...
Source: Journal of Molecular Liquids - February 23, 2017 Category: Molecular Biology Source Type: research
COX-2-dependent and independent effects of COX-2 inhibitors and NSAIDs on proatherogenic changes in human monocytes/macrophages
It is the second decade of controversy regarding the cardiovascular effects of cyclo-oxygenase-2 (COX-2) inhibitors. At this time, celecoxib is the only available COX-2-specific inhibitor for treatment of pain and inflammation. Therefore, the present study was designed primarily to determine the impact of celecoxib on cholesterol handling (uptake via scavenger receptors and efflux from the cells) and foam cell formation in human THP-1 macrophages, followed by comparison to rofecoxib and other non-steroidal anti-inflammatory drugs (NSAIDs). THP-1 human macrophages and peripheral blood mononuclear cells were incubated with: ...
Source: Journal of Investigative Medicine - February 22, 2017 Category: Research Authors: Voloshyna, I., Kasselman, L. J., Carsons, S. E., Littlefield, M. J., Gomolin, I. H., De Leon, J., Reiss, A. B. Tags: Original research Source Type: research
Evaluation of para-aminosalicylic acid (PAS) as a substrate of multiple solute carrier (SLC) uptake transporters and possible drug-interactions with NSAIDs, in vitro.
In this study, PAS was found to be a novel substrate of several transporters, and drugs that inhibit these transporters can reduce PAS elimination. PMID: 28223391 [PubMed - as supplied by publisher] (Source: Antimicrobial Agents and Chemotherapy)
Source: Antimicrobial Agents and Chemotherapy - February 20, 2017 Category: Microbiology Authors: Parvez MM, Shin HJ, Jung JA, Shin JG Tags: Antimicrob Agents Chemother Source Type: research
Characterization and regulated naproxen release of hydroxypropyl cyclosophoraose-pullulan microspheres
Publication date: 25 April 2017 Source:Journal of Industrial and Engineering Chemistry, Volume 48 Author(s): Jae Min Choi, Benel Lee, Daham Jeong, Kyeong Hui Park, Eun-Ji Choi, Yong-Joon Jeon, Someshwar D. Dindulkar, Eunae Cho, Sun Hee Do, Kyungho Lee, Im-Soon Lee, Seyeon Park, Bong-Hyun Jun, Jae-Hyuk Yu, Seunho Jung Hydroxypropyl cyclosophoraose-pullulan (HPCys-Pul) microspheres were designed as a novel hybrid system of biocompatible pullulan matrice and pendant hydroxypropyl cyclosophoraoses with drug complexing ability. The HPCys-Pul microspheres were prepared by emulsion crosslinking method, and characterized using th...
Source: Journal of Industrial and Engineering Chemistry - February 19, 2017 Category: Chemistry Source Type: research
Pharmaceutical biological degradation, sorption and mass balance determination in a conventional activated-sludge wastewater treatment plant from Murcia, Spain
Publication date: 15 May 2017 Source:Chemical Engineering Journal, Volume 316 Author(s): Isabel Martínez-Alcalá, José Manuel Guillén-Navarro, Carmen Fernández-López Pharmaceutical compounds are being detected widely in the aquatic environment due to their global consumption. Some ecotoxicological studies have revealed their implication in different toxic effects and the only mechanism available nowadays to combat with this problem are the wastewater treatment plants, which in function of the system employed seem to be more successful in the pharmaceuticals degradation. The contrib...
Source: Chemical Engineering Journal - February 10, 2017 Category: Chemistry Source Type: research
Reactive Melt Extrusion To Improve the Dissolution
Performance and Physical Stability of Naproxen Amorphous Solid Dispersions
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.6b00960 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Authors: Xu Liu, Lin Zhou and Feng Zhang Source Type: research
Diazepam Is No Better Than Placebo When Added to Naproxen for Acute Low Back Pain
Conclusion Among ED patients with acute, nontraumatic, nonradicular low back pain, naproxen+diazepam did not improve functional outcomes or pain compared with naproxen+placebo 1 week and 3 months after ED discharge. (Source: Annals of Emergency Medicine)
Source: Annals of Emergency Medicine - February 7, 2017 Category: Emergency Medicine Source Type: research
Improved tolerance to transplanting injury and chilling stress in rice seedlings treated with orysastrobin
Publication date: Available online 7 February 2017 Source:Plant Physiology and Biochemistry Author(s): Naoto Takahashi, Yukari Sunohara, Masami Fujiwara, Hiroshi Matsumoto In addition to their fungicidal activity, strobilurin-type fungicides are reported to show enhancing effects on crop growth and yield. Previous studies suggested that the fungicide has a mitigating effect on abiotic stresses. However, there are few reports about growth enhancement through abiotic stress alleviation by strobilurin-type fungicides, but the mechanism of action of the growth enhancement is still not clear. The present study revealed that or...
Source: Plant Physiology and Biochemistry - February 7, 2017 Category: Biochemistry Source Type: research
Eudragit( ®) RL as a stabilizer for supersaturation and a substrate for nanocrystal formation.
Eudragit(®) RL as a stabilizer for supersaturation and a substrate for nanocrystal formation. Eur J Pharm Biopharm. 2017 Feb 08;: Authors: Dereymaker A, Cinghia G, Van den Mooter G Abstract In order to optimize supersaturation levels and avoid early drug precipitation, Eudragit(®) RL was tested as a carrier in solid dispersions, either alone or in combination with a hydrophilic polymer (PVP K25). In vitro dissolution performance of the spray dried solid dispersions was tested. The phase behavior of the produced solid dispersions was analyzed as well as dissolution precipitates. In case of weak...
Source: European Journal of Pharmaceutics and Biopharmaceutics - February 7, 2017 Category: Drugs & Pharmacology Authors: Dereymaker A, Cinghia G, Van den Mooter G Tags: Eur J Pharm Biopharm Source Type: research
Structure and physicochemical characterization of a naproxen – picolinamide cocrystal
Naproxen (NPX) is a nonsteroidal anti-inflammatory drug with pain- and fever-relieving properties, currently marketed in the sodium salt form to overcome solubility problems; however, alternative solutions for improving its solubility across all pH values are desirable. NPX is suitable for cocrystal formation, with hydrogen-bonding possibilities via the COOH group. The crystal structure is presented of a 1:1 cocrystal of NPX with picolinamide as a coformer [systematic name: (S)-2-(6-methoxynaphthalen-2-yl)propanoic acid – pyridine-2-carboxamide (1/1), C14H14O3 · C6H6N2O]. The pharmaceutically relevant physical...
Source: Acta Crystallographica Section C - February 5, 2017 Category: Chemistry Authors: Kerr, H.E. Softley, L.K. Suresh, K. Hodgkinson, P. Evans, I.R. Tags: naproxen picolinamide cocrystal NMR crystallography DFT analysis hydrogen bonding crystal structure pharmaceuticals dimers computational chemistry research papers Source Type: research