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indomethacin

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https://www.readbyqxmd.com/read/28534130/tissue-distribution-and-dermal-drug-determination-of-indomethacin-transdermal-absorption-patches
#1
Jingjing Ma, Ying Gao, Yinghua Sun, Dawei Ding, Qi Zhang, Bingjun Sun, Menglin Wang, Jin Sun, Zhonggui He
The tissue distribution and percutaneous drug absorption of indomethacin (IND) patches were studied using commercial IND as a comparison. The concentration of IND in skin, plasma, and muscle in mice was measured by LC-MS/MS, and the IND concentration in the dermis of rats was also monitored by microdialysis. After percutaneous administration, the "double-peak" phenomenon occurred in different tissues, and the IND concentration was ranked as skin first, followed by plasma and then muscle. In particular, skin acted as a reservoir for drug release, and the "secondary hump" in tissue distribution was attributed to the subsequent release of lipophilic IND in skin...
May 22, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28532677/predicting-melt-rheology-for-hot-melt-extrusion-by-means-of-a-simple-tg-measurement
#2
Esther S Bochmann, Elgin E Üstüner, Andreas Gryczke, Karl G Wagner
The feasibility of predicting melt rheology by using the glass transition temperature (Tg) of a desired amorphous solid dispersion (ASD) for hot-melt extrusion (HME) and other melt based processes is presented. Three groups of three different active pharmaceutical ingredients (APIs) or plasticizer/copovidone mixtures, with identical glass transition in rheological testing, were used. Their rheological behavior as a function of temperature and frequency were analyzed by means of small amplitude oscillatory shear (SAOS) on an oscillatory rheometer...
May 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28531959/occurrence-and-removal-of-pharmaceuticals-hormones-personal-care-products-and-endocrine-disrupters-in-a-full-scale-water-reclamation-plant
#3
Ngoc Han Tran, Karina Yew-Hoong Gin
This study provided the first comprehensive data on the occurrence and removal of twenty-five target emerging contaminants (ECs) in a full-scale water reclamation plant (WRP) in the Southeast Asian region. Nineteen out of the twenty-five ECs were ubiquitously detected in raw influent samples. Concentrations of the detected ECs in raw influent samples ranged substantially from 44.3 to 124,966ng/L, depending upon the compound and sampling date. The elimination of ECs in full-scale conventional activated sludge (CAS) and membrane bioreactor (MBR) systems at a local WRP was evaluated and compared...
May 17, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28527126/polycaprolactone-based-nanoparticles-loaded-with-indomethacin-for-anti-inflammatory-therapy-from-preparation-to-ex-vivo-study
#4
Waisudin Badri, Karim Miladi, Sophie Robin, Céline Viennet, Qand Agha Nazari, Géraldine Agusti, Hatem Fessi, Abdelhamid Elaissari
PURPOSE: This work focused on the preparation of polycaprolactone based nanoparticles containing indomethacin to provide topical analgesic and anti-inflammatory effect for symptomatic treatment of inflammatory diseases. Indomethacin loaded nanoparticles are prepared for topical application to decrease indomethacin side effects and administration frequency. Oppositely to already reported works, in this research non-invasive method has been used for the enhancement of indomethacin dermal drug penetration...
May 19, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28526687/ffa2-activation-combined-with-ulcerogenic-cox-inhibition-induces-duodenal-mucosal-injury-via-the-5-ht-pathway-in-rats
#5
Yasutada Akiba, Koji Maruta, Kazuyuki Narimatsu, Hyder Said, Izumi Kaji, Ayaka Kuri, Ken-Ichi Iwamoto, Atsukazu Kuwahara, Jonathan D Kaunitz
Serotonin (5-HT), predominantly synthesized and released by enterochromaffin cells, is implicated in gastrointestinal symptoms such as emesis, abdominal pain and diarrhea. Since luminal short-chain fatty acids (SCFAs) release 5-HT from enterochromaffin cells, which express the SCFA receptor FFA2 in rat duodenum, we examined the effects of the selective FFA2 agonist phenylacetamide-1 (PA1) on duodenal 5-HT release with consequent bicarbonate secretion (DBS) and on indomethacin (IND)-induced enteropathy. Intestinal injury was induced by IND (10 mg/kg, sc) with or without PA1...
May 19, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28524362/a-novel-chemiluminescence-sensor-for-the-determination-of-indomethacin-based-on-sulfur-and-nitrogen-co-doped-carbon-quantum-dot-kmno4-reaction
#6
Tooba Hallaj, Mohammad Amjadi, Jamshid L Manzoori, Neda Azizi
We report on a simple and sensitive sulfur and nitrogen co-doped carbon quantum dot (S,N-CQD)-based chemiluminescence (CL) sensor for the determination of indomethacin. S,N-CQDs were prepared by a hydrothermal method and characterized by fluorescence spectra, Fourier transform infrared spectroscopy and transmission electron microscopy. To obtain the best CL system for determination of indomethacin, the reaction of S,N-CQDs with some common oxidants was studied. Among the tested systems, the S,N-CQD-KMnO4 reaction showed the highest sensitivity for the detection of indomethacin...
May 19, 2017: Luminescence: the Journal of Biological and Chemical Luminescence
https://www.readbyqxmd.com/read/28523577/ffa3-activation-stimulates-duodenal-bicarbonate-secretion-and-prevents-nsaid-induced-enteropathy-via-the-glp-2-pathway-in-rats
#7
Hyder Said, Yasutada Akiba, Kazuyuki Narimatsu, Koji Maruta, Ayaka Kuri, Ken-Ichi Iwamoto, Atsukazu Kuwahara, Jonathan D Kaunitz
BACKGROUND: Therapy with nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with enteropathy in humans and experimental animals, a cause of considerable morbidity. Unlike foregut NSAID-associated mucosal lesions, most treatments for this condition are of little efficacy. We propose that the endogenously released intestinotrophic hormone glucagon-like peptide-2 (GLP-2) prevents the development of NSAID-induced enteropathy. Since the short-chain fatty acid receptor FFA3 is expressed on enteroendocrine L cells and on enteric nerves in the gastrointestinal tract, we further hypothesized that activation of FFA3 on L cells protects the mucosa from injury via GLP-2 release with enhanced duodenal HCO3(-) secretion...
May 18, 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28516471/topical-non-steroidal-anti-inflammatory-drugs-for-analgesia-in-traumatic-corneal-abrasions
#8
REVIEW
Abel Wakai, John G Lawrenson, Annali L Lawrenson, Yongjun Wang, Michael D Brown, Michael Quirke, Omar Ghandour, Ryan McCormick, Cathal D Walsh, Ahmed Amayem, Eddy Lang, Nick Harrison
BACKGROUND: Traumatic corneal abrasions are relatively common and there is a lack of consensus about analgesia in their management. It is therefore important to document the clinical efficacy and safety profile of topical ophthalmic non-steroidal anti-inflammatory drugs (NSAIDs) in the management of traumatic corneal abrasions. OBJECTIVES: To identify and evaluate all randomised controlled trials (RCTs) comparing the use of topical NSAIDs with placebo or any alternative analgesic interventions in adults with traumatic corneal abrasions (including corneal abrasions arising from foreign body removal), to reduce pain, and its effects on healing time...
May 18, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28512667/involvement-of-leukotriene-b4-released-from-keratinocytes-in-itch-associated-response-to-intradermal-interleukin-31-in-mice
#9
Tsugunobu Andoh, Ayako Harada, Yasushi Kuraishi
A recent study suggests that interleukin-31 (IL-31) exerts its effect via indirect mechanisms rather than through direct stimulation of cutaneous nerves. However, the underlying peripheral mechanisms of IL-31-induced itch in the skin remain unclear. Therefore, the present study investigated the peripheral mechanisms underlying IL-31-induced itch in mice. IL-31-induced itch-related response was inhibited by anti-allergic drugs (tranilast and azelastine), but not by an H1 histamine receptor antagonist (terfenadine)...
May 17, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28512605/toxicity-status-and-antiulcerative-potential-of-sansevieria-trifasciata-leaf-extract-in-wistar-rats
#10
Osasenaga Macdonald Ighodaro, Abiola Muhammad Adeosun, Barinemene Francis Ojiko, Abeeb Taiwo Akorede, Oyindamola Fuyi-Williams
AIMS: The lethal dose 50% (LD50) and antiulcerative potentials of Sansevieria trifasciata (ST) leaf extract were investigated. MATERIALS AND METHODS: LD50 was determined through two routes of administration (intraperitoneal [i.p] and oral [p.o]) using the method of Lorke. The antiulcerative activity was evaluated in indomethacin-induced ulcer model (40 mg/kg body weight [BW], i.p, single dose) against a reference drug, cimetidine (100 mg/kg BW, p.o). ST was assessed at two different doses (200 and 400 mg/kg BW, p...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28512025/synthesis-of-methanesulphonamido-benzimidazole-derivatives-as-gastro-sparing-antiinflammatory-agents-with-antioxidant-effect
#11
Ratika Sharma, Alka Bali, Bhim Bahadur Chaudhari
A series of 5-methanesulphonamido benzimidazole derivatives were designed by combining the structural features of clinically useful anti-inflammatory drugs (nimesulide and rofecoxib) and antiulcer drugs (lansoprazole, omeprazole, etc.) based on physicochemical and 3D similarity studies. The compounds were evaluated for their anti-inflammatory activity in carrageenan induced rat paw edema model taking rofecoxib and indomethacin as standard drugs. In vitro antioxidant activity of the compounds was assessed by potassium ferricyanide reducing power (PFRAP) assay...
May 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28502905/inhibition-of-proinflammatory-mediators-by-coumaroyl-lupendioic-acid-a-new-lupane-type-triterpene-from-careya-arborea-on-inflammation-induced-animal-model
#12
Rayhana Begum, Manjur Ali Sheliya, Showkat R Mir, Ekta Singh, Manju Sharma
ETHNOPHARMACOLOGICAL RELEVANCE: Careya arborea Roxb. (Lecythidaceae) is a large tree found throughout India in deciduous forests and grasslands. C. arborea is traditionally used in tumors, inflammation, anthelmintic, bronchitis, epileptic fits, astringents, antidote to snake-venom, skin disease, diarrhea, dysentery with bloody stools, dyspepsia, ulcer, tooth ache, and ear pain. AIM OF THE STUDY: In our previous work, the methanolic extract of Careya arborea stem bark showed significant anti-inflammatory activity...
May 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28502186/efectiveness-of-dydrogesterone-17-oh-progesterone-and-micronized-progesterone-in-prevention-of-preterm-birth-in-women-with-a-short-cervix
#13
Olga Anatolievna Pustotina
OBJECTIVE: to compare the efficacy of dydrogesterone, 17-OH progesterone (17OHP) and oral or vaginal micronized progesterone with cerclage for the prevention of preterm birth in women with a short cervix. METHODS: The study included 95 women with singleton gestation and cervical length (CL)≤ 25 mm. Among these, 35 women were asymptomatic at 15-24 weeks and 60 had symptoms of threatened late miscarriage (LM) or preterm delivery (PD). Patients were randomized to receive dydrogesterone, 17OHP or oral/vaginal micronized progesterone; after one week of therapy 15 women underwent cerclage...
May 14, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28502103/reduced-platelet-aggregation-in-women-after-intercourse-a-possible-role-for-the-cyclooxygenase-pathway
#14
Gabriel Mayoral-Andrade, Laura Pérez-Campos-Mayoral, Abraham Majluf-Cruz, Eduardo Perez-Campos Mayoral, Carlos Perezcampos Mayoral, Ana Rocha-Núñez, Margarito Martinez, Edgar Zenteno, Leticia Hernandez-Gonzalez, María Guadalupe López Juan, Alma Dolores Pérez-Santiago, Eduardo Pérez-Campos
We hypothesise that molecules in the cyclooxygenase pathway affect platelet activity when seminal fluid (SF) is present. We considered the influence of SF on platelet aggregation in women, and believe that the prostanoids in SF signalling are significant. Thirty-one female subjects were studied, 20 of whom were sexually active. Male partners were given either aspirin or indomethacin to inhibit cyclooxygenase. The 6-keto prostaglandin F1α (6-keto PGF1α) and prostaglandin E metabolite (PGE-M) in SF were measured by competitive assay...
May 14, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28501682/the-role-of-arachidonic-acid-cyclooxygenase-cascade-phosphodiesterase-iv-and-rho-kinase-in-h2s-induced-relaxation-in-the-mouse-corpus-cavernosum
#15
Fatma Aydinoglu, Nuran Ogulener
BACKGROUND: Penile corpus cavernosum is an extremely vascularized tissue and cavernosal smooth muscle tone is regulated by the balance between contractile and relaxant factor. We investigated the possible role of arachidonic acid/cyclooxygenase cascade, phosphodiesterase IV (PDEIV) and Rho-kinase in exogenous hydrogen sulfide (H2S)-induced relaxation in mouse corpus cavernosum. METHODS: The relaxant response to H2S (NaHS as exogenous H2S; 1-1000μM) were obtained in isolated mouse corpus cavernosum tissues which pre-contracted by phenylephrine (5μM)...
February 24, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28501097/orofacial-pain-and-headaches-associated-with-exfoliation-glaucoma
#16
Noboru Noma, Mayumi Iwasa, Andrew Young, Mariko Ikeda, Yung-Chu Hsu, Maasa Yamamoto, Kenji Inoue, Yoshiki Imamura
BACKGROUND AND OVERVIEW: Exfoliation syndrome is the most common identifiable cause of open-angle glaucoma. The authors report a case of exfoliation glaucoma in a patient who had orofacial pain. CASE DESCRIPTION: A 77-year-old woman was treated at the orofacial pain clinic for left-sided facial pain and headaches of 7 months' duration. Her cataracts and open-angle glaucoma had been diagnosed approximately 3 years earlier. Her main symptoms were orofacial pain, eye redness, inflammation of the eyelids, and eyelid edema...
May 11, 2017: Journal of the American Dental Association
https://www.readbyqxmd.com/read/28499935/sub-chronic-lead-exposure-produces-%C3%AE-1-adrenoceptor-downregulation-decreasing-arterial-pressure-reactivity-in-rats
#17
Cindy Medici Toscano, Maylla Ronacher Simões, Maria Jesus Alonso, Mercedes Salaices, Dalton Valentim Vassallo, Mirian Fioresi
Lead is considered a causative factor for hypertension and other cardiovascular diseases. AIMS: To investigate the effects of sub-chronic lead exposure on blood pressure reactivity and cardiac β1-adrenoceptor activity and to evaluate whether the effects found in vitro are similar to those found in vivo. MAIN METHODS: Male Wistar rats were randomly distributed into two groups: control rats (Ct) and rats administered drinking water containing 100ppm lead (Pb) for 30days...
May 9, 2017: Life Sciences
https://www.readbyqxmd.com/read/28497473/topical-analgesics-for-acute-and-chronic-pain-in-adults-an-overview-of-cochrane-reviews
#18
REVIEW
Sheena Derry, Philip J Wiffen, Eija A Kalso, Rae F Bell, Dominic Aldington, Tudor Phillips, Helen Gaskell, R Andrew Moore
BACKGROUND: Topical analgesic drugs are used for a variety of painful conditions. Some are acute, typically strains or sprains, tendinopathy, or muscle aches. Others are chronic, typically osteoarthritis of hand or knee, or neuropathic pain. OBJECTIVES: To provide an overview of the analgesic efficacy and associated adverse events of topical analgesics (primarily nonsteroidal anti-inflammatory drugs (NSAIDs), salicylate rubefacients, capsaicin, and lidocaine) applied to intact skin for the treatment of acute and chronic pain in adults...
May 12, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28493718/tamarixetin-3-o-%C3%AE-d-glucopyranoside-from-azadirachta-indica-leaves-gastroprotective-role-through-inhibition-of-matrix-metalloproteinase-9-activity-in-mice
#19
Dharmendra K Yadav, Yogesh P Bharitkar, Abhijit Hazra, Uttam Pal, Sugreev Verma, Sayantan Jana, Umesh P Singh, Nakul C Maiti, Nirup B Mondal, Snehasikta Swarnakar
Neem (Azadirachta indica) is a well-known medicinal and insecticidal plant. Although previous studies have reported the antiulcer activity of neem leaf extract, the lead compound is still unidentified. The present study reports tamarixetin 3-O-β-d-glucopyranoside (1) from a methanol extract of neem leaves and its gastroprotective activity in an animal model. Compound 1 showed significant protection against indomethacin-induced gastric ulceration in mice in a dose-dependent manner. Moreover, ex vivo and circular dichroism studies confirmed that 1 inhibited the enzyme matrix metalloproteinase-9 (MMP-9) activity with an IC50 value of ca...
May 11, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28489292/dual-stimuli-responsive-nanoparticles-for-controlled-release-of-anticancer-and-anti-inflammatory-drugs-combination
#20
Liandong Feng, Yuqi Wang, Zhiliang Luo, Zheng Huang, Yan Zhang, Kai Guo, Deju Ye
Dual stimuli-responsive nanoparticles capable of fine-tuning drug release to augment therapeutic efficacy have become as promising tools for anticancer drugs delivery. However, rational design of these 'smart' nanoparticles for selective delivery and controlling release of multidrug combination in cancer cells to achieve synergistic effects remain challenging. Here we report a pH/redox dual responsive nanoparticle FA-DOX-Ind-NP based on a novel tumor targeting and biodegradable poly(β-amino ester) polymer, and demonstrate its high ability to enter into cancer cells and release a combination of anticancer drug doxorubicin and nonsteroidal anti-inflammatory drug indomethacin to achieve synergistic chemo-anti-inflammatory effects and overcome multidrug resistance...
May 10, 2017: Chemistry: a European Journal
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