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https://www.readbyqxmd.com/read/28068097/characterization-of-phase-separation-propensity-for-amorphous-spray-dried-dispersions
#1
Daniel McNamara, Shawn Yin, Duohai Pan, George Crull, Peter Timmins, Balvinder Vig
A generalized screening approach, applying isothermal calorimetry at 37°C 100%RH, to formulations of spray dried dispersions (SDDs) for two active pharmaceutical ingredients (APIs) (BMS-903452 and BMS-986034) is demonstrated. APIs 452 and 034, with similar chemotypes, were synthesized and promoted during development for oral dosing. Both APIs were formulated as SDDs for animal exposure studies using the polymer hydroxypropylmethlycellulose acetyl succinate M grade (HPMCAS M). 452 formulated at 30% (wt/wt%) was an extremely robust SDD that was able to withstand 40°C 75%RH open storage conditions for 6 months with no physical evidence of crystallization or loss of dissolution performance...
January 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28062541/evaluation-of-a-novel-renewable-hepatic-cell-model-for-prediction-of-clinical-cyp3a4-induction-using-a-correlation-based-ris-approach
#2
Rongjun Zuo, Feng Li, Sweta Parikh, Li Cao, Kirsten L Cooper, Yulong Hong, Jin Liu, Ronald A Faris, Daochuan Li, Hongbing Wang
Metabolism enzyme induction-mediated drug-drug interactions need to be carefully characterized in vitro for drug candidates in order to predict in vivo outcomes of safety risk and therapeutic efficiency. Currently, both the FDA and EMA recommend using primary human hepatocytes as the "Gold Standard" in vitro test system for studying the induction potential of candidate drugs on cytochrome P450 (CYP), CYP3A4, CYP1A2, and CYP2B6. However, primary human hepatocytes are known to bear inherent limitations such as limited supply and large lot-to-lot variations which result in an experimental burden to qualify new lots...
January 6, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28049248/nestin-expression-in-the-adult-mouse-retina-with-pharmaceutically-induced-retinal-degeneration
#3
Chan Hee Moon, Heeyoon Cho, Yoon Kyung Kim, Tae Kwann Park
The present study investigated the temporal pattern and cellular localization of nestin in the adult mouse retina with pharmaceutically induced retinal degeneration using N-methyl-N-nitrosourea (MNU). After a single intraperitoneal injection of MNU in 8-week-old C57BL/6 mice, the animals were sacrificed at 1, 3, 5, 7, and 21 days (n = 6, in each stage). The eyes were examined by means of immunohistochemical tests using nestin, ionized calcium-binding adaptor molecule (Iba-1), CD11b, F4/80, and glial fibrillary acidic protein (GFAP)...
February 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/28025997/a-novel-chk1-binding-peptide-that-enhances-genotoxic-sensitivity-through-the-cellular-redistribution-of-nuclear-chk1
#4
Kwang Seok Kim, Kyu Jin Choi, Sangwoo Bae
Since checkpoint kinase 1 (Chk1) is an essential factor for cell viability following DNA damage, the inhibition of Chk1 has been a major focus of pharmaceutical development to enhance the sensitivity of tumor cells to chemo- and radiotherapy that damage DNA. However, due to the off-target effects of conventional Chk1-targeting strategies and the toxicity of Chk1 inhibitors, alternative strategies are required to target Chk1. To facilitate such efforts, in this study, we identified a specific Chk1-binding 12-mer peptide from the screening of a phage display library and characterized the peptide in terms of cellular cytotoxicity, and in terms of its effect on Chk1 activity and sensitivity to genotoxic agents...
November 2016: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28024262/levothyroxine-sodium-revisited-a-wholistic-structural-elucidation-approach-of-new-impurities-via-hplc-hrms-ms-on-line-h-d-exchange-nmr-spectroscopy-and-chemical-synthesis
#5
M Ruggenthaler, J Grass, W Schuh, C G Huber, R J Reischl
The structural elucidation of unknown pharmaceutical impurities plays an important role in the quality control of newly developed and well-established active pharmaceutical ingredients (APIs). The United States Pharmacopeia (USP) monograph for the API Levothyroxine Sodium, a synthetic thyroid hormone, features two high pressure liquid chromatography (HPLC) methods using UV-VIS absorption detection to determine organic impurities in the drug substance. The impurity profile of the first USP method ("Procedure 1") has already been extensively studied, however for the second method ("Procedure 2"), which exhibits a significantly different impurity profile, no wholistic structural elucidation of impurities has been performed yet...
December 14, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28004818/3-d-microwell-array-system-for-culturing-virus-infected-tumor-cells
#6
Rami El Assal, Umut A Gurkan, Pu Chen, Franceline Juillard, Alessandro Tocchio, Thiruppathiraja Chinnasamy, Chantal Beauchemin, Sebnem Unluisler, Serli Canikyan, Alyssa Holman, Srikar Srivatsa, Kenneth M Kaye, Utkan Demirci
Cancer cells have been increasingly grown in pharmaceutical research to understand tumorigenesis and develop new therapeutic drugs. Currently, cells are typically grown using two-dimensional (2-D) cell culture approaches, where the native tumor microenvironment is difficult to recapitulate. Thus, one of the main obstacles in oncology is the lack of proper infection models that recount main features present in tumors. In recent years, microtechnology-based platforms have been employed to generate three-dimensional (3-D) models that better mimic the native microenvironment in cell culture...
December 22, 2016: Scientific Reports
https://www.readbyqxmd.com/read/28004015/influenza-infection-modulates-vesicular-trafficking-and-induces-golgi-complex-disruption
#7
Vibha Yadav, Antonito T Panganiban, Kerstin Honer Zu Bentrup, Thomas G Voss
Influenza A virus (IFV) replicates its genome in the nucleus of infected cells and uses the cellular protein transport system for genome trafficking from the nucleus to the plasma membrane. However, many details of the mechanism of this process, and its relationship to subsequent cytoplasmic virus trafficking, have not been elucidated. We examined the effect of nuclear transport inhibitors Leptomycin B (LB), 5,6 dichloro-1-β-d-ribofuranosyl-benzimidazole (DRB), the vesicular transport inhibitor Brefeldin A (BFA), the caspase inhibitor ZWEHD, and microtubule inhibitor Nocodazole (NOC) on virus replication and intracellular trafficking of viral nucleoprotein (NP) from the nucleus to the ER and Golgi...
December 2016: Virusdisease
https://www.readbyqxmd.com/read/27996302/determination-of-interference-during-in-vitro-pyrogen-detection-development-and-characterization-of-a-cell-based-assay
#8
Linda Palma, Francesca Rossetti, Sabrina Dominici, Costantina Buondelmonte, Marco B L Rocchi, Gian P Rizzardi, Giuliana Vallanti, Mauro Magnani
Contamination of pharmaceutical products and medical devices with pyrogens such as endotoxins is the most common cause of systemic inflammation and, in worst cases, of septic shock. Thus, quantification of pyrogens is crucial. The limulus amebocyte lysate (LAL)-based assays are the reference tests for in vitro endotoxin detection, in association with the in vivo rabbit pyrogen test (RPT), according to European Pharmacopoeia (EP 2.6.14), and U.S. Pharmacopoeia (USP <85>). However, several substances interfere with LAL assay, while RPT is not accurate, not quantitative, and raises ethical limits...
December 20, 2016: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/27995760/enri-a-tool-for-selecting-structure-based-virtual-screening-target-conformations
#9
Rahmad Akbar, Siti Azma Jusoh, Rommie E Amaro, Volkhard Helms
Finding pharmaceutically relevant target conformations from an arbitrary set of protein conformations remains a challenge in structure-based virtual screening (SBVS). The growth in the number of available conformations, either experimentally determined or computationally derived, obscures the situation further. While the inflated conformation space potentially contains viable druggable targets, the increase of conformational complexity, as a consequence, poses a selection problem. To address this challenge, we took advantage of machine learning methods, namely an over-sampling and a binary classification procedure, and present a novel method to select druggable receptor conformations...
December 20, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27987924/quantitative-analysis-of-the-major-linkage-region-tetrasaccharides-in-heparin
#10
Yin Chen, Kalib St Ange, Lei Lin, Xinyue Liu, Xing Zhang, Robert J Linhardt
Heparin is a polysaccharide based anticoagulant drug composed of a complex mixture of glycosaminoglycan chains and peptidoglycosaminoglycan chains. In an effort to better characterize this important polysaccharide based drug, we examined the peptide components of the minor peptidoglycosaminoglycan chains comprising heparin. Three different the glycan-peptide linkage regions tetrasaccharide fragments were isolated from pharmaceutical heparin using heparin lyase II and characterized the structure of these tetrasaccharides using nuclear magnetic resonance spectroscopy and mass spectrometry...
February 10, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/27979317/estrogen-receptor-%C3%AE-as-a-pharmaceutical-target
#11
REVIEW
Margaret Warner, Bo Huang, Jan-Ake Gustafsson
A major issue in clinical endocrinology today is how to use hormones to achieve the health benefits that they clearly can provide but avoid the negative side effects, that is, how to develop more precise medicines. This problem of how to use hormones is pervasive in clinical endocrinology. It is true for estrogen, progesterone, androgen, vitamin D, and thyroid hormone, and the problem is amplified in the case of new ligands for the more recently discovered nuclear receptors. Selective targeting of hormone receptor subtypes is one attractive way to harness the beneficial effects of hormones while reducing unwanted side effects...
January 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/27951698/structure-and-mobility-of-lactose-in-lactose-sodium-montmorillonite-nanocomposites
#12
Joel Hellrup, Michael Holmboe, Karol P Nartowski, Yaroslav Z Khimyak, Denny Mahlin
This study aims at investigating the molecular level organization and molecular mobility in montmorillonite nanocomposites with the uncharged organic low-molecular-weight compound lactose commonly used in pharmaceutical drug delivery, food technology, and flavoring. Nanocomposites were prepared under slow and fast drying conditions, attained by drying at ambient conditions and by spray-drying, respectively. A detailed structural investigation was performed with modulated differential scanning calorimetry, powder X-ray diffraction, solid-state nuclear magnetic resonance spectroscopy, scanning electron microscopy, microcalorimetry, and molecular dynamics simulations...
December 13, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/27938895/dispersive-raman-spectroscopy-for-quantifying-amorphous-drug-content-in-intact-tablets
#13
Busolo Wa Wabuyele, Sutthilug Sotthivirat, George X Zhou, Jason Ash, Sundeep S Dhareshwar
Process-induced inadvertent phase change of an active pharmaceutical ingredient in a drug product could impact chemical stability, physical stability, shelf life, and bioperformance. In this study, dispersive Raman spectroscopy is presented as an alternative method for the nondestructive, high-throughput, at-line quantification of amorphous conversion. A quantitative Raman method was developed using a multivariate partial least squares (PLS) regression calibration technique with solid-state nuclear magnetic resonance (ssNMR) spectroscopy as the reference method...
December 6, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27934635/metabolism-of-the-mek1-2-inhibitor-pimasertib-involves-a-novel-conjugation-with-phospho-ethanolamine-in-patients-with-solid-tumors
#14
Holger Scheible, Friedrich Kraetzer, Andreas Marx, Andreas Johne, Elmar Wimmer
Pimasertib (AS703026 or MSC1936369B) is a selective inhibitor of MEK1/2, the mitogen-activated protein kinase (MAPK) signaling pathway, which is often dysregulated in cancer cells. Pimasertib has shown potent preclinical anti tumor activity and its clinical activity is being investigated in various tumor types. In this phase I study, the disposition and biotransformation of (14)C-radiolabeled pimasertib was investigated in six patients with locally advanced or metastatic solid tumors (NCT 01713036). Ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) and radiodetection techniques were used to investigate the profiles and structures of metabolites in plasma, urine and feces after a single oral dose of (14)C-pimasertib...
December 1, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27922103/hypothalamic-activation-is-essential-for-endotoxemia-induced-acute-muscle-wasting
#15
Kaipeng Duan, Qiyi Chen, Minhua Cheng, Chenyan Zhao, Zhiliang Lin, Shanjun Tan, Fengchan Xi, Tao Gao, Jialiang Shi, Juanhong Shen, Weiqin Li, Wenkui Yu, Jieshou Li, Ning Li
Growing evidence suggests acute skeletal muscle wasting is a key factor affecting nutritional support and prognosis in critical patients. Previously, plenty of studies of muscle wasting focused on the peripheral pathway, little was known about the central role. We tested the hypothesis whether central inflammatory pathway and neuropeptides were involved in the process. In lipopolysaccharide (LPS) treated rats, hypothalamic NF-κB pathway and inflammation were highly activated, which was accompanied with severe muscle wasting...
December 6, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27920947/the-daniel-k-inouye-college-of-pharmacy-scripts-poha-berry-physalis-peruviana-with-potential-anti-inflammatory-and-cancer-prevention-activities
#16
Leng Chee Chang, Mayuramas Sang-Ngern, John M Pezzuto, Carolyn Ma
The Daniel K. Inouye College of Pharmacy, during a historic event in Spring 2016, graduated the first two students in the Pacific region to earn a PhD in pharmaceutical sciences at the University of Hawai'i at Hilo. The college offers PhD programs in these five disciplines: Cancer Biology, Medicinal Chemistry, Pharmaceutics, Pharmacognosy, and Pharmacology. One of the Pharmacognosy dissertations focused on plant-derived natural products with potential anti-inflammatory and cancer chemopreventive activities...
November 2016: Hawai'i Journal of Medicine & Public Health: a Journal of Asia Pacific Medicine & Public Health
https://www.readbyqxmd.com/read/27916640/ppar-agonists-could-tissue-targeting-pave-the-way
#17
Anne Bugge, Dorte Holst
Over the last couple of decades, the PPAR family of transcription factors has received much attention from the pharmaceutical industry due to their profound ability to improve glucose and lipid metabolism upon agonist activation. However, more recently the interest in these nuclear receptors has faded because several clinical trials have shown that it is difficult to develop a ligand that significantly ameliorates glucose and lipid metabolism disorders without concomitantly inducing unacceptable side-effects...
December 2, 2016: Biochimie
https://www.readbyqxmd.com/read/27900420/nmr-based-metabolomic-approach-to-study-urine-samples-of-chronic-inflammatory-rheumatic-disease-patients
#18
Alessia Vignoli, Donatella Maria Rodio, Anna Bellizzi, Anatoly Petrovich Sobolev, Elena Anzivino, Monica Mischitelli, Leonardo Tenori, Federico Marini, Roberta Priori, Rossana Scrivo, Guido Valesini, Ada Francia, Manuela Morreale, Maria Rosa Ciardi, Marco Iannetta, Cristiana Campanella, Donatella Capitani, Claudio Luchinat, Valeria Pietropaolo, Luisa Mannina
The nuclear magnetic resonance (NMR)-based metabolomic approach was used as analytical methodology to study the urine samples of chronic inflammatory rheumatic disease (CIRD) patients. The urine samples of CIRD patients were compared to the ones of both healthy subjects and patients with multiple sclerosis (MS), another immuno-mediated disease. Urine samples collected from 39 CIRD patients, 25 healthy subjects, and 26 MS patients were analyzed using (1)H NMR spectroscopy, and the NMR spectra were examined using partial least squares-discriminant analysis (PLS-DA)...
November 30, 2016: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/27889102/analysis-of-gene-expression-and-regulation-implicates-c2h9orf152-has-an-important-role-in-calcium-metabolism-and-chicken-reproduction
#19
Long Liu, Yanfeng Fan, Zhenhe Zhang, Chan Yang, Tuoyu Geng, Daoqing Gong, Zhuocheng Hou, Zhonghua Ning
The reproductive system of a female bird is responsible for egg production. The genes highly expressed in oviduct are potentially important. From RNA-seq analysis, C2H9orf152 (an orthologous gene of human C9orf152) was identified as highly expressed in chicken uterus. To infer its function, we obtained and characterized its complete cDNA sequence, determined its spatiotemporal expression, and probed its transcription factor(s) through pharmaceutical approach. Data showed that the complete cDNA sequence was 1468bp long with a 789bp of open reading frame...
January 2017: Animal Reproduction Science
https://www.readbyqxmd.com/read/27878482/an-in-vitro-approach-for-water-quality-determination-activation-of-nf-%C3%AE%C2%BAb-as-marker-for-cancer-related-stress-responses-induced-by-anthropogenic-pollutants-of-drinking-water
#20
Luis F Spitta, Sebastian Diegeler, Christa Baumstark-Khan, Christine E Hellweg
Epidemiological studies show that there is a link between urban water pollution and increase in human morbidity and mortality. With the increase in number of new substances arising from the chemical, pharmaceutical, and agricultural industries, there is an urgent need to develop biological test systems for fast evaluation of potential risks to humans and the environmental ecosystems. Here, a combined cellular reporter assay based on the cellular survival and the stress-induced activation of the survival-promoting factor nuclear factor κB (NF-κB) and its use for the detection of cytotoxicity and cancer-related stress responses is presented...
November 22, 2016: Environmental Science and Pollution Research International
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