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https://www.readbyqxmd.com/read/28806859/analysis-of-low-molecular-weight-compounds-using-maldi-and-ldi-tof-ms-direct-detection-of-active-pharmaceutical-ingredients-in-different-formulations
#1
João L Bronzel, Cintia D F Milagre, Humberto M S Milagre
Matrix-Assisted Laser Desorption/Ionization Mass Spectrometry (MALDI-MS) is a high throughput, easy to use analytical technique. The simple sample preparation of this technique and its tolerance to the presence of contaminants are among its advantages. In contrast, depending on the matrix used, MALDI can ionize and generates ions in the low m/z range that complicate the interpretation of the spectra of low molecular weight compounds. To address this issue, one can envisage the use of tunable ionic matrices that can reduce the low m/z interferents...
August 14, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28806704/chiral-pharmaceuticals-a-review-on-their-environmental-occurrence-and-fate-processes
#2
REVIEW
Edmond Sanganyado, Zhijiang Lu, Qiuguo Fu, Daniel Schlenk, Jay Gan
More than 50% of pharmaceuticals in current use are chiral compounds. Enantiomers of the same pharmaceutical have identical physicochemical properties, but may exhibit differences in pharmacokinetics, pharmacodynamics and toxicity. The advancement in separation and detection methods has made it possible to analyze trace amounts of chiral compounds in environmental media. As a result, interest on chiral analysis and evaluation of stereoselectivity in environmental occurrence, phase distribution and degradation of chiral pharmaceuticals has grown substantially in recent years...
August 5, 2017: Water Research
https://www.readbyqxmd.com/read/28806701/application-of-different-spectrophotometric-methods-for-simultaneous-determination-of-elbasvir-and-grazoprevir-in-pharmaceutical-preparation
#3
Khalid A M Attia, Nasr M El-Abasawi, Ahmed El-Olemy, Ahmed H Abdelazim
The first three UV spectrophotometric methods have been developed of simultaneous determination of two new FDA approved drugs namely; elbasvir and grazoprevir in their combined pharmaceutical dosage form. These methods include simultaneous equation, partial least squares with and without variable selection procedure (genetic algorithm). For simultaneous equation method, the absorbance values at 369 (λmax of elbasvir) and 253nm (λmax of grazoprevir) have been selected for the formation of two simultaneous equations required for the mathematical processing and quantitative analysis of the studied drugs...
August 10, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28806699/a-portable-synthesis-of-water-soluble-carbon-dots-for-highly-sensitive-and-selective-detection-of-chlorogenic-acid-based-on-inner-filter-effect
#4
Huan Yang, Liu Yang, Yusheng Yuan, Shuang Pan, Jidong Yang, Jingjing Yan, Hui Zhang, Qianqian Sun, Xiaoli Hu
In this work, a simple and facile hydrothermal method for synthesis of water-soluble carbon dots (CDs) with malic acid and urea, and were then employed as a high-performance fluorescent probe for selective and sensitive determination of chlorogenic acid (CGA) based on inner filter effect. The as-synthesized CDs was systematically characterized by Transmission electron microscopy (TEM), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), Energy disperse spectroscopy (EDS), UV-vis absorption spectroscopy, spectrofluorophotometry, and the results indicated that the sizes of CDs were mainly distributed in the range of 1...
August 1, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28806675/biotransformation-of-nsaids-by-pig-liver-microsomes-in%C3%A2-vitro-kinetics-metabolites-identification-and-toxicity-prediction
#5
Liyun Ma, Xiaojing Mao, Xiao Sun, Li Xu
Non-steroidal anti-inflammatory drugs (NSAIDs) are one of the most frequently used pharmaceuticals in animals. In the current study, the biotransformation of five NSAIDs by pig liver microsomes (PLMs) was studied. The pseudo-first-order kinetics mode was obtained for the metabolization of the studied NSAIDs by PLMs in vitro. The metabolites were identified by high performance liquid chromatography with a high-resolution LTQ-Orbitrap mass spectrometry. The hydroxylation of benzene was confirmed to be the dominating metabolic pathway...
August 8, 2017: Chemosphere
https://www.readbyqxmd.com/read/28806550/discrepant-responses-of-the-electron-transfer-capacity-of-soil-humic-substances-to-irrigations-with-wastewaters-from-different-sources
#6
Wenbing Tan, Yuan Zhang, Beidou Xi, Xiaosong He, Rutai Gao, Caihong Huang, Hui Zhang, Dan Li, Xinyu Zhao, Meng Li, Li Li, Jie Jiang, Guoan Wang
An increasing area of agricultural land is irrigated with wastewater worldwide due to the scarcity of fresh water resources. Whether wastewater irrigations can affect the electron transfer capacity (ETC) of natural organic matter in soils is unclear. In this study, we assess the responses of the electron-accepting capacity (EAC) and electron-donating capacity (EDC) of soil humic substances (HS) to irrigations with wastewaters from different sources. We show that the EAC of soil HS increases and the EDC of soil HS decreases after irrigation with domestic wastewater...
August 11, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28805961/reducing-branded-prescription-drug-prices-a-review-of-policy-options
#7
G Caleb Alexander, Jeromie Ballreich, Mariana P Socal, Taruja Karmarkar, Antonio Trujillo, Jeremy Greene, Joshua Sharfstein, Gerard Anderson
The high prices of specialty pharmaceuticals are causing some public programs to ration care and many private insurers, including Medicare drug plans, to place specialty drugs on high cost sharing tiers. As a result, access to these drugs is severely restricted, and only a small portion of the population with the disease is receiving treatment. This concern has generated a wide range of proposed solutions. We conducted a literature review and identified fifty-two solutions in the peer reviewed literature that we classified into five broad categories: revising the patent system; encouraging research to increase development of new drugs; altering pharmaceutical regulation; decreasing market demand; and developing innovative pricing strategies...
August 14, 2017: Pharmacotherapy
https://www.readbyqxmd.com/read/28805837/synthesis-of-cu-catalysed-quinazolinones-using-a-csp3-h-functionalisation-cyclisation-strategy
#8
Aniket V A Gholap, Soham Maity, Carola Schulzke, Debabrata Maiti, Anant R Kapdi
A series of 2,3-disubstituted-4(3H)-quinazolinones were synthesised via a copper-catalysed Csp3-H functionalisation/cyclisation of 2-amino-N,N-dialkylbenzamides. In comparison to the reported methods this strategy allows an easy access to diversely substituted quinazolinones under mild conditions in air. The reaction also exhibits good functional group tolerance and would be of value to heterocyclic researchers as well as pharmaceutical process chemists. The reaction is proposed to proceed through a double SET type radical mechanism...
August 14, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28805572/personalized-medicine-and-nonmotor-symptoms-in-parkinson-s-disease
#9
Nataliya Titova, K Ray Chaudhuri
Parkinson's disease (PD) is a multineurotransmitter dysfunction related disorder resulting in a range of motor and nonmotor symptoms. Phenotypic heterogeneity is pronounced in PD and nonmotor symptoms dominant subtypes have been described. These endophenotypes may be underpinned by considerable nondopaminergic dysfunction; however, conventional treatment of PD continues to be mostly reliant on dopamine replacement strategy or manipulation of brain dopaminergic pathways. Consequently, treatment of many nondopaminergic nonmotor and some motor symptoms remains a key unmet need...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28805468/long-term-persistence-with-single-pill-fixed-dose-combination-therapy-versus-two-pills-of-amlodipine-and-perindopril-for-hypertension-australian-experience
#10
Leon A Simons, Eric Chung, Michael Ortiz
OBJECTIVE: To study treatment persistence and mortality using a single-pill, fixed-dose combination tablet compared with a two-pill combination for hypertension. RESEARCH DESIGN AND METHODS: We analyzed Australian Pharmaceutical Benefit Scheme records 2011-2014 in a 10% random sample of concessional patients prescribed concomitant amlodipine and perindopril - either as a single-pill, fixed-dose combination tablet (n = 9340) or as two-pill combination therapy (n = 3093)...
August 14, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28805268/organo-photoredox-catalyzed-oxidative-dehydrogenation-of-n-heterocycles
#11
Balaraman Ekambaram, Manoj K Sahoo, Garima Jaiswal, Jagannath Rana
We report here for the first time the catalytic oxidative dehydrogenation of N-heterocycles by a visible-light organo-photoredox catalyst with low catalyst loading (0.1 - 1 mol%). The reaction proceeds efficiently under base- and additive-free conditions with ambient air at room temperature. The utility of this benign approach is demonstrated by the synthesis of various pharmaceutically relevant N-heteroarenes such as quinoline, quinoxaline, quinazoline, acridine, and indole.
August 14, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28805084/covalent-immobilisation-of-transglutaminase-stability-and-applications-in-protein-pegylation
#12
Antonella Grigoletto, Anna Mero, Hiroki Yoshioka, Oddone Schiavon, Gianfranco Pasut
Microbial transglutaminase enzyme (mTGase) is an extremely useful enzyme that is increasingly employed in the food and pharmaceutical industries and as a tool for protein modification and tagging. The current study describes how we immobilised mTGase (iTGase) on a solid support to improve its stability during the PEGylation process by which polyethylene glycol chains are attached to protein and peptide drugs. When the enzyme was immobilised at the N-terminal sequence on agarose beads, it retained more than 53% of its starting activity...
August 13, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28804696/neonatal-safety-information-reported-to-the-fda-during-drug-development-studies
#13
Debbie Avant, Gerri Baer, Jason Moore, Panli Zheng, Alfred Sorbello, Ron Ariagno, Lynne Yao, Gilbert J Burckart, Jian Wang
BACKGROUND: Relatively few neonatal drug development studies have been conducted, but an increase is expected with the enactment of the Food and Drug Administration Safety and Innovation Act (FDASIA). Understanding the safety of drugs studied in neonates is complicated by the unique nature of the population and the level of illness. The objective of this study was to examine neonatal safety data submitted to the FDA in studies pursuant to the Best Pharmaceuticals for Children Act (BPCA) and the Pediatric Research Equity Act (PREA) between 1998 and 2015...
2017: Therapeutic Innovation & Regulatory Science
https://www.readbyqxmd.com/read/28804600/analysis-of-health-economics-assessment-reports-for-pharmaceuticals-in-france-understanding-the-underlying-philosophy-of-ceesp-assessment
#14
Mondher Toumi, Anastasiia Motrunich, Aurélie Millier, Cécile Rémuzat, Christos Chouaid, Bruno Falissard, Samuel Aballéa
Background: Despite the guidelines for Economic and Public Health Assessment Committee (CEESP) submission having been available for nearly six years, the dossiers submitted continue to deviate from them, potentially impacting product prices. Objective: to review the reports published by CEESP, analyse deviations from the guidelines, and discuss their implications for the pricing and reimbursement process. Study design: CEESP reports published until January 2017 were reviewed, and deviations from the guidelines were extracted...
2017: Journal of Market Access & Health Policy
https://www.readbyqxmd.com/read/28803799/constructing-novel-dihydrofuran-and-dihydroisoxazole-analogues-of-isocombretastatin-4-as-tubulin-polymerization-inhibitors-through-3-2-reactions
#15
Ming-Yu Song, Chen-Yu Cao, Qiu-Rui He, Qing-Miao Dong, Ding Li, Jiang-Jiang Tang, Jin-Ming Gao
[3+2] reactions play a key role in constructing various pharmaceutical moleculars. In this study, using Mn(OAc)3 mediated and 1,3-dipolar [3+2] cyclization reactions, 38 novel dihydrofuran and dihydroisoxazole analogues of isoCA-4 were synthesized as inhibitors of tubulin polymerization. Among them, compound 6g was found to be the most potent cytotoxic agents against PC-3 cells with IC50 value of 0.47μM, and compound 5p exhibted highest activity on HeLa cells with IC50 vaule of 2.32µM. Tubulin polymerization assay revealed that 6g was a dose-dependent and effective inhibitor of tubulin assembly...
July 29, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28803741/the-cardiovascular-toxicity-of-triadimefon-in-early-life-stage-of-zebrafish-and-potential-implications-to-human-health
#16
Hong-Cui Liu, Tian-Yi Chu, Li-Li Chen, Wen-Jun Gui, Guo-Nian Zhu
The health risk of triadimefon (TF) to cardiovascular system of human is still unclear, especially to pesticide suicides population, occupational population (farmers, retailers and pharmaceutical workers), and special population (young children and infants, pregnant women, older people, and those with compromised immune systems) who are at a greater risk. Therefore, firstly we explored the toxic effects and possible mechanism of cardiovascular toxicity induced by TF using zebrafish model. Zebrafish at stage of 48 h post fertilization (hpf) exposed to TF for 24 h exhibited morphological malformations which were further confirmed by histopathologic examination, including pericardial edema, circulation abnormalities, serious venous thrombosis and increased distance between the sinus venosus (SV) and bulbus arteriosus (BA) regions of the heart...
August 10, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28803725/schistosomiasis-drugs-used-and-treatment-strategies
#17
REVIEW
Lidiany da Paixão Siqueira, Danilo Augusto Ferreira Fontesa, Cindy Siqueira Britto Aguilera, Taysa Renata Ribeiro Timoteo, Matheus Alves Angelos, Laysa Creusa Paes Barreto Barros Silva, Camila Gomes de Melo, Larissa Araújo Rolim, Rosali Maria Ferreira da Silva, Pedro José Rolim Neto
Neglected tropical diseases (NTDs) affect millions of people in different geographic regions, especially the poorest and most vulnerable. Currently NTDs are prevalent in 149 countries, seventeen of these neglected tropical parasitic diseases are classified as endemic. One of the most important of these diseases is schistosomiasis, also known as bilharzia, a disease caused by the genus Schistosoma. It presents several species, such as S. haematobium, S. japonicum and S. mansoni, the latter being responsible for parasitosis in Brazil...
August 10, 2017: Acta Tropica
https://www.readbyqxmd.com/read/28803645/liquid-chromatography-quadrupole-orbitrap-mass-spectrometry-method-for-selected-pharmaceuticals-in-water-samples
#18
Jalal T Althakafy, Chadin Kulsing, Michael R Grace, Philip J Marriott
This study developed an analytical approach for sub-ppb level detection and confirmation of 13 pharmaceuticals and personal care products (PPCPs) in water samples using ultra high pressure liquid chromatography hyphenated with a quadrupole Orbitrap mass spectrometer (UHPLC- Q-Orbitrap-MS). Sample preparation was performed by using solid phase extraction (SPE) employing hydrophilic-lipophilic balance cartridges, with elution of sorbed analytes using methanol. Acceptable automatic gain control (AGC) target and maximum injection time (IT) were 1×10(6) and 200ms, respectively, resulting in a mass accuracy <2ppm...
August 3, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28803364/volatile-terpenoids-multiple-functions-biosynthesis-modulation-and-manipulation-by-genetic-engineering
#19
REVIEW
Farhat Abbas, Yanguo Ke, Rangcai Yu, Yuechong Yue, Sikandar Amanullah, Muhammad Muzammil Jahangir, Yanping Fan
Terpenoids play several physiological and ecological functions in plant life through direct and indirect plant defenses and also in human society because of their enormous applications in the pharmaceutical, food and cosmetics industries. Through the aid of genetic engineering its role can by magnified to broad spectrum by improving genetic ability of crop plants, enhancing the aroma quality of fruits and flowers and the production of pharmaceutical terpenoids contents in medicinal plants. Terpenoids are structurally diverse and the most abundant plant secondary metabolites, playing an important role in plant life through direct and indirect plant defenses, by attracting pollinators and through different interactions between the plants and their environment...
August 12, 2017: Planta
https://www.readbyqxmd.com/read/28803263/carotenoids-from-the-extreme-halophilic-archaeon-haloterrigena-turkmenica-identification-and-antioxidant-activity
#20
Giuseppe Squillaci, Roberta Parrella, Virginia Carbone, Paola Minasi, Francesco La Cara, Alessandra Morana
Haloterrigena turkmenica was able to synthesize carotenoids when grown in halobacteria medium. These molecules have antioxidant properties and find application in food, cosmetic, and pharmaceutical fields. The carotenoids were extracted with methanol, separated by RP-HPLC, and identified by mass spectrometry and UV/Vis spectra analyses. The C50 carotenoids were the main pigments, and C30, C40, and C51 carotenoids were also detected. Seven geometric isomers were distinguished for bacterioruberin, monoanhydrobacterioruberin, and bisanhydrobacterioruberin...
August 12, 2017: Extremophiles: Life Under Extreme Conditions
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