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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 calixarenes 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 calixarene 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
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
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
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
Gastroprotective Properties of Cashew Gum, a Complex Heteropolysaccharide of Anacardium occidentale, in Naproxen‐Induced Gastrointestinal Damage in Rats
ABSTRACT Long‐term use nonsteroidal anti‐inflammatory drug is associated with gastrointestinal (GI) lesion formation. The aim of this study was to investigate the protective activity of cashew gum (CG), a complex heteropolysaccharide extracted from Anacardium occidentale on naproxen (NAP)‐induced GI damage. Male Wistar rats were pretreated with vehicle or CG (1, 3, 10, and 30 mg/kg, p.o.) twice daily for 2 days; after 1 h, NAP (80 mg/kg, p.o.) was administered. The rats were euthanized on the 2nd day of treatment, 4 h after NAP administration. Stomach lesions were measured using digital calipers. The medial sm...
Source: Drug Development Research - May 11, 2015 Category: Drugs & Pharmacology Authors: Nathalia S. Carvalho, Mônica M. Silva, Renan O. Silva, Lucas A. D. Nicolau, Francisca Beatriz M. Sousa, Samara R. B. Damasceno, Durcilene A. Silva, André L. R. Barbosa, José Roberto S. A. Leite, Jand Venes R. Medeiros Tags: Research Article Source Type: research
Transformation of acidic poorly water soluble drugs into ionic liquids.
In conclusion, the creation of TBP ionic liquids or solid salts from APIs is a valuable concept addressing dissolution and solubility challenges of poorly water soluble acidic compounds. The data suggested that tailor-made counterions may substantially expand the formulation scientist's armamentarium to meet challenges of poorly water soluble drugs. PMID: 25976317 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 11, 2015 Category: Drugs & Pharmacology Authors: Balk A, Wiest J, Widmer T, Galli B, Holzgrabe U, Meinel L Tags: Eur J Pharm Biopharm Source Type: research
Self-assembly of amphiphilic anionic calixarene and encapsulation of poorly soluble naproxen and flurbiprofen
Org. Biomol. Chem., 2015, Accepted ManuscriptDOI: 10.1039/C5OB00703H, CommunicationAnna Notti, Lucia Barbera, Giuseppe Gattuso, Franz Heinrich Kohnke, Sebastiano Pappalardo, Melchiorre F. Parisi, Ilenia Pisagatti, Salvatore Patane, Norberto Micali, Valentina VillariSupramolecular aggregates formed through the association of an amphiphilic tetra-O-butylsolfonato calixarene 1 were investigated in aqueous solution by a combination of different techniques (NMR, DLS and AFM). The ability of...The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Organic Biomolecular Chemistry)
Source: RSC - Organic Biomolecular Chemistry - May 8, 2015 Category: Molecular Biology Authors: Anna Notti Source Type: research
Efficacy and safety of tanezumab monotherapy or combined with non-steroidal anti-inflammatory drugs in the treatment of knee or hip osteoarthritis pain
Conclusions Subjects receiving partial symptomatic relief of OA pain with NSAIDs may receive greater benefit with tanezumab monotherapy. While only coadministration of tanezumab with NSAIDs met the definition of superiority, combination treatment did not provide important benefits over tanezumab monotherapy; small differences in efficacy were negated by treatment-limiting or irreversible safety outcomes. Trial registration number NCT00809354 (Source: Annals of the Rheumatic Diseases)
Source: Annals of the Rheumatic Diseases - May 8, 2015 Category: Rheumatology Authors: Schnitzer, T. J., Ekman, E. F., Spierings, E. L. H., Greenberg, H. S., Smith, M. D., Brown, M. T., West, C. R., Verburg, K. M. Tags: Pain (neurology), Biological agents, Degenerative joint disease, Drugs: musculoskeletal and joint diseases, Musculoskeletal syndromes, Osteoarthritis Clinical and epidemiological research Source Type: research
Prevalence of potentially inappropriate medicine use in older New Zealanders: a population‐level study using the updated 2012 Beers criteria
ConclusionsThe updated Beers 2012 criteria identified that the use of PIMs at a population level is common in older New Zealanders. (Source: Journal of Evaluation in Clinical Practice)
Source: Journal of Evaluation in Clinical Practice - May 5, 2015 Category: Journals (General) Authors: Sujita W. Narayan, Prasad S. Nishtala Tags: Original Article Source Type: research
Efficacy and tolerability studies evaluating a sleep aid and analgesic combination of naproxen sodium and diphenhydramine in the dental impaction pain model in subjects with induced transient insomnia
ConclusionsOnly the NS 440 mg/DPH 50 mg combination demonstrated improvement in both sleep latency vs. DPH 50 mg and sleep maintenance (WASO) vs. NS 440 mg. There were no serious or unexpected adverse events reported in either study. Clinical Trial Registration: NCT01280591 (study 1); NCT01495858 (study 2) (Source: International Journal of Clinical Practice)
Source: International Journal of Clinical Practice - May 1, 2015 Category: Internal Medicine Authors: S. Cooper, I. Laurora, Y. Wang, P. Venkataraman, R. An, T. Roth Tags: Original Paper Source Type: research
Medication Guide Reading Behaviors and Attitudes Among Subjects With Migraine, Asthma, or COPD
Conclusions: The results provide insights into potential revisions to the medication guides that may improve reading behaviors. (Source: Therapeutic Innovation and Regulatory Science)
Source: Therapeutic Innovation and Regulatory Science - April 30, 2015 Category: Drugs & Pharmacology Authors: Bibeau, K. B., DiSantostefano, R. L., Hinds, D. Tags: Policy Source Type: research
Abstract P5-11-01: Correlation of the effects of potential and known chemopreventive agents on proliferation rates in normal mammary glands and mammary cancers with their chemopreventive efficacy
In conclusion, determining the effect of a potential chemopreventive agent on cell proliferation following short-term treatment appears to be an effective method for predicting its efficacy in preventing mammary cancers. These data further confirm that Ki67 measurements are useful in Phase II prevention trials as a biomarker of agent efficacy. Citation Format: Brandy M Heckman-Stoddard, Clinton J Grubbs, Fariba Moeinpour, Vernon E Steele, Ronald A Lubet. Correlation of the effects of potential and known chemopreventive agents on proliferation rates in normal mammary glands and mammary cancers with their chemopreventive eff...
Source: Cancer Research - April 30, 2015 Category: Cancer & Oncology Authors: Heckman-Stoddard, B. M., Grubbs, C. J., Moeinpour, F., Steele, V. E., Lubet, R. A. Tags: Poster Session Abstracts Source Type: research
Polymer strip films as a robust, surfactant-free platform for delivery of BCS Class II drug nanoparticles
Publication date: 15 July 2015 Source:International Journal of Pharmaceutics, Volume 489, Issues 1–2 Author(s): Scott M. Krull , Ramana Susarla , Afolawemi Afolabi , Meng Li , Ye Ying , Zafar Iqbal , Ecevit Bilgili , Rajesh N. Davé The robustness of the polymer strip film platform to successfully deliver a variety of BCS Class II drug nanoparticles without the need for surfactant while retaining positive characteristics such as nanoparticle redispersibility and fast dissolution is demonstrated. Fenofibrate (FNB), griseofulvin (GF), naproxen (NPX), phenylbutazone (PB), and azodicarbonamide (AZD) were considered as mode...
Source: International Journal of Pharmaceutics - April 29, 2015 Category: Drugs & Pharmacology Source Type: research
Formulation and process optimization of naproxen nanosuspensions stabilized by hydroxy propyl methyl cellulose
Publication date: 20 August 2015 Source:Carbohydrate Polymers, Volume 127 Author(s): Bibaswan Mishra , Jagannath Sahoo , Prasanna Kumar Dixit In present study precipitation–ultrasonication was used to obtain nanosuspensions of poorly water-soluble drug, naproxen (NPX). We investigated the effects of HPMC concentration (X1) and time of ultrasonication (X2) on imperative attributes like mean particle size (Y1), % drug content (Y2), and time required to 90% drug release (Y3) via 32 factorial design. The morphology of nanosuspensions was found almost spherical by SEM observation. DSC and XRD studies suggested slight crysta...
Source: Carbohydrate Polymers - April 17, 2015 Category: Biomedical Science Source Type: research
Model‐based prediction of the acute and long‐term safety profile of naproxen in rats
Conclusions and ImplicationsThese results show that the use of a model‐based approach provides the opportunity to integrate pharmacokinetics, pharmacodynamics and toxicity data, enabling optimisation of the design, analysis and interpretation of toxicology experiments. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - April 17, 2015 Category: Drugs & Pharmacology Authors: Tarjinder Sahota, Ian Sanderson, Meindert Danhof, Oscar Della Pasqua Tags: Research Paper Source Type: research
Consistency of Response to Sumatriptan/Naproxen Sodium in a Randomized Placebo‐Controlled, Cross‐Over Study for the Acute Treatment of Migraine in Adolescence
The objective of this study was to examine the efficacy of S/NS vs placebo in the primary end‐points of pain‐free response at 2 hours (2hPF), 24‐hour sustained pain‐free response (24hPF), and pain‐free response at 2 hours with early intervention (2hPFE) calculated as percentage out of all attacks. In the study, 94 subjects treated 347 attacks in total: treating 277 with S/NS and 70 with placebo. Compared with placebo, S/NS produced higher 2hPF rates (S/NS 37%, placebo 18%; P < .004), and 2hPFE with rates (S/NS 32%, 18% placebo; P < .03). Compared with placebo, 24hPF rates were S/NS 86%, placebo 78%,...
Source: Headache: The Journal of Head and Face Pain - April 17, 2015 Category: Neurology Authors: Paul Winner, Steven Linder, Andrew D. Hershey Tags: Research Submission Source Type: research
Comment on “Purity Analysis of the Pharmaceuticals
Naproxen and Propranolol: A Guided-Inquiry Laboratory Experiment in
the Analytical Chemistry Laboratory”
Journal of Chemical EducationDOI: 10.1021/acs.jchemed.5b00133 (Source: Journal of Chemical Education)
Source: Journal of Chemical Education - April 16, 2015 Category: Chemistry Authors: Alan M. Rosan Source Type: research
Deciphering the Pathogenesis of NSAID-Enteropathy Using Proton Pump Inhibitors and a Hydrogen Sulfide-Releasing NSAID.
Abstract 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. 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 ...
Source: American Journal of Physiology. Gastrointestinal and Liver Physiology - April 16, 2015 Category: Physiology Authors: Blackler RW, De Palma G, Manko A, Da Silva GJ, Flannigan KL, Bercik P, Surette MG, Buret AG, Wallace JL Tags: Am J Physiol Gastrointest Liver Physiol Source Type: research