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https://www.readbyqxmd.com/read/29166624/impact-of-processing-methods-on-the-dissolution-of-artemether-from-two-non-ordered-mesoporous-silicas
#1
Hira Tahir, Yasser Shahzad, Laura J Waters, Talib Hussain, Abid Mehmood Yousaf, Tariq Mahmood, Rizwan Sheikh
Poor aqueous solubility is often linked with a poor dissolution rate and ultimately, limited bioavailability of pharmaceutical compounds. This study describes the application of mesoporous materials (Syloid 244 and Syloid AL1) in improving the dissolution rate of a drug with poor aqueous solubility, namely artemether, utilising different processing methods including physical mixing, co-grinding and solid dispersions prepared by solvent evaporation and the lyophilisation technique. The prepared formulations were extensively characterised for their solid-state properties and the drug release attributes were studied...
November 19, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29166563/mechanochemical-synthesis-of-pharmaceutical-cocrystal-suspensions-via-hot-melt-extrusion-enhancing-cocrystal-yield
#2
Shu Li, Tao Yu, Yiwei Tian, Colette Lagan, David S Jones, Gavin P Andrews
Pharmaceutical cocrystals have attracted increasing attention over the past decade as an alternative way to modify the physicochemical properties and hence improve the bioavailability of a drug, without sacrificing thermodynamic stability. Our previous work has demonstrated the viability of in-situ formation of ibuprofen/isonicotinamide cocrystal suspensions within a matrix carrier via a single-step hot-melt extrusion (HME) process. The key aim of the current work is to establish optimised processing conditions to improve cocrystal yield within extruded matrices...
November 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29161028/exploring-the-active-centre-of-lsd1-corest-complex-by-molecular-dynamics-simulation-utilizing-its-co-crystallized-cofactor-tetrahydrofolate-as-a-probe
#3
Waleed A A Zalloum, Hiba M Zalloum
Epigenetic targeting of cancer is a recent era to manipulate the gene without destroying the genetic material. Lysine-specific demethylase 1 (LSD1) is one of the enzymes associated with the chromatin for post-translational modifications, where it demethylates lysine amino acid in the chromatin H3 tail. Many studies showed that inhibiting LSD1 could potentially be used to treat cancer epigenetically. LSD1 is associated with its corepressor protein CoREST, and uses tetrahydrofolate as a cofactor to accept CH2 from the demethylation process...
November 21, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29159257/development-and-analytical-performance-of-a-new-architect-automated-dipeptidyl-peptidase-4-immunoassay
#4
Philip M Hemken, Nicolette M Jeanblanc, Tracey Rae, Susan E Brophy, Maria J Datwyler, Ying Xu, T Scott Manetz, Inna Vainshtein, Meina Liang, Xiaodong Xiao, Partha S Chowdhury, Chien-Ying Chang, Katie Streicher, Lydia Greenlees, Koustubh Ranade, Gerard J Davis
Background: Dipeptidyl peptidase-4 (DPP-4) may be a suitable biomarker to identify people with severe asthma who have greater activation of the interleukin-13 (IL-13) pathway and may therefore benefit from IL-13-targeted treatments. We report the analytical performance of an Investigational Use Only immunoassay and provide data on the biological range of DPP-4 concentrations. Methods: We assessed assay performance, utilising analyses of precision, linearity and sensitivity; interference from common endogenous assay interferents, and from asthma and anti-diabetic medications, were also assessed...
December 2017: Pract Lab Med
https://www.readbyqxmd.com/read/29156708/a-preclinical-evaluation-of-the-mek-inhibitor-refametinib-in-her2-positive-breast-cancer-cell-lines-including-those-with-acquired-resistance-to-trastuzumab-or-lapatinib
#5
John O'Shea, Mattia Cremona, Clare Morgan, Malgorzata Milewska, Frankie Holmes, Virginia Espina, Lance Liotta, Joyce O'Shaughnessy, Sinead Toomey, Stephen F Madden, Aoife Carr, Naomi Elster, Bryan T Hennessy, Alex J Eustace
Purpose: The MEK/MAPK pathway is commonly activated in HER2-positive breast cancer, but little investigation of targeting this pathway has been undertaken. Here we present the results of an in vitro preclinical evaluation of refametinib, an allosteric MEK1/2 inhibitor, in HER2-positive breast cancer cell lines including models of acquired resistance to trastuzumab or lapatinib. Methods: A panel of HER2-positive breast cancer cells were profiled for mutational status and also for anti-proliferative response to refametinib alone and in combination with the PI3K inhibitor (PI3Ki) copanlisib and the HER2-targeted therapies trastuzumab and lapatinib...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29155388/polyelectrolyte-multilayers-for-bio-applications-recent-advancements
#6
REVIEW
Suman Pahal, Ruchi Gakhar, Ashok M Raichur, Manoj M Varma
The synergistic relationship between structure and the bulk properties of polyelectrolyte multilayer (PEM) films has generated tremendous interest in their application for loading and release of bioactive species. Layer-by-layer assembly is the simplest, cost effective process for fabrication of such PEMs films, leading to one of the most widely accepted platforms for incorporating biological molecules with nanometre precision. The bulk reservoir properties of PEM films render them a potential candidate for applications such as biosensing, drug delivery and tissue engineering...
December 2017: IET Nanobiotechnology
https://www.readbyqxmd.com/read/29146633/comparison-of-outcomes-of-antibiotic-drugs-and-appendectomy-coda-trial-a-protocol-for-the-pragmatic-randomised-study-of-appendicitis-treatment
#7
Giana H Davidson, David R Flum, David A Talan, Larry G Kessler, Danielle C Lavallee, Bonnie J Bizzell, Farhood Farjah, Skye D Stewart, Anusha Krishnadasan, Erin E Carney, Erika M Wolff, Bryan A Comstock, Sarah E Monsell, Patrick J Heagerty, Annie P Ehlers, Daniel A DeUgarte, Amy H Kaji, Heather L Evans, Julianna T Yu, Katherine A Mandell, Ian C Doten, Kevin S Clive, Karen M McGrane, Brandon C Tudor, Careen S Foster, Darin J Saltzman, Richard C Thirlby, Erin O Lange, Amber K Sabbatini, Gregory J Moran
INTRODUCTION: Several European studies suggest that some patients with appendicitis can be treated safely with antibiotics. A portion of patients eventually undergo appendectomy within a year, with 10%-15% failing to respond in the initial period and a similar additional proportion with suspected recurrent episodes requiring appendectomy. Nearly all patients with appendicitis in the USA are still treated with surgery. A rigorous comparative effectiveness trial in the USA that is sufficiently large and pragmatic to incorporate usual variations in care and measures the patient experience is needed to determine whether antibiotics are as good as appendectomy...
November 15, 2017: BMJ Open
https://www.readbyqxmd.com/read/29145996/-comparative-profile-of-the-use-of-filter-needles-in-quebec-and-france-in-healthcare-facility
#8
L Painchart, P Odou, J-F Bussières
OBJECTIVES: The manipulation of drugs from glass ampules can generate particles when the ampule is broken. Several authors recommend the use of filter needle to withdraw the drug content. The main objective is to establish an inventory of the use of filter needles and the perception of pharmacists in Quebec and in France. METHODS: This is a cross-sectional descriptive study. A questionnaire was sent to all health facilities in Quebec (n=30) and a selection of hospitals in France (n=100)...
November 13, 2017: Annales Pharmaceutiques Françaises
https://www.readbyqxmd.com/read/29143575/determination-of-illegal-adulteration-of-dietary-supplements-with-synthetic-hair-growth-compounds-by-uplc-and-lc-q-tof-ms
#9
Ji Hyun Lee, Gihaeng Kang, Han Na Park, Jihee Kim, Nam Sook Kim, Seongsoo Park, Sung-Kwan Park, Sun Young Baek, Hoil Kang
In this study, we developed a UPLC-PDA and LC-Q-TOF/MS method to identify and measure the following prohibited substances that may be found in dietary supplements: triaminodil, minoxidil, bimatoprost, alimemazine, diphenylcyclopropenone, α-tradiol, finasteride, methyltestosterone, spironolatone, flutamide, cyproterone, dutasteride, and testosterone 17-propionate.The method was validated according to International Conference on Harmonization guidelines in terms of specificity, linearity, accuracy, precision, LOD, LOQ, recovery, and stability...
November 16, 2017: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
https://www.readbyqxmd.com/read/29138099/effect-of-an-antimicrobial-stewardship-programme-on-antimicrobial-utilisation-and-costs-in-patients-with-leukaemia-a-retrospective-interventional-controlled-study
#10
Miranda So, Muhammad Mamdani, Andrew Morris, Tim Lau, Raewyn Broady, Uday Deotare, Jennifer Grant, Dennis Dong Hwan Kim, Aaron D Schimmer, Andre Schuh, Salomeh Shajari, Marilyn Steinberg, Chaim M Bell, Shahid Husain
OBJECTIVES: To examine the effectiveness of an antimicrobial stewardship programme (ASPs) on utilisation and cost of antimicrobials in leukaemia patients in Canada. METHODS: We conducted a multisite, retrospective, observational time-series study from 2005 to 2013. We implemented academic detailing as the intervention of an ASP in leukaemia units at a hospital, piloted February-July 2010, then fully implemented December 2010-March 2013, with no intervention in August-November 2010...
November 11, 2017: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/29137884/uptake-and-effectiveness-of-folfirinox-for-advanced-pancreatic-cancer-a-population-based-study
#11
S Karim, J Zhang-Salomans, J J Biagi, T Asmis, C M Booth
AIMS: Although FOLFIRINOX is a standard treatment option for advanced pancreas cancer, there are few data describing utilisation and effectiveness in routine clinical practice. Here we report practice patterns and outcomes in the general population of Ontario, Canada. MATERIALS AND METHODS: Using the Ontario Cancer Registry and New Drug Funding Program, we identified all patients with pancreas cancer treated with palliative intent gemcitabine or FOLFIRINOX in Ontario during 2006-2014...
November 11, 2017: Clinical Oncology: a Journal of the Royal College of Radiologists
https://www.readbyqxmd.com/read/29133323/characteristics-and-healthcare-utilisation-patterns-of-high-cost-beneficiaries-in-the-netherlands-a-cross-sectional-claims-database-study
#12
Joost Johan Godert Wammes, Marit Tanke, Wilma Jonkers, Gert P Westert, Philip Van der Wees, Patrick Pt Jeurissen
OBJECTIVE: To determine medical needs, demographic characteristics and healthcare utilisation patterns of the top 1% and top 2%-5% high-cost beneficiaries in the Netherlands. DESIGN: Cross-sectional study using 1 year claims data. We broke down high-cost beneficiaries by demographics, the most cost-incurring condition per beneficiary and expensive treatment use. SETTING: Dutch curative health system, a health system with universal coverage...
November 12, 2017: BMJ Open
https://www.readbyqxmd.com/read/29127626/impact-of-infliximab-and-etanercept-biosimilars-on-biological-disease-modifying-antirheumatic-drugs-utilisation-and-nhs-budget-in-the-uk
#13
Mohammed I Aladul, Raymond W Fitzpatrick, Stephen R Chapman
OBJECTIVE: Biological disease-modifying antirheumatic drugs (bDMARDs) are effective but expensive options for treating rheumatoid arthritis. The introduction of infliximab and etanercept biosimilars presents a significant potential cost saving in a financially constrained health system such as the National Health Service (NHS) in the UK. This study examines the impact of the introduction of infliximab and etanercept biosimilars on the utilisation of bDMARDs and subsequent budget impact...
November 10, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/29124308/the-%C3%AE-6-%C3%AE-7-region-of-the-hsp70-substrate-binding-domain-mediates-heat-shock-response-and-prion-propagation
#14
Linan Xu, Weibin Gong, Sarah A Cusack, Huiwen Wu, Harriët M Loovers, Hong Zhang, Sarah Perrett, Gary W Jones
Hsp70 is a highly conserved chaperone that in addition to providing essential cellular functions and aiding in cell survival following exposure to a variety of stresses is also a key modulator of prion propagation. Hsp70 is composed of a nucleotide-binding domain (NBD) and substrate-binding domain (SBD). The key functions of Hsp70 are tightly regulated through an allosteric communication network that coordinates ATPase activity with substrate-binding activity. How Hsp70 conformational changes relate to functional change that results in heat shock and prion-related phenotypes is poorly understood...
November 9, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/29123429/assessment-of-prescribed-medications-and-pattern-of-distribution-for-potential-drug-drug-interactions-among-chronic-kidney-disease-patients-attending-the-nephrology-clinic-of-lagos-university-teaching-hospital-in-sub-saharan-west-africa
#15
Olumuyiwa John Fasipe, Peter Ehizokhale Akhideno, Obiyo Nwaiwu, Alex Adedotun Adelosoye
Introduction: Life expectancy has increased significantly among chronic kidney disease (CKD) patients due to the extensive use of polypharmacy practice for medication prescriptions. This predisposes them to potential drug-drug interactions (DDIs), which can lead to an increase in morbidity, mortality, length of hospital stay, and health care cost. Methods: This was a 30-month retrospective study that reviewed the medical case records of consenting adult CKD patients from January 2014 to June 2016...
2017: Clinical Pharmacology: Advances and Applications
https://www.readbyqxmd.com/read/29123086/assessing-the-impact-of-imperfect-adherence-to-artemether-lumefantrine-on-malaria-treatment-outcomes-using-within-host-modelling
#16
Joseph D Challenger, Katia Bruxvoort, Azra C Ghani, Lucy C Okell
Artemether-lumefantrine (AL) is the most widely-recommended treatment for uncomplicated Plasmodium falciparum malaria worldwide. Its safety and efficacy have been extensively demonstrated in clinical trials; however, its performance in routine health care settings, where adherence to drug treatment is unsupervised and therefore may be suboptimal, is less well characterised. Here we develop a within-host modelling framework for estimating the effects of sub-optimal adherence to AL treatment on clinical outcomes in malaria patients...
November 9, 2017: Nature Communications
https://www.readbyqxmd.com/read/29119617/computer-aided-design-of-human-sialyltransferase-inhibitors-of-hst8sia-iii
#17
Christopher Dobie, Andrew P Montgomery, Rémi Szabo, Danielle Skropeta, Haibo Yu
Sialyltransferase (ST) upregulation and the resultant hypersialylation of tumour cell surfaces is an established hallmark of many cancers including lung, breast, ovarian, pancreatic and prostate cancer. The role of ST enzymes in tumour cell growth and metastasis, as well as links to multi-drug resistance, has seen ST inhibition emerge as a target for potential antimetastatic cancer treatments. The most potent of these reported inhibitors are transition-state analogues. Although there are several examples of these in the literature, many have suspected poor pharmacokinetic properties and are not readily synthetically accessible...
November 9, 2017: Journal of Molecular Recognition: JMR
https://www.readbyqxmd.com/read/29105853/measuring-the-impact-of-medicines-regulatory-interventions-systematic-review-and-methodological-considerations
#18
Thomas Goedecke, Daniel Morales, Alexandra Pacurariu, Xavier Kurz
AIM: Evaluating the public health impact of regulatory interventions is important but there is currently no common methodological approach to guide this evaluation. This systematic review provides a descriptive overview of the analytical methods for impact research. METHODS: We searched MEDLINE and EMBASE for articles with an empirical analysis evaluating the impact of European Union or non-European Union regulatory actions to safeguard public health published until March 2017...
November 5, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29104757/effect-of-nalfurafine-hydrochloride-in-patients-with-chronic-liver-disease-with-refractory-pruritus-on-sleep-disorders-a-study-protocol-for-single-arm-prospective-interventional-study
#19
Kazunori Yoh, Hiroki Nishikawa, Hirayuki Enomoto, Yoshinori Iwata, Akio Ishii, Yukihisa Yuri, Noriko Ishii, Yuho Miyamoto, Kunihiro Hasegawa, Chikage Nakano, Ryo Takata, Takashi Nishimura, Nobuhiro Aizawa, Yoshiyuki Sakai, Naoto Ikeda, Tomoyuki Takashima, Hiroko Iijima, Shuhei Nishiguchi
Introduction: Chronic liver disease (CLD)-related pruritus manifests as cholestasis symptoms, which can cause severe itches in the whole body and significantly decrease quality of daily activities and sleep. The actigram, which documents movement by means of an accelerometer, has been demonstrated to be useful for assessing sleep quality. Nalfurafine hydrochloride, which is a selective κ-opioid receptor agonist, exerts its antipruritic efficacies through a novel mechanism. We aimed to prospectively examine the effect of nalfurafine hydrochloride on sleep quality for patients with CLD with pruritus utilising actigram...
2017: BMJ Open Gastroenterology
https://www.readbyqxmd.com/read/29101139/public-views-towards-community-health-and-hospital-based-outpatient-services-and-their-utilisation-in-zhejiang-china-a-mixed-methods-study
#20
Dan Wu, Tai Pong Lam, Kwok Fai Lam, Xu Dong Zhou, Kai Sing Sun
OBJECTIVE: China is engaged in promoting community health services (CHS) nationwide. This study examines the public's views towards CHS and their utilisation of community-based and hospital-based outpatient services. DESIGN: A mixed methods study using qualitative interviews and a cross-sectional survey. STUDY SETTING AND PARTICIPANTS: The study was conducted among the public between September 2014 and September 2015 in Zhejiang province, China...
November 3, 2017: BMJ Open
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