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https://www.readbyqxmd.com/read/28725150/development-and-evaluation-of-ketoprofen-sustained-release-matrix-tablet-using-hibiscus-rosa-sinensis-leaves-mucilage
#1
M Kaleemullah, K Jiyauddin, E Thiban, S Rasha, S Al-Dhalli, S Budiasih, O E Gamal, A Fadli, Y Eddy
Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipient. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. Therefore, Ketoprofen matrix tablets were formulated by employing Hibiscus rosa-sinensis leaves mucilage as natural polymer and HPMC (K100M) as a synthetic polymer to sustain the drug release from matrix system. Direct compression method was used to develop sustained released matrix tablets...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28718961/photodegradation-kinetics-transformation-and-toxicity-prediction-of-ketoprofen-carprofen-and-diclofenac-acid-in-aqueous-solutions
#2
Jian Li, Li-Yun Ma, Lu-Shuang Li, Li Xu
In this study, the photodegradation of three commonly used non-steroidal anti-inflammatory drugs, ketoprofen (KET), carprofen (CAR) and diclofenac acid (DIC), was conducted under UV irradiation. The kinetic results showed that the studied three pharmaceuticals obeyed to the first-order reaction with the decreasing rate constants of 1.54×10(-4) s(-1) , 5.91×10(-5) s(-1) and 7.78×10(-6) s(-1) for CAR, KET and DIC, respectively. Moreover, the main transformation products (TPs) were identified by ion-pair liquid-liquid extraction combined with injection port derivatization-gas chromatography-mass spectrometer and high performance liquidchromatography-quadrupole-time of flight mass spectrometer analysis...
July 18, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28718023/two-year-survey-of-specific-hospital-wastewater-treatment-and-its-impact-on-pharmaceutical-discharges
#3
Laure Wiest, Teofana Chonova, Alexandre Bergé, Robert Baudot, Frédérique Bessueille-Barbier, Linda Ayouni-Derouiche, Emmanuelle Vulliet
It is well known that pharmaceuticals are not completely removed by conventional activated sludge wastewater treatment plants. Hospital effluents are of major concern, as they present high concentrations of pharmaceutically active compounds. Despite this, these specific effluents are usually co-treated with domestic wastewaters. Separate treatment has been recommended. However, there is a lack of information concerning the efficiency of separate hospital wastewater treatment by activated sludge, especially on the removal of pharmaceuticals...
July 17, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28711781/the-nature-of-hydrogen-bonding-interactions-in-nonsteroidal-anti-inflammatory-drugs-revealed-by-polarized-ir-spectroscopy
#4
Barbara Hachuła
The influence of hydrogen-bonding interactions in the solid phase on the IR spectroscopic pattern of the νOH band of nonsteroidal anti-inflammatory drugs (NSAIDs) was studied experimentally by IR spectroscopy with the use of polarized light at two temperatures (293K and 77K) and in isotopic dilution. The neat and deuterated crystals of (S)-naproxen ((S)-NPX), (R)-flurbiprofen ((R)-FBP), (RS)-flurbiprofen ((RS)-FBP) and (RS)-ketoprofen ((RS)-KTP) were obtained by melt crystallization between the two squeezed CaF2 plates...
July 9, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28710861/differential-protein-modulation-by-ketoprofen-and-ibuprofen-underlines-different-cellular-response-by-gastric-epithelium
#5
L Brandolini, M d'Angelo, A Antonosante, S Villa, L Cristiano, V Castelli, E Benedetti, M Catanesi, A Aramini, A Luini, S Parashuraman, E Mayo, A Giordano, A Cimini, M Allegretti
Ketoprofen L-lysine salt (KLS), is widely used due to its analgesic efficacy and tolerability, and L-lysine was reported to increase the solubility and the gastric tolerance of ketoprofen. In a recent report, L-lysine salification has been shown to exert a gastroprotective effect due to its specific ability to counteract the NSAIDs-induced oxidative stress and up-regulate gastroprotective proteins. In order to derive further insights into the safety and efficacy profile of KLS, in this study we additionally compared the effect of lysine and arginine, another amino acid counterion commonly used for NSAIDs salification, in control and in ethanol challenged human gastric mucosa model...
July 15, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28687530/comparison-of-segmental-dependent-permeability-in-human-and-in-situ-perfusion-model-in-rat
#6
Ruiz-Picazo Alejandro, Lozoya-Agullo Isabel, Ortiz-Azcarate Miguel, Merino-Sanjuán Matilde, González-Álvarez Marta, González-Álvarez Isabel, Bermejo Marival
Nowadays, alternative methods have been developed to predict intestinal permeability values in human as in vitro, in situ or ex vivo methods. They were developed by the necessity to avoid the problems of the human permeability experiments. However, determination of human permeability is needed to properly validate the alternative methods. For this reason, recently, Dahlgren et al. published an indirect method based on a deconvolution technique to estimate the human permeability in different gastrointestinal segments (jejunum, ileum and colon)...
July 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28687046/formulation-and-in-vitro-in-vivo-evaluation-of-chitosan-based-film-forming-gel-containing-ketoprofen
#7
Dong-Won Oh, Ji-Hyun Kang, Hyo-Jung Lee, Sang-Duk Han, Min-Hyung Kang, Yie-Hyuk Kwon, Joon-Ho Jun, Dong-Wook Kim, Yun-Seok Rhee, Ju-Young Kim, Eun-Seok Park, Chung-Woong Park
The film forming gel, adhered to skin surfaces upon application and formed a film, has an advantage onto skin to provide protection and continuous drug release to the application site. This study aimed to prepare a chitosan-based film forming gel containing ketoprofen (CbFG) and to evaluate the CbFG and film from CbFG (CbFG-film). CbFG were prepared with chitosan, lactic acid and various skin permeation enhancers. The physicochemical characteristics were evaluated by texture analysis, viscometry, SEM, DSC, XRD and FT-IR...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28686186/development-of-a-new-microextraction-fiber-combined-to-on-line-sample-stacking-capillary-electrophoresis-uv-detection-for-acidic-drugs-determination-in-real-water-samples
#8
Maria Espina-Benitez, Lilia Araujo, Avismelsi Prieto, Alberto Navalón, José Luis Vílchez, Paola Valera, Ana Zambrano, Vincent Dugas
A new analytical method coupling a (off-line) solid-phase microextraction with an on-line capillary electrophoresis (CE) sample enrichment technique was developed for the analysis of ketoprofen, naproxen and clofibric acid from water samples, which are known as contaminants of emerging concern in aquatic environments. New solid-phase microextraction fibers based on physical coupling of chromatographic supports onto epoxy glue coated needle were studied for the off-line preconcentration of these micropollutants...
July 7, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28667742/gingival-bleeding-a-possible-serious-adverse-drug-reaction-an-observational-study-in-the-french-pharmacovigilance-database
#9
Emmanuelle Bondon-Guitton, Thibaut Mourgues, Vanessa Rousseau, Sarah Cousty, Judith Cottin, Guillaume Drablier, Joëlle Micallef, Jean-Louis Montastruc
INTRODUCTION: Antithrombotic drugs are known to increase the risk of gingival bleeding because they affect coagulation. However, other drugs could also be involved in gingival bleeding. AIM: We performed a pharmacoepidemiological study to identify the drugs most frequently "suspected" in the occurrence of gingival bleeding. MATERIAL AND METHODS: We selected reports of "gingival bleeding" from 1 January 1985 to 30 September 2014 in the French PharmacoVigilance Database...
July 1, 2017: Journal of Clinical Periodontology
https://www.readbyqxmd.com/read/28666165/a-novel-enantioseparation-approach-based-on-liposome-electrokinetic-capillary-chromatography
#10
Xiaoqi Li, Yingxiang Du, Zijie Feng, Xiaodong Sun, Zhifeng Huang
As a novel separation mode of capillary electrophoresis (CE), liposome electrokinetic capillary chromatography (LEKC) has aroused considerable attention in recent years; however, the enantioseparation based on this new system has not been previously investigated. In this study, we proposed a brand-new LEKC chiral separation approach using liposomes comprised of phosphatidylcholine (PC) and cholesterol as pseudo-stationary phase and sulfobutyl ether-β-cyclodextrin (SBE-β-CD) as chiral selector. Compared with the single CD system and CD-SDS-MEKC system, this LEKC method presented an obviously preferable enantioseparation of four model drugs (naproxen, warfarin, ketoprofen and amlodipine)...
June 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28662899/l-type-amino-acid-transporter-1-utilizing-prodrugs-how-to-achieve-effective-brain-delivery-and-low-systemic-exposure-of-drugs
#11
Elena Puris, Mikko Gynther, Johanna Huttunen, Aleksanteri Petsalo, Kristiina M Huttunen
L-type amino acid transporter 1 (LAT1) is selectively expressed in the blood-brain barrier (BBB) and brain parenchyma. This transporter can facilitate brain delivery of neuroprotective agents and additionally give opportunity to minimize systemic exposure. Here, we investigated structure-pharmacokinetics relationship of five newly synthesized LAT1-utilizing prodrugs of the cyclooxygenase inhibitor, ketoprofen, in order to identify beneficial structural features of prodrugs to achieve both targeted brain delivery and low peripheral distribution of the parent drug...
June 27, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28658254/inhaled-nitric-oxide-prevents-nsaid-induced-renal-impairment-in-pseudo-normovolaemic-piglets
#12
Stephane Junot, Stephanie Keroak, Jerome R E Del Castillo, Jean-Yves Ayoub, Christian Paquet, Jeanne-Marie Bonnet-Garin, Eric Troncy
OBJECTIVE: Inhaled nitric oxide (iNO) is commonly used as a treatment of pulmonary hypertension. Its action is purported to be specific to the lung, but extrapulmonary effects have been reported. The objective of this study was to evaluate if iNO could compensate the renal impairment induced by ketoprofen, a conventional non-steroidal anti-inflammatory drug (NSAID), during general anaesthesia. METHODS: Under pseudo-normovolaemic condition, thirty piglets were randomly assigned into 5 equal groups and equipped for renal and systemic parameters measurements...
2017: PloS One
https://www.readbyqxmd.com/read/28656057/drug-bearing-supramolecular-filament-hydrogels-as-anti-inflammatory-agents
#13
Zhipeng Chen, Lei Xing, Qin Fan, Andrew G Cheetham, Ran Lin, Barbara Holt, Liwen Chen, Yanyu Xiao, Honggang Cui
We report here on the covalent conversion of the anti-inflammatory agent ketoprofen into self-assembling prodrugs that enable the effective purification of ketoprofen enantiomers, the improved selectivity and potency of ketoprofen, as well as the formation of one-component drug-bearing supramolecular hydrogels. We found that the ketoprofen hydrogelator could exhibit much-enhanced selectivity for cyclooxygenase 2 (COX-2) over COX-1, reduce the concentration of inflammatory cytokines (IL-1 and TNFα), and induce apoptosis in fibroblast-like synoviocytes while maintaining biocompatibility with healthy chondrocytes...
2017: Theranostics
https://www.readbyqxmd.com/read/28653347/preliminary-evaluation-of-pleurotus-ostreatus-for-the-removal-of-selected-pharmaceuticals-from-hospital-wastewater
#14
Laura Palli, Francesc Castellet-Rovira, Miriam Pérez-Trujillo, Donatella Caniani, Montserrat Sarrà-Adroguer, Riccardo Gori
The fungus Pleurotus ostreatus was investigated to assess its ability to remove diclofenac, ketoprofen and atenolol spiked at 10 mg/L each one in hospital wastewater. The degradation test was carried out in a fluidized bed bioreactor testing both the batch and the continuous mode (hydraulic retention time in the range 1.63-3 d). In batch mode, diclofenac disappeared in less than 24 h, ketoprofen was degraded up to almost 50% in 5 d while atenolol was not removed. In continuous mode, diclofenac and ketoprofen removals were about 100% and 70% respectively; atenolol degradation was negligible during the first 20 d but it increased up to 60% after a peak of laccase production and notable biomass growth...
June 27, 2017: Biotechnology Progress
https://www.readbyqxmd.com/read/28635050/prediction-of-sustained-fetal-toxicity-induced-by-ketoprofen-based-on-pk-pd-analysis-using-human-placental-perfusion-and-rat-toxicity-data
#15
Shingo Tanaka, Takeshi Kanagawa, Kazuo Momma, Satoko Hori, Hiroki Satoh, Takeshi Nagamatsu, Tomoyuki Fujii, Tadashi Kimura, Yasufumi Sawada
AIM: We encountered a case of fetal toxicity due to ductus arteriosus (DA) constriction in a 36-week pregnant woman who had applied multiple ketoprofen patches. The aim of this study was to present the case and develop a model to quantitatively predict the fetal toxicity risk of transdermal administration of ketoprofen. METHODS: Human placenta perfusion studies were conducted to estimate transplacental pharmacokinetic parameters. Using a developed model and these parameters, human fetal plasma concentration profiles of ketoprofen administered to mothers were simulated...
June 21, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28633956/a-time-adjustable-pulsatile-release-system-for-ketoprofen-in-vitro-and-in-vivo-investigation-in-a-pharmacokinetic-study-and-an-ivivc-evaluation
#16
Haiying Wang, Lizhen Cheng, Haoyang Wen, Caiyan Li, Yuenan Li, Xiaoyu Zhang, Yongfei Wang, Yanyan Wang, Tuanjie Wang, Weisan Pan, Xinggang Yang
A time-adjustable pulsatile release system (TAPS) containing ketoprofen (KF) as an active pharmaceutical agent was developed having been designed for bedtime dosing and releasing drug in the early morning to control the symptoms of rheumatoid arthritis (RA). The formulation involved a tablet core (KF) and a control-release layer, and the coating membrane was composed of EC and Eudragit L100. A single-factor study, a central composite design and a response surface method were selected to optimize the formula and the optimum prescription was as follows: tablet core (KF 50mg, MCC 70mg, lactose 40mg, L-HPC 38mg), and film (EC 7...
June 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28603129/pharmaceutical-and-in-vitro-therapeutic-equivalence-studies-of-ketoprofen-enteric-coated-100-mg-tablets
#17
Farya Zafar, Muhammad Harris Shoaib, Huma Ali, Rabia Ismail Yousuf, Ghazala Raza Naqvi, Zebun Nisa, Yusra Shafiq
The objective of this study was to assess the quality of six different brands of enteric coated Ketoprofen 100 mg tablets, KPB2 to KPB6 are available in commercial market of Karachi, Pakistan, while KPB1 was obtained from international source. We performed different physico-chemical assessments i.e. weight variation, diameter, hardness, friability, thickness, disintegration, content uniformity, assay and dissolution test. Results of all the investigations were found to be in adequate limits. Also pharmaceutical equivalence was determined by selecting different tests and assay assessment...
January 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28589306/application-of-a-biodegradable-polyesteramide-derived-from-l-alanine-as-novel-excipient-for-controlled-release-matrix-tablets
#18
Ana Dora Bonillo Martínez, Inés Carmen Rodríguez Galán, María Victoria Margarit Bellver
This pre-formulation study assays the capacity of the polyesteramide PADAS, poly (L-alanine-dodecanediol-L-alanine-sebacic), as an insoluble tablet excipient matrix for prolonged drug release. The flow properties of PADAS were suitable for tableting, and the compressibility of tablets containing exclusively PADAS was evaluated by ESEM observation of the microstructure. The tablets were resistant to crushing and non-friable and they did not undergo disintegration (typical features of an inert matrix). Tablets containing 33...
June 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28578813/multiclass-method-for-the-determination-of-pharmaceuticals-and-personal-care-products-in-compost-from-sewage-sludge-using-ultrasound-and-salt-assisted-liquid-liquid-extraction-followed-by-ultrahigh-performance-liquid-chromatography-tandem-mass-spectrometry
#19
A Luque-Muñoz, J L Vílchez, A Zafra-Gómez
An analytical method for the analysis of 16 pharmaceuticals and personal care products in compost from sewage sludge is successfully validated. Ultrasound assisted extraction with a mixture of acetonitrile:ethyl acetate (1:1, v/v) containing 10% (v/v) of acetic acid was carried out. Two cycles of extraction of 10min were applied. A clean-up of the extracts using salt-assisted liquid-liquid extraction (SALLE) was also included. Experimental design was used for the optimization of the main parameters involved in the extraction and cleaned-up steps...
May 26, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28561772/chiral-derivatives-of-xanthones-investigation-of-the-effect-of-enantioselectivity-on-inhibition-of-cyclooxygenases-cox-1-and-cox-2-and-binding-interaction-with-human-serum-albumin
#20
Carla Fernandes, Andreia Palmeira, Inês I Ramos, Carlos Carneiro, Carlos Afonso, Maria Elizabeth Tiritan, Honorina Cidade, Paula C A G Pinto, M Lúcia M F S Saraiva, Salette Reis, Madalena M M Pinto
Searching of new enantiomerically pure chiral derivatives of xanthones (CDXs) with potential pharmacological properties, particularly those with anti-inflammatory activity, has remained an area of interest of our group. Herein, we describe in silico studies and in vitro inhibitory assays of cyclooxygenases (COX-1 and COX-2) for different enantiomeric pairs of CDXs. The evaluation of the inhibitory activities was performed by using the COX Inhibitor Screening Assay Kit. Docking simulations between the small molecules (CDXs; known ligands and decoys) and the enzyme targets were undertaken with AutoDock Vina embedded in PyRx-Virtual Screening Tool software...
May 31, 2017: Pharmaceuticals
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