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Yu-Ting Cheng, Chi-Cheng Lu, Gow-Chin Yen
The gastrointestinal mucosa provides the first protective barrier for digested food and xenobiotics, which are easily attacked by toxic substances. Non-steroidal anti-inflammatory drugs (NSAIDs), including aspirin, diclofenac, indomethacin, and ketoprofen, are widely used in clinical medicine, but these drugs may cause oxidative stress, leading to gastrointestinal damage, such as ulcers. Lansoprazol, omeprazole, and other clinical drugs are widely used to treat duodenal and gastric ulcers and haven been shown to have multiple biological functions, such as antioxidant activity and the ability to upregulate antioxidant enzymes in vivo...
November 24, 2016: Molecular Nutrition & Food Research
Alejo J Nevado-Holgado, Simon Lovestone
Alzheimer's disease (AD) represents a substantial unmet need, due to increasing prevalence in an ageing society and the absence of a disease modifying therapy. Epidemiological evidence shows a protective effect of non steroidal anti inflammatory (NSAID) drugs, and genome wide association studies (GWAS) show consistent linkage to inflammatory pathways; both observations suggesting anti-inflammatory compounds might be effective in AD therapy although clinical trials to date have not been positive. In this study, we use pathway enrichment and fuzzy logic to identify pathways (KEGG database) simultaneously affected in both AD and by NSAIDs (Sulindac, Piroxicam, Paracetamol, Naproxen, Nabumetone, Ketoprofen, Diclofenac and Aspirin)...
2017: Computational and Structural Biotechnology Journal
Miguel Peñín-Ibáñez, María Jesús Santos-Delgado, Luis María Polo-Díez
A two-dimensional achiral-chiral LC-LC method in heart-cut mode for ketoprofen and its enantiomeric fraction determination was proposed. A C8 column was used in the first dimension, and the chiral column was an α1-acid glycoprotein. The mobile phase of the chiral system was optimized by a factorial design. The effect of temperature on retention and on enantiomeric resolution was studied. Particular attention was paid to mobile phase compatibility for the two columns and to transferring time, using ketoprofen standards...
November 19, 2016: Analytical and Bioanalytical Chemistry
Sertac Guler, Ilyas Ertok, Nurdan Yilmaz Sahin, Hayri Ramadan, Yavuz Katirci
Dexketoprofen trometamol (DT), a nonsteroidal anti-inflammatory drug, is a highly water-soluble salt and active enantiomer of rac-ketoprofen. Its parenteral form is commonly used for acute pain management in emergency departments of our country. Side effects such as diarrhea, indigestion, nausea, stomach pain, and vomiting may be seen after the use of DT. Anaphylactic shock (AS) secondary to infusion of DT is very rare and, to our knowledge, it is the first case report describing this side effect. This case report was presented to emphasize that AS may be seen after the use of DT...
September 2016: Turkish Journal of Emergency Medicine
Hamed Hamishehkar, Soheila Hosseini, Abdolhossein Naseri, Azam Safarnejad, Farzaneh Rasoulzadeh
Introduction: The drug-plasma protein interaction is a fundamental issue in guessing and checking the serious drug side effects related with other drugs. The purpose of this research was to study the interaction of cephalexin with bovine serum albumin (BSA) and displacement reaction using site probes. Methods: The interaction mechanism concerning cephalexin (CPL) with BSA was investigated using various spectroscopic methods and molecular modeling method. The binding sites number, n, apparent binding constant, K, and thermodynamic parameters, ΔG(0), ΔH(0), and ΔS(0) were considered at different temperatures...
2016: BioImpacts: BI
I Aparici-Espert, M C Cuquerella, C Paris, V Lhiaubet-Vallet, M A Miranda
Using a sunscreen-based photocage, we have demonstrated that it is possible to prevent photodegradation of a bioactive compound and to achieve its controlled photorelease. The concept has been proven linking avobenzone, one of the most important UVA blockers, to ketoprofen, which is a representative example of a photosensitive drug.
November 16, 2016: Chemical Communications: Chem Comm
N K Yadav, Sanju Nanda, Gajanand Sharma, O P Katare
Various preclinical/clinical studies support the effectiveness of ketoprofen in periodontitis; however, the literature reveals that novel delivery systems have been less explored for the drug in periodontitis. The current investigation aims to explore the potential of a pro-vesicular approach-based proniosomal drug delivery of ketoprofen for its effectiveness and validation in experimental periodontal disease (EPD). Formulations were developed using I-optimal mixture design. Developed formulations were characterized for entrapment efficiency, vesicle size, and in vitro drug release...
November 14, 2016: AAPS PharmSciTech
María Ramos-Payan, Santiago Maspoch, Andreu Llobera
In this work, the traditional liquid phase microextraction (LPME) has been miniaturized into a microfluidic device (μLPME) where liquid phase microextraction is combined with an HPLC procedure. This integration enables extraction and determination of acid drugs by μLPME and HPLC, respectively. The analytes selected for the test are five widely used non-steroidal anti-inflammatory drugs (NSAIDs): salicylic acid (SAC), ketoprofen (KTP), naproxen (NAX), diclofenac (DIC) and ibuprofen (IBU). They have successfully been detected in biological (urine and saliva) and environmental (lake and river water) samples with excellent clean up, high extraction efficiency and good enrichment factor under stopped-flow conditions...
November 23, 2016: Analytica Chimica Acta
Bhekumuzi P Gumbi, Brenda Moodley, Grace Birungi, Patrick G Ndungu
A method was optimized for derivatization, separation, detection and quantification of salicylic acid, acetylsalicylic acid, nalidixic acid, ibuprofen, phenacetin, naproxen, ketoprofen, meclofenamic acid and diclofenac in surface water using gas chromatography-mass spectrometry. For most of the acidic drugs, recovery was in the range 60-110% and the percent standard deviation was below 15% for the entire method, with limits of detection ranging from 0.041 to 1.614 μg L(-1). The developed method was applied in the analysis of acidic drugs in Umgeni River system, KwaZulu-Natal South Africa...
November 1, 2016: Chemosphere
Xiangju Mao, Man He, Beibei Chen, Bin Hu
By wrapping a porous membrane around the coated stir bar, a novel membrane protected stir bar sorptive extraction (MPSBSE) was proposed to filter out the high molecular weight interferences (such as humic acid), resulting in the analysis of real environmental water samples without filtration or centrifugation. Hydrophilic and hydrophobic membranes were compared and hydrophobic polytetrafluoroethylene (PTFE) membrane impregnated with methanol was employed to protect the C18 coated stir bar. The impregnated methanol improves the transfer of target analytes from sample solution to the pores and lumen of the membrane, and then to the coated stir bar inside...
October 24, 2016: Journal of Chromatography. A
Rohan M Shah, Daniel S Eldridge, Enzo A Palombo, Ian H Harding
Stearic acid-based solid lipid nanoparticles (SLNs) were prepared using the microwave assisted one-pot microemulsions procedure pioneered by our group. In this study, non-steroidal anti-inflammatory drugs (NSAIDs) including indomethacin, ketoprofen and nimesulide were selected as ideal "test" drugs, based on their poor water solubility. The model drugs were incorporated within the SLNs by the microwave-assisted procedure at the time of SLN production. The microwave-produced drug-loaded SLNs were evaluated in terms of their physicochemical characteristics, drug release behavior and their uptake into against A549 cell line (human lung epithelial cells)...
October 24, 2016: International Journal of Pharmaceutics
H Satoh, R Kondo, T Shinoda, S Idaka, K Ishigami, S Shiotani
Recent progress in endoscopic techniques has revealed that non-steroidal anti-inflammatory drugs (NSAIDs) often cause ulcers in the small intestine in humans, but effective therapy is not available at present. In the present study, we investigated the effects of feeding condition and the amount of dietary fiber (DF) in the diet on the formation of gastrointestinal ulcers induced by NSAIDs in dogs. Several types of diets containing various percentages of DF were given to dogs. Indomethacin (1 or 3 mg/kg, p.o...
August 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
Vandit Sardana, Joanna Burzynski, Paul Zalzal
PURPOSE: Topical ketoprofen in Transfersome gel has been used for the alleviation of symptoms in osteoarthritis. Non-steroidal anti-inflammatory drugs (NSAIDs) are associated with various side effects. Topical NSAIDs are known to have a lower side-effect profile when compared with systemic administration. The present systematic review aimed to determine the safety and efficacy of topical ketoprofen in Transfersome gel in knee osteoarthritis (OA). METHODS: A systematic literature review was performed...
October 24, 2016: Musculoskeletal Care
M Mezzelani, S Gorbi, D Fattorini, G d'Errico, M Benedetti, M Milan, L Bargelloni, F Regoli
The aim of the present investigation was to provide new insights on accumulation and possible adverse effects of various non-steroidal anti-inflammatory drugs (NSAIDs) in mussels, Mytilus galloprovincialis, exposed to an environmentally realistic concentration (0.5μg/L) of individual compounds, Acetaminophen (AMP), Diclofenac (DIC), Ibuprofen (IBU), Ketoprofen (KET) or Nimesulide (NIM). The measurement of drugs in mussel tissues was integrated with both functional alterations at cellular level and transcriptomic responses...
November 2016: Aquatic Toxicology
Gemma Amo, José A Cornejo-García, Jesus M García-Menaya, Concepcion Cordobes, M J Torres, Gara Esguevillas, Cristobalina Mayorga, Carmen Martinez, Natalia Blanca-Lopez, Gabriela Canto, Alfonso Ramos, Miguel Blanca, José A G Agúndez, Elena García-Martín
The high-affinity IgE receptor (Fcε RI) is a heterotetramer of three subunits: Fcε RIα, Fcε RIβ, and Fcε RIγ (αβγ2) encoded by three genes designated as FCER1A, FCER1B (MS4A2), and FCER1G, respectively. Recent evidence points to FCERI gene variability as a relevant factor in the risk of developing allergic diseases. Because Fcε RI plays a key role in the events downstream of the triggering factors in immunological response, we hypothesized that FCERI gene variants might be related with the risk of, or with the clinical response to, selective (IgE mediated) non-steroidal anti-inflammatory (NSAID) hypersensitivity...
2016: Frontiers in Pharmacology
O A Shavlovskaya
Lower back pain (LBP) remains an important problem due to its high prevalence. LBP is the fifth in frequency among reasons for seeking treatment, and one of the most common among the chronic pain syndromes. Nonsteroidal anti-inflammatory drugs (NSAIDs) are considered to be the «gold standard» in relieving back pain. In treatment of acute musculoskeletal pain syndromes, special attention is drawn to drugs characterized by high analgesic activity and a short half-life. Among the drugs in this group, dexketoprofen (a derivative of propionic acid), a water-soluble salt of the dextrorotatory enantiomer of ketoprofen, deserves special attention...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Vanessa S S Gonçalves, Ana A Matias, Joana Poejo, Ana T Serra, Catarina M M Duarte
During the development of intranasal drug delivery systems for local/systemic effect or brain targeting, it is necessary to assess its cytotoxicity and drug transport through nasal epithelium. In order to avoid animal experiments or the use of excised tissues, in vitro cell models, such as RPMI 2650 cells, are being preferred during recent years. Nevertheless, the deposition of solid formulations into nasal cell layers with further transepithelial transport rate of drugs has been poorly studied or reported...
October 1, 2016: International Journal of Pharmaceutics
T Guzzo, W Mandaliti, R Nepravishta, A Aramini, E Bodo, I Daidone, M Allegretti, A Topai, M Paci
Inclusion of drugs in cyclodextrins (CDs) is a recognized tool for modifying several properties such as solubility, stability, bioavailability, and so on. The photoreactive behavior of the β-CD/ketoprofen (KP) complex upon UV exposure showed a significant increase in photodecarboxylation, whereas the secondary degradation products by hydroxylation of the benzophenone moiety were inhibited. The results may account for an improvement of KP photophysical properties upon inclusion, thus better fostering its topical use...
October 11, 2016: Journal of Physical Chemistry. B
Yoshihiko Uehara, Yasuhiko Murata, Soichiro Shiga, Yoshio Hosoi
BACKGROUND: It is well known that radiation exposure to the heart and the use of non-steroidal anti-inflammatory drugs (NSAIDs) increase the risk of myocardial infarction (MI). Some NSAIDs are also known to act synergistically with ionizing radiation and have radio-sensitizing effects in radiotherapy. These evidences suggest that NSAIDs may affect the risk of MI after radiation exposure to the heart. In the present study, we investigated effects of NSAIDs on radiation-induced expression of cell adhesion molecules and COX-2, which are associated with inflammation and an increased risk of MI, in human endothelial cells...
October 28, 2016: Biochemical and Biophysical Research Communications
Iman Khalil, Saad E Itani, Zeina Naja, Ahmad Salah Naja, Fouad M Ziade, Jean-Marc Ayoubi, Mariam A El-Rajab, Zoher M Naja
STUDY OBJECTIVE: Compare the effectiveness of nerve stimulator-guided pudendal nerve block (PNB) vs general anesthesia (GA) for anterior and posterior (AP) colporrhaphy in terms of pain relief and analgesic consumption within 24 and 48 hours postoperatively. DESIGN: Prospective randomized trial. PATIENTS: Fifty-seven patients whose ages ranged between 20 and 53 years scheduled to undergo AP colporrhaphy due to the presence of cystorectocele...
November 2016: Journal of Clinical Anesthesia
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