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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
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
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
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
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
Acute Migraine Treatment in Adults
This study aims to review current medical office‐based acute migraine therapy in adults and provides readers with an organized approach to this important facet of migraine treatment. A general literature review includes a review of several recent published guidelines. Acetaminophen, 4 nonsteroidal anti‐inflammatory drugs (NSAIDs) (ibuprofen, acetylsalicylic acid [ASA], naproxen sodium, and diclofenac potassium), and 7 triptans (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan) have good evidence for efficacy and form the core of acute migraine treatment. NSAID–triptan com...
Source: Headache: The Journal of Head and Face Pain - April 15, 2015 Category: Neurology Authors: Werner J. Becker Tags: Review Article Source Type: research
Hydrogel with a basic instinct for drug delivery
Gel that releases naproxen in alkaline surroundings is promising step toward relieving drug’s side effects (Source: Chemistry World | Latest News)
Source: Chemistry World | Latest News - April 15, 2015 Category: Chemistry Authors: Christopher Barnard Source Type: research
Acute Migraine Treatment in Adults.
This study aims to review current medical office-based acute migraine therapy in adults and provides readers with an organized approach to this important facet of migraine treatment. A general literature review includes a review of several recent published guidelines. Acetaminophen, 4 nonsteroidal anti-inflammatory drugs (NSAIDs) (ibuprofen, acetylsalicylic acid [ASA], naproxen sodium, and diclofenac potassium), and 7 triptans (almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan) have good evidence for efficacy and form the core of acute migraine treatment. NSAID-triptan combinati...
Source: Headache - April 15, 2015 Category: Neurology Authors: Becker WJ Tags: Headache Source Type: research
Pharmaceuticals and iodinated contrast media in a hospital wastewater: A case study to analyse their presence and characterise their environmental risk and hazard.
Abstract This work analyses the presence of twenty-five pharmaceutical compounds belonging to seven different therapeutic groups and one iodinated contrast media (ICM) in a Spanish medium-size hospital located in the Valencia Region. Analysis of the target compounds in the hospital wastewater was performed by means of solid phase extraction (SPE) followed by liquid chromatography-tandem mass spectrometry analysis (HPLC-MS/MS). A screening level risk assessment combining the measured environmental concentrations (MECs) with dose-response data based on Predicted No Effect Concentration (PNEC) was also applied to esti...
Source: Environmental Research - April 10, 2015 Category: Environmental Health Authors: Mendoza A, Aceña J, Pérez S, López de Alda M, Barceló D, Gil A, Valcárcel Y Tags: Environ Res Source Type: research
Alexia with agraphia as a rare presentation of migraine (P1.309)
CONCLUSIONS:This represents the first-ever case report of alexia with agraphia presenting as migraine aura. The pathophysiology of cortical spreading depression within migraine auras easily supports cortical dysfunction of the angular gyrus preceding or during a migraine attack.Disclosure: Dr. Suhaib has nothing to disclose. Dr. Vaughn has received personal compensation for activities with various multiple sclerosis surveys. (Source: Neurology)
Source: Neurology - April 8, 2015 Category: Neurology Authors: Suhaib, O., Vaughn, A. Tags: Headache I Source Type: research
Individual non-steroidal anti-inflammatory drugs and risk of acute kidney injury: A systematic review and meta-analysis of observational studies.
CONCLUSION: A statistically significant elevated AKI risk among traditional NSAID users has been demonstrated in this meta-analysis. The pooled risk ratios among individual traditional NSAIDs were not significantly different. The pooled risk ratios of specific COX-2 inhibitors and the two traditional NSAIDs with the most COX-2 selectivity (diclofenac and meloxicam) were also comparable with other traditional NSAIDs even though they did not achieve a statistical significance. PMID: 25862494 [PubMed - as supplied by publisher] (Source: European Journal of Internal Medicine)
Source: European Journal of Internal Medicine - April 7, 2015 Category: Internal Medicine Authors: Ungprasert P, Cheungpasitporn W, Crowson CS, Matteson EL Tags: Eur J Intern Med Source Type: research
NSAIDs and spontaneous abortions – true effect or an indication bias?
ConclusionsThe increased use of NSAIDs during the last few days that preceded a spontaneous abortion to relieve pain associated with the miscarriage could bias studies assessing the association between exposure to NSAIDs and spontaneous abortions. (Source: British Journal of Clinical Pharmacology)
Source: British Journal of Clinical Pharmacology - April 6, 2015 Category: Drugs & Pharmacology Authors: Sharon Daniel, Gideon Koren, Eitan Lunenfeld, Amalia Levy Tags: Methods in clinical pharmacology Source Type: research
Ictal adipokines are associated with pain severity and treatment response in episodic migraine
Conclusions: Both pretreatment migraine pain severity and treatment response are associated with changes in adipokine levels. Adipokines represent potential novel migraine biomarkers and drug targets. (Source: Neurology)
Source: Neurology - April 6, 2015 Category: Neurology Authors: Chai, N. C., Gelaye, B., Tietjen, G. E., Dash, P. D., Gower, B. A., White, L. W., Ward, T. N., Scher, A. I., Peterlin, B. L. Tags: Migraine, All Pain ARTICLE Source Type: research
Optimization and dissolution performance of spray-dried naproxen nano-crystals
Publication date: 30 May 2015 Source:International Journal of Pharmaceutics, Volume 486, Issues 1–2 Author(s): Sumit Kumar , Jie Shen , Banu Zolnik , Nakissa Sadrieh , Diane J. Burgess The purpose of this study was to investigate the in vitro dissolution performance of the different sized spray-dried nano-crystalline powders of naproxen. A DoE approach was used to formulate and optimize nano-crystalline suspensions. The critical wet milling operation parameters were i.e., drug concentration, drug-to-stabilizer ratio, stabilizer type (HPMC E15 or Tween 80) and milling intensity. The nano-crystalline suspensions were opt...
Source: International Journal of Pharmaceutics - April 6, 2015 Category: Drugs & Pharmacology Source Type: research
Oral analgesia for relieving post-caesarean pain.
CONCLUSIONS: Eight trials with 962 women were included in the analysis, but only four trials were of high quality. All the trials were small. We carried out subgroup analysis for different drugs within the same group and for high versus low doses of the same drug. However, the relatively few studies (one to two trials) and numbers of women (40 to 136) limits the reliability of these subgroup analyses.Due to limited data available no conclusions can be made regarding the safest and the most effective form of oral analgesia for post-caesarean pain. Further studies are necessary. PMID: 25821010 [PubMed - in process] (Sour...
Source: Cochrane Database of Systematic Reviews - April 2, 2015 Category: Journals (General) Authors: Mkontwana N, Novikova N Tags: Cochrane Database Syst Rev Source Type: research
Is Ultrasound Guidance Needed for Shoulder Injections?
MJ is a 44-year-old teacher who has had right lateral shoulder pain for 5 weeks. The pain developed acutely after he played a pickup game of basketball. He initially presented to his primary care physician, who suspected an acute rotator cuff injury and prescribed naproxen, 500 mg twice daily, along with physical therapy. MJ has completed 4 weeks of appropriate therapy focusing on scapular retraction exercise, pectoralis stretching, and rotator cuff strengthening. He experienced no relief from the therapy or medication, so his primary care physician obtained a shoulder magnetic resonance (MR) arthrogram, which demonstrated...
Source: PM and R - April 1, 2015 Category: Rehabilitation Authors: Jonathan T. Finnoff, John G. Costouros, David J. Kennedy Tags: Point/Counterpoint Source Type: research
Naproxen Prevention of Urinary Bladder Cancer
The COX inhibitors (NSAID/Coxibs) are a major focus for the chemoprevention of cancer. The COX-2–specific inhibitors have progressed to clinical trials and have shown preventive efficacy in colon and skin cancers. However, they have significant adverse cardiovascular effects. Certain NSAIDs (e.g., naproxen) have a good cardiac profile, but can cause gastric toxicity. The present study examined protocols to reduce this toxicity of naproxen. Female Fischer-344 rats were treated weekly with the urinary bladder–specific carcinogen hydroxybutyl(butyl)nitrosamine (OH-BBN) for 8 weeks. Rats were dosed daily with NPX (...
Source: Cancer Prevention Research - March 31, 2015 Category: Cancer & Oncology Authors: Lubet, R. A., Scheiman, J. M., Bode, A., White, J., Minasian, L., Juliana, M. M., Boring, D. L., Steele, V. E., Grubbs, C. J. Tags: Research Articles Source Type: research
(401) Analgesic effectiveness of a new, extended-release ibuprofen in postoperative dental pain
Analgesic effects of an immediate-release/extended-release (IR/ER) 600 mg formulation of ibuprofen (IBU) with q12h dosing were evaluated in 2 single-center, randomized, double-blind, placebo-controlled dental pain studies (Study 1: single dose, 24-hour study; Study 2: multiple doses, 48-hour study). Subjects aged 16–40 years with at least moderate pain following third molar extraction received single doses of 2 IBU 600 mg IR/ER formulations (A or B), naproxen sodium (NAP) 220 mg, or placebo (2:2:2:1 ratio) in Study 1; 4 doses IBU 600 mg IR/ER or placebo (1:1 ratio) in Study 2. (Source: The Journal of Pain)
Source: The Journal of Pain - March 27, 2015 Category: Materials Science Authors: S. Christensen, S. Meeves, S. Jayawardena, S. Daniels, E. Paluch Source Type: research
Influence of excipients on solubility and dissolution of pharmaceuticals
Publication date: 15 May 2015 Source:International Journal of Pharmaceutics, Volume 485, Issues 1–2 Author(s): Raphael Paus , Anke Prudic , Yuanhui Ji In this work, solubilities and dissolution profiles of the active pharmaceutical ingredients (APIs) indomethacin and naproxen were measured in water in the presence of one excipient out of polyethylene glycol (PEG) 2000, 6000 and 12000, polyvinylpyrrolidone (PVP) K 25 and mannitol. It was found that the solubility of indomethacin and naproxen was increased with an addition of the selected excipients, which was also predicted by the perturbed-chain statistical associating...
Source: International Journal of Pharmaceutics - March 27, 2015 Category: Drugs & Pharmacology Source Type: research
A multiresidue liquid chromatographic/tandem mass spectrometric method for the detection and quantitation of 15 nonsteroidal anti-inflammatory drugs (NSAIDs) in bovine meat and milk.
This study concerns a validated liquid chromatographic/tandem mass spectrometric (LC-MS/MS) multiresidue method for the simultaneous detection, identification, and quantitation of 15 nonsteroidal anti-inflammatory drugs (NSAIDs) in bovine meat and milk. The NSAIDs considered are carprofen, diclofenac, flufenamic acid, flunixin (5-hydroxyflunixin as marker metabolite in milk), ketoprofen, mefenamic acid, meloxicam, 4-methylaminoantipyrine (marker metabolite of metamizole in meat and milk), naproxen, niflumic acid, phenylbutazone (and metabolite oxyphenbutazone), ramifenazone, salicylic acid, and tolfenamic acid. These compo...
Source: Analytical and Bioanalytical Chemistry - March 27, 2015 Category: Chemistry Authors: van Pamel E, Daeseleire E Tags: Anal Bioanal Chem Source Type: research
Modulation of intestinal afferent nerve sensitivity to inflammatory mediators following systemic endotoxin in mice
Conclusions & InferencesSystemic endotoxin sensitizes mesenteric afferent nerve fibers to 5‐HT, BK and mechanical stimuli. The underlying mechanism responsible for this sensitization seems to involve mast cells and the COX‐2 pathway. Endotoxin sensitizes intestinal afferent nerves in mice in vitro to 5‐HT, bradykinin and mechanical ramp distension. This sensitization was dependent on mast cells and the COX‐2 but not to the COX‐1 pathway. (Source: Neurogastroenterology and Motility)
Source: Neurogastroenterology and Motility - March 26, 2015 Category: Gastroenterology Authors: B. Xue, M. S. Kasparek, M. H. Müller, M. E. Kreis Tags: Original Article Source Type: research
Characterization of the comparative drug binding to intra- (liver fatty acid binding protein) and extra- (human serum albumin) cellular proteins.
This study compared the extent, affinity, and kinetics of drug binding to human serum albumin (HSA) and liver fatty acid binding protein (LFABP) using ultrafiltration and surface plasmon resonance (SPR). 2. Binding of basic and neutral drugs to both HSA and LFABP was typically negligible. Binding of acidic drugs ranged from minor (fu > 0.8) to extensive (fu < 0.1). Of the compounds screened, the highest binding to both HSA and LFABP was observed for the acidic drugs torsemide and sulfinpyrazone, and for β-estradiol (a polar, neutral compound). 3. The extent of binding of acidic drugs to HSA was up to 40%...
Source: Xenobiotica - March 24, 2015 Category: Research Authors: Rowland A, Hallifax D, Nussio MR, Shapter JG, Mackenzie PI, Brian Houston J, Knights KM, Miners JO Tags: Xenobiotica Source Type: research
Formulation and evaluation of ileo-colonic targeted matrix-mini-tablets of Naproxen for Chronotherapeutic treatment of Rheumatoid Arthritis
Publication date: Available online 20 March 2015 Source:Saudi Pharmaceutical Journal Author(s): Mohd Abdul Hadi , N.G. Raghavendra Rao , A Srinivasa Rao In this present research work, the aim was to develop ileo-colonic targeted matrix-mini-tablets-filled capsule system of Naproxen for chronotherapeutic treatment of Rheumatoid Arthritis. So Matrix-mini-tablets of Naproxen were prepared using microsomal enzyme dependent and pH-sensitive polymers by direct compression method which were further filled into an empty HPMC capsule. The compatibility was assessed using FT-IR and DSC studies for pure drug, polymers and their phy...
Source: Saudi Pharmaceutical Journal - March 21, 2015 Category: Drugs & Pharmacology Source Type: research
Characterization of naproxen-loaded solid SMEDDSs prepared by spray drying: The effect of the polysaccharide carrier and naproxen concentration
Publication date: 15 May 2015 Source:International Journal of Pharmaceutics, Volume 485, Issues 1–2 Author(s): Katja Čerpnjak , Alenka Zvonar , Franc Vrečer , Mirjana Gašperlin The purpose of this study was to prepare solid SMEDDS (sSMEDDS) particles produced by spray-drying using maltodextrin (MD), hypromellose (HPMC), and a combination of the two as a solid carrier. Naproxen (NPX) as the model drug was dissolved (at 6% concentration) or partially suspended (at 18% concentration) in a liquid SMEDDS composed of Miglyol® 812, Peceol™, Gelucire® 44/14, and Solutol® HS 15. Among the sSMEDDSs tested, the MD-based s...
Source: International Journal of Pharmaceutics - March 19, 2015 Category: Drugs & Pharmacology Source Type: research
Relative benefit-risk comparing diclofenac to other traditional non-steroidal anti-inflammatory drugs and cyclooxygenase-2 inhibitors in patients with osteoarthritis or rheumatoid arthritis: a network meta-analysis
Conclusions: The benefit-risk profile of diclofenac was comparable to other treatments used for pain relief in OA and RA; benefits and risks vary in individuals and need consideration when making treatment decisions. (Source: Arthritis Research and Therapy)
Source: Arthritis Research and Therapy - March 19, 2015 Category: Rheumatology Authors: Anneloes van WalsemShaloo PandhiRichard NixonPatricia GuyotAndreas KarabisR Moore Source Type: research
Relationship Between Structural Alerts in NSAIDs and Idiosyncratic Hepatotoxicity: An Analysis of Spontaneous Report Data from the WHO Database
Conclusions This study shows that although spontaneous reports have many limitations, the findings are in line with previous research on the reactive metabolite concept. Whether SAs and the number of SAs in the NSAIDs actually play a role in the observed hepatotoxicity must be investigated in future studies. (Source: Drug Safety)
Source: Drug Safety - March 19, 2015 Category: Drugs & Pharmacology Source Type: research
Changes in the solid state of anhydrous and hydrated forms of sodium naproxen under different grinding and environmental conditions: Evidence of the formation of new hydrated forms.
Abstract The aim of the present work was to investigate the solid state change of the anhydrous and hydrate solid forms of sodium naproxen under different grinding and environmental conditions. Grinding was carried out manually in a mortar under the following conditions: at room temperature under air atmosphere (Method A), in the presence of liquid nitrogen under air atmosphere (Method B), at room temperature under nitrogen atmosphere (Method C), and in presence of liquid nitrogen under nitrogen atmosphere (Method D). Among the hydrates, the following forms were used: a dihydrate form (DSN) obtained by exposing the...
Source: European Journal of Pharmaceutics and Biopharmaceutics - March 18, 2015 Category: Drugs & Pharmacology Authors: Censi R, Rascioni R, Martino PD Tags: Eur J Pharm Biopharm Source Type: research
Using gait analysis to assess weight bearing in rats with Freund's complete adjuvant-induced monoarthritis to improve predictivity: Interfering with the cyclooxygenase and nerve growth factor pathways.
Abstract Lack of predictive power for drug effects has been a major criticism against animal pain models. It is therefore important to define the utility and limitations of different models. The aim of this study was to extend previous work on gait analysis as a tool to investigate pharmacological effects in monoarthritic rats, specifically to test the hypothesis that monoarthritis induced by Freund's complete adjuvant (FCA) provides a better estimate of overall analgesic efficacy of established, and novel, clinically effective and ineffective therapeutic approaches. Male rats injected intra-articularly into one an...
Source: European Journal of Pharmacology - March 16, 2015 Category: Drugs & Pharmacology Authors: Ängeby Möller K, Berge OG, Finn A, Stenfors C, Svensson CI Tags: Eur J Pharmacol Source Type: research
Effects of various factors of ultrasonic treatment on the extraction recovery of drugs from fish tissues.
Abstract In the present research, a combined extraction method of ultrasound-assisted extraction (UAE) in conjunction with solid phase extraction (SPE) was applied to isolation and enrichment of selected drugs (metoprolol, ticlopidine, propranolol, carbamazepine, naproxen, acenocumarol, diclofenac, ibuprofen) from fish tissues. The extracted analytes were separated and determined by ultra-high performance liquid chromatography with UV detection (UHPLC-UV) technique. The selectivity of the developed UHPLC-UV method was confirmed by comparison with ultra-high performance liquid chromatography-tandem mass spectrometry...
Source: Ultrasonics Sonochemistry - March 12, 2015 Category: Chemistry Authors: Magiera S, Pardylla A, Baranowska I Tags: Ultrason Sonochem Source Type: research
Characterization of the anti-inflammatory properties of NCX 429, a dual-acting compound releasing nitric oxide and naproxen
Publication date: 1 April 2015 Source:Life Sciences, Volume 126 Author(s): Angela Amoruso , Luigia Grazia Fresu , Jesmond Dalli , Daniela Miglietta , Claudio Bardelli , Donata Federici Canova , Mauro Perretti , Sandra Brunelleschi Aims Cyclooxygenase (COX)-inhibiting nitric oxide donors (CINODs) are a new class of drugs that structurally combine a COX inhibitor with a nitric oxide (NO) donating moiety. This combination reduces potential toxicity of the non-steroidal anti-inflammatory drugs (NSAIDs) whilst maintaining the analgesic and anti-inflammatory effects. The present study was undertaken to investigate the anti-inf...
Source: Life Sciences - March 11, 2015 Category: Biology Source Type: research
Process Parameter Dependent Growth Phenomena during the Fine Grinding of Naproxen in a Planetary Ball Mill.
Abstract The production of nanosuspensions has proved to be an effective method for overcoming bioavailability challenges of poorly water soluble drugs. Wet milling in stirred media mills and planetary ball mills has become an established top-down-method for producing such drug nanosuspensions. The quality of the resulting nanosuspension is determined by the stability against agglomeration on the one hand, and the process parameters of the mill on the other hand. In order to understand the occurring dependencies, a detailed screening study, not only on adequate stabilizers, but also on their optimum concentration w...
Source: European Journal of Pharmaceutics and Biopharmaceutics - March 9, 2015 Category: Drugs & Pharmacology Authors: Bitterlich A, Laabs C, Krautstrunk I, Dengler M, Juhnke M, Grandeury A, Bunjes H, Kwade A Tags: Eur J Pharm Biopharm Source Type: research
Fabric phase sorptive extraction: A new sorptive microextraction technique for the determination of non-steroidal anti-inflammatory drugs from environmental water samples.
Abstract Fabric phase sorptive extraction (FPSE) is a new, yet very promising member of the sorbent-based sorptive microextraction family. It has simultaneously improved both the extraction sensitivity and the speed of the extraction by incorporating high volume of sol-gel hybrid inorganic-organic sorbents into permeable fabric substrates. The advantages of FPSE have been investigated for the determination of four non-steroidal anti-inflammatory drugs, ibuprofen, naproxen, ketoprofen and diclofenac, in environmental water samples in combination with gas chromatography-mass spectrometry. Initially, the significance ...
Source: Analytica Chimica Acta - March 7, 2015 Category: Chemistry Authors: Racamonde I, Rodil R, Quintana JB, Sieira BJ, Kabir A, Furton KG, Cela R Tags: Anal Chim Acta Source Type: research
Anomalous Role Change of Tertiary Amino and Ester
Groups as Hydrogen Acceptors in Eudragit E Based Solid Dispersion
Depending on the Concentration of Naproxen
Molecular PharmaceuticsDOI: 10.1021/mp5005417 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - March 3, 2015 Category: Drugs & Pharmacology Authors: Hiroshi Ueda, Shinobu Wakabayashi, Junko Kikuchi, Yasuo Ida, Kazunori Kadota and Yuichi Tozuka Source Type: research
Follow-up evaluation of cognitive function in the randomized Alzheimer's Disease Anti-inflammatory Prevention Trial and its Follow-up Study
Conclusions Treatment for 1 to 3 years with naproxen or celecoxib did not protect against cognitive decline in older adults with a family history of AD. (Source: Alzheimer's and Dementia: The Journal of the Alzheimer's Association)
Source: Alzheimer's and Dementia: The Journal of the Alzheimer's Association - March 2, 2015 Category: Geriatrics Source Type: research
[Cardiovascular safety of non-steroidal anti-inflammatory drugs].
Abstract BACKGROUND The selective cyclooxygenase (COX)-2 inhibitor rofecoxib was withdrawn from the market in 2004 due to cardiovascular toxicity. We have evaluated data on adverse cardiovascular effects caused by COX-2 inhibitors and other non-steroidal anti-inflammatory drugs (NSAIDs) since 2004.MATERIAL AND METHOD Searches in PubMed (2004-2014) identified 243 relevant articles. Following a selection process, 63 articles were reviewed and evaluated in light of Norwegian practice.RESULTS The results from the studies reviewed are heterogenous. A majority of data indicate that all the selective COX-2 inhibitors, dic...
Source: Tidsskrift for den Norske Laegeforening - March 1, 2015 Category: Journals (General) Authors: Møllersen MV, Norgård H, Spigset O, Slørdal L Tags: Tidsskr Nor Laegeforen Source Type: research
Intravenous lipid emulsion therapy in three cases of canine naproxen overdose
Abstract ObjectiveTo report a case series of canine naproxen overdoses successfully treated with intravenous lipid emulsion therapy (IVLE). Series SummaryThree dogs were presented for acute ingestion of naproxen and were treated with IVLE. Baseline and post treatment serum naproxen concentrations were measured. The first exposure involved ingestion of 61 mg/kg of an over‐the‐counter naproxen formulation in a 7‐month‐old male intact Labrador Retriever. Pre‐IVLE toxin concentration assessed by high performance liquid chromatography (HPLC) was 73 μg/mL with a one‐hour post‐IVLE concentration decreasing to 30 μ...
Source: Journal of Veterinary Emergency and Critical Care - March 1, 2015 Category: Veterinary Research Authors: Jennifer M. Herring, Maureen A. McMichael, Raffaella Corsi, Virginie Wurlod Tags: Case Series Source Type: research
The H 2 S-releasing naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with ligature-induced periodontitis
Conclusion The H2S-releasing moiety in the ATB-346 compound not only does not impair the effects of the parent naproxen on periodontitis, but also improves bone quality and prevents the gastric mucosa damage due to prostaglandin inhibition, thus configuring a potentially new adjuvant therapy for periodontal diseases. (Source: Medical Gas Research)
Source: Medical Gas Research - February 27, 2015 Category: Biomedical Science Source Type: research