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Rosuvastatin

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https://www.readbyqxmd.com/read/29042279/long-circulating-pegylated-chitosan-nanoparticles-of-rosuvastatin-calcium-development-and-in-vitro-and-in-vivo-evaluations
#1
Mukund Hirpara, Jyothsna Manikkath, K Sivakumar, Renuka S Managuli, Karthik Gourishetti, Nandakumar Krishnadas, Rekha R Shenoy, Jayaprakash Belle, Chamallamudi Mallikarjuna Rao, Srinivas Mutalik
The aim of this study was to improve the pharmacokinetics and pharmacodynamics profile of rosuvastatin calcium by formulating long-circulating PEGylated chitosan nanoparticles (NPs). Chitosan was PEGylated by a carbodiimide mediated reaction, using a carboxylic acid derivative of PEG (polyethylene glycol). The NPs were optimised for particle size, polydispersity index, zeta potential and drug entrapment efficiency. In vitro drug release, pharmacokinetic and pharmacodynamics studies of the optimized nanoparticles were performed...
October 14, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29040850/biosynthesis-of-tert-butyl-3r-5s-6-chloro-3-5-dihydroxyhexanoate-by-carbonyl-reductase-from-rhodosporidium-toruloides-in-mono-and-biphasic-media
#2
Zhi-Qiang Liu, Lin Wu, Ling Zheng, Wen-Zhong Wang, Xiao-Jian Zhang, Li-Qun Jin, Yu-Guo Zheng
tert-Butyl (3R,5S)-6-chloro-3,5-dihydroxyhexanoate ((3R,5S)-CDHH) is the key intermediate for synthesis of atorvastatin and rosuvastatin. Carbonyl reductase exhibits excellent activity toward tert-butyl (S)-6-chloro-5-hydroxy-3-oxohexanoate ((S)-CHOH) to synthesize (3R,5S)-CDHH. In this study, a whole cell biosynthesis reaction system to produce (3R,5S)-CDHH was constructed in organic solvents. A solution of 10% (v/v) Tween-80 was introduced to the reaction system as a co-solvent, which greatly enhanced biotransformation process, giving 98...
October 5, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/29020356/a-common-missense-variant-of-lilrb5-is-associated-with-statin-intolerance-and-myalgia
#3
Moneeza K Siddiqui, Cyrielle Maroteau, Abirami Veluchamy, Aleksi Tornio, Roger Tavendale, Fiona Carr, Ngu-Uma Abelega, Dan Carr, Katyrzyna Bloch, Par Hallberg, Qun-Ying Yue, Ewan R Pearson, Helen M Colhoun, Andrew D Morris, Eleanor Dow, Jacob George, Munir Pirmohamed, Paul M Ridker, Alex S F Doney, Ana Alfirevic, Mia Wadelius, Anke-Hilse Maitland-van der Zee, Daniel I Chasman, Colin N A Palmer
Aims: A genetic variant in LILRB5 (leukocyte immunoglobulin-like receptor subfamily-B) (rs12975366: T > C: Asp247Gly) has been reported to be associated with lower creatine phosphokinase (CK) and lactate dehydrogenase (LDH) levels. Both biomarkers are released from injured muscle tissue, making this variant a potential candidate for susceptibility to muscle-related symptoms. We examined the association of this variant with statin intolerance ascertained from electronic medical records in the GoDARTS study...
August 29, 2017: European Heart Journal
https://www.readbyqxmd.com/read/29020193/generalizing-randomized-clinical-trial-results-implementation-and-challenges-related-to-missing-data-in-the-target-population
#4
Jin-Liern Hong, Michele Jonsson Funk, Robert LoCasale, Sara E Dempster, Stephen R Cole, Michael Webster-Clark, Jessie K Edwards, Til Stürmer
Statins are indicated in patients with elevated high-sensitivity C-reactive protein and normal low-density lipoprotein cholesterol based on the multi-country JUPITER trial (2003-2008) results, but the benefit in real-world populations remains unknown. We sought to generalize JUPITER results to trial-eligible population using the UK Clinical Practice Research Datalink (CPRD) 2001-2014. We multiply imputed missing baseline characteristics for the CPRD population and selected the trial-eligible CPRD population as target population based on observed and imputed values...
August 10, 2017: American Journal of Epidemiology
https://www.readbyqxmd.com/read/29019117/physiologically-based-pharmacokinetic-modeling-of-transporter-mediated-hepatic-clearance-and-liver-partitioning-of-oatp-and-oct-substrates-in-cynomolgus-monkeys
#5
Bridget L Morse, Jamus G MacGuire, Anthony M Marino, Yue Zhao, Maxine Fox, Yueping Zhang, Hong Shen, W Griffith Humphreys, Punit Marathe, Yurong Lai
In the present investigations, we evaluate in vitro hepatocyte uptake and partitioning for the prediction of in vivo clearance and liver partitioning. Monkeys were intravenously co-dosed with rosuvastatin and bosentan, substrates of the organic anion transporting polypeptides (OATPs), and metformin, a substrate of organic cation transporter 1 (OCT1). Serial plasma and liver samples were collected over time. Liver and plasma unbound fraction was determined using equilibrium dialysis. In vivo unbound partitioning (Kpu,u) for rosuvastatin, bosentan, and metformin, calculated from total concentrations in the liver and plasma, were 243, 553, and 15, respectively...
October 10, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28994701/study-of-statin-and-loratadine-induced-muscle-pain-mechanisms-using-human-skeletal-muscle-cells
#6
Yat Hei Leung, Jacques Turgeon, Veronique Michaud
Many drugs can cause unexpected muscle disorders, often necessitating the cessation of an effective medication. Inhibition of monocarboxylate transporters (MCTs) may potentially lead to perturbation of l-lactic acid homeostasis and muscular toxicity. Previous studies have shown that statins and loratadine have the potential to inhibit l-lactic acid efflux by MCTs (MCT1 and 4). The main objective of this study was to confirm the inhibitory potentials of atorvastatin, simvastatin (acid and lactone forms), rosuvastatin, and loratadine on l-lactic acid transport using primary human skeletal muscle cells (SkMC)...
October 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28992467/effect-of-statin-on-arginine-metabolites-in-treated-hiv-infection
#7
Sahera Dirajlal-Fargo, Vanessa El Kamari, Abdus Sattar, Khurshid Alam, Nicholas Funderburg, Danielle Labbato, Lisa Pirro, Chris T Longenecker, Wai Hong Wilson, Grace A McComsey
BACKGROUND AND AIMS: Asymmetric dimethylarginine (ADMA) is an inhibitor of nitric oxide and an independent risk factor for cardiovascular disease. We examined the effect of statin on ADMA in HIV + patients on stable ART, and whether such an effect contributes to the favorable changes on carotid intima media thickness. METHODS: This is a secondary analysis of SATURN-HIV, in which HIV + adults on stable ART with HIV-1 RNA< 1000 copies/mL and LDL-cholesterol <130 mg/dL were randomized to 10 mg daily rosuvastatin or placebo...
September 28, 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28988251/efficacy-and-safety-of-a-generic-rosuvastatin-in-a-real-world-setting-prospective-observational-clinical-study-in-lebanese-patients
#8
Mohamad Betto, Jocelyne Fares, Nada Saliba, Hajar Ballout
BACKGROUND: No published studies have assessed the efficacy and safety of rosuvastatin generics. OBJECTIVES: Primary objective to assess the safety and efficacy of a generic rosuvastatin in reducing plasma low-density-lipoprotein cholesterol (LDL-C) in Lebanese dyslipidemic patients. Changes in high-density lipoprotein cholesterol, triglycerides and adverse effects were secondary objectives. DESIGN: Prospective, observational, non-comparative...
September 2017: Annals of Saudi Medicine
https://www.readbyqxmd.com/read/28980533/rosuvastatin-administered-intraperitoneally-reduces-the-formation-of-postoperative-adhesions-in-rats
#9
Stefan Chiorescu, Nicolae Ovidiu Grad, Ion Aurel Mironiuc, Octavian Aurel Andercou
OBJECTIVES: The purpose of the present experimental research was to assess the efficacy of intraperitoneal administration of rosuvastatin in preventing the formation of postoperative peritoneal adhesions. MATERIAL AND METHOD: Peritoneal adhesions were induced in 120 male rats of the Wistar-Bratislava breed, divided into 4 groups (n=30), using a parietal and visceral abrasion model. Group I was designated as the control group; in the case of group II, a saline solution was administered intraperitoneally, while in the case of groups III and IV, rosuvastatin solution with a concentration of 10 mg/kg and 5 mg/kg, respectively, was administered in a single dose, during laparotomy...
September 26, 2017: Annali Italiani di Chirurgia
https://www.readbyqxmd.com/read/28974102/the-effect-of-rosuvastatin-on-vascular-disease-differs-by-smoking-status-in-treated-hiv-infection
#10
Corrilynn Olesky Hileman, Grace A McComsey
BACKGROUND: Smoking is an important contributor to cardiovascular disease (CVD) risk and is highly prevalent in the HIV population. In SATURN-HIV, a 96-week, randomized placebo-controlled trial testing the effect of rosuvastatin on subclinical vascular disease and immune activation in HIV-infected adults, rosuvastatin improved immune activation and arrested common carotid artery intima media thickness (CCA IMT) progression. METHODS: In this exploratory analysis, ANOVA was used to test for effect modification by smoking...
October 3, 2017: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/28965256/effects-of-rosuvastatin-and-atorvastatin-on-nonsustained-ventricular-tachycardia-in-patients-with-st-elevation-myocardial-infarction-a-retrospective-analysis
#11
Xianqing Hu, Jian Cheng, Chunjian Li
BACKGROUND/AIMS: Early and intensive atorvastatin treatment can decrease nonsustained ventricular tachycardia (nsVT) in patients with ST-segment elevation myocardial infarction (STEMI). The objective of this study was to compare the effects of hydrophilic rosuvastatin and lipophilic atorvastatin on nsVT in STEMI patients treated with primary percutaneous coronary intervention (PCI). METHODS: The data from a cohort of patients undergoing primary PCI at Jinhua Municipal Central Hospital from January 1, 2013 through June 30, 2016 were analyzed...
September 30, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28962887/a-population-based-cohort-study-on-the-drug-specific-effect-of-statins-on-sepsis-outcome
#12
Chien-Chang Lee, Meng-Tse Gabriel Lee, Tzu-Chun Hsu, Lorenzo Porta, Shy-Shin Chang, Chia-Hung Yo, Kuang-Chau Tsai, Matthew Lee
BACKGROUND: Whether statin treatment, proved by recent experimental studies to have an antimicrobial activity, exerts a drug- or a class-specific effect in sepsis remains unknown. METHODS: Short-term mortality in patients with sepsis was analyzed using data from the National Health Insurance Research Database. Use of statins was defined as the cumulative use of a specific statin (atorvastatin, simvastatin, or rosuvastatin) for > 30 days prior to the index sepsis admission...
September 27, 2017: Chest
https://www.readbyqxmd.com/read/28960806/regional-evidence-and-international-recommendations-to-guide-lipid-management-in-asian-patients-with-type-2-diabetes-with-special-reference-to-renal-dysfunction
#13
REVIEW
Titus Wl Lau, Kevin Ek Tan, Jason Cj Choo, T G Ng, Tavintharan S, Juliana C N Chan
The anticipated increase in the prevalence and incidence of type 2 diabetes in Asia, and its associated cardiovascular-renal complications will place a significant burden on patients, caregivers and society. Despite the proven effectiveness of lipid management in reducing these complications, there are major treatment gaps especially in Asian patients with young-onset diabetes and chronic kidney disease. Recent international guidelines recommended the adoption of absolute risk estimation of atherosclerosis and cardiovascular disease to guide treatment intensity...
September 28, 2017: Journal of Diabetes
https://www.readbyqxmd.com/read/28947528/stability-of-extemporaneously-prepared-rosuvastatin-oral-suspension
#14
Abdel Naser Zaid, Rania Shtayah, Ayman Qadumi, Mashour Ghanem, Rawan Qedan, Marah Daibes, Somud Abu Awwad, Nidal Jaradat, Naim Kittana
PURPOSE: The stability of an extemporaneously prepared rosuvastatin suspension stored over 30 days under various storage conditions was evaluated. METHODS: Rosuvastatin suspension was extemporaneously prepared using commercial rosuvastatin tablets as the source of active pharmaceutical ingredient. The organoleptic properties, dissolution profile, and stability of the formulation were investigated. For the stability studies, samples of the suspension were stored under 2 storage conditions, room temperature (25 °C and 60% relative humidity) and accelerated stability chambers (40 °C and 75% relative humidity)...
October 1, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28943594/effect-of-rosuvastatin-on-cholesterol-efflux-capacity-and-endothelial-function-in-type-2-diabetes-mellitus-and-dyslipidemia
#15
Kyong Yeun Jung, Kyoung Min Kim, Sun Kyoung Han, Han Mi Yun, Tae Jung Oh, Sung Hee Choi, Kyong Soo Park, Hak Chul Jang, Soo Lim
BACKGROUND: Quality and quantity of high-density lipoprotein cholesterol (HDL-C) may be associated with cardiovascular risk. We investigated the effect of rosuvastatin on cholesterol efflux (CE) for HDL function and vascular health.Methods and Results:We enrolled 30 dyslipidemic patients with type 2 diabetes mellitus and 20 healthy subjects as controls. Vascular health was assessed on flow-medicated dilation (FMD), nitroglycerin-induced dilatation of the brachial artery and carotid artery intima-media thickness (cIMT)...
September 22, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28940950/rosuvastatin-pretreatment-suppresses-distant-organ-injury-following-unilateral-renal-ischemia-reperfusion-in-hypertensive-dahl-salt-sensitive-rats
#16
Makoto Kanno, Masaaki Nakayama, Wan-Jun Zhu, Yoshimitsu Hayashi, Junichiro James Kazama
AIM: Ischemia-reperfusion (I/R) induces distant organ injury (DOI) via inflammation and oxidative stress. Statins have anti-inflammatory and anti-oxidant effects independent of their cholesterol-lowering properties. To clarify whether statins could suppress DOI, we investigated the effect of rosuvastatin (RO) on the contralateral kidney following unilateral renal I/R. METHODS: Dahl salt-sensitive rats (6-week-old) were randomly divided into four groups: sham, sham with RO, I/R, and I/R with RO...
September 22, 2017: Nephrology
https://www.readbyqxmd.com/read/28931488/carboxylate-cross-linked-cyclodextrin-a-nanoporous-scaffold-for-enhancement-of-rosuvastatin-oral-bioavailability
#17
Mai Mahmoud Gabr, Sana Mohamed Mortada, Marwa Ahmed Sallam
Cyclodextrins play an important role in supramolecular chemistry acting as building blocks than can be cross-linked by various linker molecules forming nano-porous structures called nanosponges (NS). NS have the ability to enhance the stability, solubility and bioavailability of various actives. This work aimed at elaborating rosuvastatin (ROS) loaded NS to improve its oral bioavailability. Carboxylate-linked NS were synthesized by reacting β-CD with pyromellitic dianhydride (PDA) at different molar ratios under specific conditions...
September 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28925467/effects-of-rosuvastatin-on-pentraxin-3-level-and-platelet-aggregation-rate-in-elderly-patients-with-acute-myocardial-infarction-undergoing-elective-interventional-therapy-a-double-blind-controlled-study
#18
Y-H Li, L-H Wang, Q Li, D-W Yu, Y-S Gai, S-X Cai, F Tian, H-Y Zhou
OBJECTIVE: To investigate clinical effects of rosuvastatin on blood lipid levels, hemorheological profiles, vascular endothelial function, pentraxin 3 (PTX-3) level, the number of granule membrane glycoprotein (GMP-140) molecules and platelet aggregation rate in elderly patients with acute myocardial infarction (AMI) undergoing elective percutaneous coronary intervention (PCI). PATIENTS AND METHODS: Total of 120 elderly patients admitted with AMI undergoing elective PCI from July 2014 to January 2016 were selected...
August 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28920182/neovascularization-and-synaptic-function-regulation-with-memantine-and-rosuvastatin-in-a-rat-model-of-chronic-cerebral-hypoperfusion
#19
Nan Zhang, Chenchen Song, Baomin Zhao, Mengya Xing, Lanlan Luo, Marc L Gordon, Yan Cheng
Cerebral hypoperfusion is an important factor in the pathogenesis of cerebrovascular diseases and neurodegenerative disorders. We investigated the effects of memantine and rosuvastatin on both neovascularization and synaptic function in a rat model of chronic cerebral hypoperfusion, which was established by the bilateral common carotid occlusion (2VO) method. We tested learning and memory ability, synaptic function, circulating endothelial progenitor cell (EPC) number, expression of neurotrophic factors, and markers of neovasculogenesis and cell proliferation after memantine and/or rosuvastatin treatment...
September 17, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28919738/surface-modification-of-endovascular-stents-with-rosuvastatin-and-heparin-loaded-biodegradable-nanofibers-by-electrospinning
#20
Milka Janjic, Foteini Pappa, Varvara Karagkiozaki, Christakis Gitas, Kiriakos Ktenidis, Stergios Logothetidis
This study describes the development of drug-loaded nanofibrous scaffolds as a nanocoating for endovascular stents for the local and sustained delivery of rosuvastatin (Ros) and heparin (Hep) to injured artery walls after endovascular procedures via the electrospinning process. PURPOSE: The proposed hybrid covered stents can promote re-endothelialization; improve endothelial function; reduce inflammatory reaction; inhibit neointimal hyperplasia of the injured artery wall, due to well-known pleiotropic actions of Ros; and prevent adverse events such as in-stent restenosis (ISR) and stent thrombosis (ST), through the antithrombotic action of Hep...
2017: International Journal of Nanomedicine
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