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Romina Pezzoli, John G Lyons, Noel Gately, Clement L Higginbotham
The investigation of the miscibility between active pharmaceutical ingredients (API's) and polymeric excipients is of great interest for the formulation and development of amorphous solid dispersions, especially in the context of the prediction of the stability of these systems. Two different methods were applied to determine the miscibility between model compounds poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA) and indomethacin (IND), viz. the measurement of the glass transition temperature (Tg ) and the melting point depression method framed on the Flory-Huggins theory...
July 14, 2018: International Journal of Pharmaceutics
Islam Ibrahim Hegab, Rania Nagi Abd-Ellatif, Mona Tayssir Sadek
The protective effect of N- acetylcysteine (NAC) and genistein (GEN) on an experimental model of indomethacin (IND) - induced gastric injury was investigated. 50 male rats were divided into 5 groups: control (I), IND (II), NAC pretreated (III), GEN Pretreated (IV), NAC+GEN pretreated (V). Rats were orally administered NAC (500 mg/kg), GEN (10 mg/kg) or both once daily for 7 days before the induction of the gastric injury by IND (50 mg/kg). Stomach was removed for biochemical analysis and histopathological examinations...
July 16, 2018: Canadian Journal of Physiology and Pharmacology
Mario Ficker, Matthijs J M Theeuwen, Anna Janaszewska, Michal Gorzkiewicz, Søren W Svenningsen, Barbara Klajnert-Maculewicz, Jørn B Christensen
COX-2 inhibitors such as Non-steroidal anti-inflammatory drugs (NSAIDs) are the most common treatment for chronic inflammatory diseases like arthritis and atherosclerosis. However, they are associated with severe side effects such as cardiovascular events or stomach bleeding, due to co-inhibition of other enzymes (COX1) and off target accumulation. PAMAM-dendrimers can solubilize these lipophilic drugs and increase their bioavailability; furthermore PAMAM dendrimers seem to have some per se accumulation in inflammatory sides...
July 16, 2018: Molecular Pharmaceutics
Masataka Hanada, Scott V Jermain, Xingyu Lu, Yongchao Su, Robert O Williams
This study focuses on the relationship between drug dissolution properties, physical stability against recrystallization, and specific mechanical energy (SME) from a hot melt extrusion (HME) process of ternary amorphous solid dispersions (ASDs) containing indomethacin (IND), HPMC and mesoporous silica (XDP) prepared using different HME screw condition (the number of kneading zones /rotation speed). The screw condition greatly influenced the amorphous characteristics of the processed material and SME values...
July 10, 2018: International Journal of Pharmaceutics
Yaochun Yu, Ping Han, Li-Jun Zhou, Zhong Li, Michael Wagner, Yujie Men
Biotransformation of various micropollutants (MPs) has been found to be positively correlated with nitrification in activated sludge communities. To further elucidate the roles played by ammonia-oxidizing bacteria (AOB) and nitrite-oxidizing bacteria (NOB), we investigated the biotransformation capabilities of an NOB pure culture ( Nitrobacter sp.), and an AOB ( Nitrosomonas europaea)/NOB ( Nitrobacter sp.) co-culture for fifteen MPs, whose biotransformation was reported previously to be associated with nitrification...
July 13, 2018: Environmental Science & Technology
Sinan Bayindir, Yusuf Temel, Adnan Ayna, Mehmet Ciftci
Glucose-6-phosphate dehydrogenase (G6PD) and 6-phosphogluconate dehydrogenase (6PGD) play an important function in various biochemical processes as they generate reducing power of the cell. Thus, metabolic reprogramming of reduced nicotinamide adenine dinucleotide phosphate (NADPH) homeostasis is reported to be a vital step in cancer progression as well as in combinational therapeutic approaches. In this study, N-benzoylindoles 9a--9d, which form the main framework of many natural indole derivatives such as indomethacin and N-benzoylindoylbarbituric acid, were synthesized through three easy and effective steps as an in vitro inhibitor effect of G6PD and 6PGD...
July 10, 2018: Journal of Biochemical and Molecular Toxicology
Andrew M Tomlin, David J Woods, Hywel S Lloyd, Ralph A H Stewart, Murray W Tilyard
PURPOSE: Existing knowledge of medicines that increase the risk of an adverse event may be corroborated and augmented by population studies specifically assessing the risk associated with the concurrent use of these medicines and use by patients with existing comorbidity. An American Heart Association review recently identified a variety of medicines that may cause or exacerbate heart failure (HF), many with evidence from limited evaluation of population data. We assessed the risk of first-time HF associated with the use of 50 of these medicines by New Zealand's primary care population...
July 10, 2018: Pharmacoepidemiology and Drug Safety
Marco Martin González-Chávez, Angel Josabad Alonso-Castro, Juan Ramón Zapata-Morales, Víctor Arana-Argáez, Julio Cesar Torres-Romero, Yessica Elisa Medina-Rivera, Ernesto Sánchez-Mendoza, Salud Pérez-Gutiérrez
Salvia tiliifolia Vahl (Lamiaceae) is used for the empirical treatment of pain and inflammation. The diterpenoid tilifodiolide (TFD) was isolated from Salvia tiliifolia. The in vitro anti-inflammatory effects of TFD (0.1-200 µM) were assessed using murine macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The in vivo anti-inflammatory activity of TFD was assessed using the carrageenan-induced paw edema test for 6 h. The antinociceptive effects of TFD were evaluated using the formalin test and the acetic acid induced-writhing test...
June 2018: Drug Development Research
Gregory T Wolf, Jeffrey S Moyer, Michael J Kaplan, Jason G Newman, James E Egan, Neil L Berinstein, Theresa L Whiteside
Head and neck squamous cell carcinoma (HNSCC) is an immunosuppressive malignancy characterized by tumor-driven immune-system abnormalities that contribute to disease progression. For patients with surgically resectable HNSCC, treatment is often curative surgery followed by irradiation or chemoradiation in high-risk settings to reduce the risk of recurrence. Poor survival and considerable morbidity of current treatments suggest the need for new therapeutic modalities that can improve outcomes. Defects in antitumor immunity of HNSCC patients include suppressed dendritic cell (DC) maturation, deficient antigen-presenting cell function, compromised natural killer (NK)-cell cytotoxicity, increased apoptosis of activated T lymphocytes, and impaired immune-cell migration to tumor sites...
2018: OncoTargets and Therapy
Ya'nan Deng, Jiwei Shen, Jiawei Liu, Yinmao Wei, Chaozhan Wang
Poly(2-naphthyl acrylate) was first grafted onto silica-coated magnetic nanoparticles by surface-initiated atom transfer radical polymerization to prepare a reversed-phase magnetic adsorbent. The resulting polymer brush displays enhanced extraction efficiency by offering active sites on the surfaces of adsorbent. It was applied to the preconcentration of the non-steroidal antiinflammatory drugs (NSAIDs) indomethacin (InDo) and diclofenac (DIC). These drugs interact with the sorbent through hydrophobic and π-interactions, and via electrostatic attraction...
July 9, 2018: Mikrochimica Acta
Daniela Doni, Giuseppe Paterlini, Anna Locatelli, Sara Arnoldi, Maria Chiara Magri, Davide Bernasconi, Maria Grazia Valsecchi, Paolo Emilio Tagliabue
Premature birth is a leading cause of neonatal morbidity and mortality. Since gestational age at birth is the most important predictive factor of adverse neonatal outcomes, strategies to postpone premature labor are of major importance. Studies on tocolytic drugs show that COX inhibitors such as indomethacin are superior to others in terms of efficiency in delaying birth, but results concerning neonatal outcomes associated with prenatal exposure to these drugs show controversial results. Indomethacin is also used in the postnatal age for pharmacologic treatment of patent ductus arteriosus (PDA), but no data concerning the effects of antenatal exposure on postnatal ductal patency are available...
July 9, 2018: Journal of Maternal-fetal & Neonatal Medicine
Xiaoyu Kang, Liyue Zheng, Wei Zeng, Shengye Yang, Hao Sun, Rongchun Zhang, Xiangping Wang, Biaoluo Wang, Qin Tao, Shaowei Yao, Jie Chen, Yanglin Pan, Xuegang Guo
BACKGROUND: Post-ERCP pancreatitis (PEP) is the most common adverse event of ERCP. Rectal indomethacin has been widely administered to decrease the incidence of PEP in high-risk patients. However, it cannot completely prevent the occurrence of PEP. The purpose of the study was to evaluate the risk factors for PEP in high-risk patients receiving post-ERCP indomethacin. METHODS: From June 2012 to July 2015, patients undergoing ERCP and at high risk for PEP in three tertiary hospitals in China were enrolled...
July 6, 2018: Journal of Gastrointestinal Surgery: Official Journal of the Society for Surgery of the Alimentary Tract
Masashi Kawami, Tadashi Shimonakamura, Ryoko Yumoto, Mikihisa Takano
PURPOSE: Alveolar clearance of proteins, such as albumin, plays an essential role in recovery from lung injuries. Albumin is known to be oxidized by reactive oxygen species (ROS), leading to generation of advanced oxidation protein products (AOPP)-albumin in the alveolar lining fluid. In this study, we aimed to characterize the uptake of FITC-labeled AOPP-albumin (FITC-AOPP-albumin) into human alveolar epithelial cell line, A549. METHODS: FITC-AOPP-albumin uptake into A549 cells and its effect of ROS generation was evaluated using fluorescence spectrometer and flow cytometry, respectively...
2018: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
Yunxiao Lyu, Yunxiao Cheng, Bin Wang, Yueming Xu, Weibing Du
BACKGROUND: Recently, although studies have investigated the role of NSAIDs in the prevention of post-endoscopic retrograde cholangiopancreatography pancreatitis (PEP), selection of the ideal drug, the time and route of its administration for the appropriate population remain controversial. METHODS: A systematic search was done in sources including PubMed, Embase, Web of Science, the Cochrane Library Central, and from from August 1, 1990 to August 1, 2017...
July 4, 2018: BMC Gastroenterology
Tamorah Lewis, Leon Van Haandel, Allison Scott, J Steven Leeder
No abstract text is available yet for this article.
July 2, 2018: Pediatric Research
Koji Takeuchi, Kikuko Amagase
Endogenous prostaglandins (PGs), produced from arachidonic acid by the two isoforms of cyclooxygenase (COX), play a pivotal role in maintaining mucosal integrity by modulating various functions of the gastrointestinal (GI) tract, and PGE2 is most effective in these actions. The PGE2 receptor is classified into 4 specific G-protein coupled subtypes, EP1-EP4, and their distribution accounts for the multiple effects of this prostanoid. PGE2 prevents acid-reflux esophagitis and indomethacin-induced gastric lesions through EP1 receptors, while endogenous PGs protect the stomach against cold restraint stress mediated by mainly PGI2/IP receptors and partly EP4 receptors...
June 28, 2018: Current Pharmaceutical Design
Vittorio Romagnoli, Annalisa Pedini, Monica Santoni, Grazia Scutti, Massimo Colaneri, Marco Pozzi, Paola E Cogo, Virgilio P Carnielli
AimThe aim of this study was to determine the spontaneous closure rate of patent ductus arteriosus at a 2-year follow-up, following failed medical therapy and beyond initial hospital discharge, and to evaluate in-hospital spontaneous or pharmacological closure rates.Materials and methodsA retrospective evaluation was conducted in a cohort of preterm infants admitted to the Neonatal ICU of Ancona between January, 2004 and June, 2013. Inclusion criteria were gestational age between 24+0 and 29+6 weeks or birth weight 1...
June 29, 2018: Cardiology in the Young
M Joice, G I Vasileiadis, D F Amanatullah
Aims: The aim of this study was to assess the efficacy of non-selective and selective non-steroidal anti-inflammatory drugs (NSAIDs) in preventing heterotopic ossification (HO) after total hip arthroplasty (THA). Methods: A thorough and systematic literature search was conducted and 29 studies were found that met inclusion criteria. Data were extracted and statistical analysis was carried out generating forest plots. Results: Non-selective NSAIDs showed a significant decrease in the odds for forming HO after THA (odds ratio (OR) -1...
July 2018: Bone & Joint Journal
David G Lehenbauer, Charles D Fraser, Todd C Crawford, Naru Hibino, Susan Aucott, Joshua C Grimm, Nishant Patel, J Trent Magruder, Duke E Cameron, Luca Vricella
OBJECTIVE: The safety of surgical closure of patent ductus arteriosus (PDA) in very low birth weight premature neonates has been questioned because of associated morbidities. However, these studies are vulnerable to significant bias as surgical ligation has historically been utilized as "rescue" therapy. The objective of this study was to review our institutions' outcomes of surgical PDA ligation. METHODS: All neonates with operative weight of ≤1.00 kg undergoing surgical PDA ligation from 2003 to 2015 were analyzed...
July 2018: World Journal for Pediatric & Congenital Heart Surgery
Abdi Wira Septama, Ibrahim Jantan, Pharkphoom Panichayupakaranant
OBJECTIVES: To investigate the effects of flavonoids isolated from Artocarpus heterophyllus. heartwood on chemotaxis, phagocytosis, reactive oxygen species (ROS) production and myeloperoxidase (MPO) activity of human phagocytes. METHODS: Chemotaxis was evaluated using a modified Boyden chamber and phagocytosis was determined by flowcytometer. Respiratory burst was investigated by luminol-based chemiluminescence assay while MPO activity was determined by colorimetric assay...
June 25, 2018: Journal of Pharmacy and Pharmacology
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