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Hitoshi Ono, Yasunari Kojima, Hiroshi Harada, Yoshikazu Abe, Takuro Endo, Mamoru Kobayashi
1. The pharmacokinetic and metabolite profiles of mizagliflozin, a novel selective sodium glucose co-transporter 1 inhibitor designed to act only in the intestine, were investigated in rats. 2. Mizagliflozin administrated intravenously (0.3 mg/kg) and orally (3 mg/kg) declined with a short half-life (0.23 and 1.14 h, respectively). The absolute bioavailability was only 0.02%. Following intravenous administration of [14 C]mizagliflozin (0.3 mg/kg), radioactivity in plasma was also rapidly declined. Up to 24 h after oral administration of [14 C]mizagliflozin (1 mg/kg), radioactivity was recovered in the faeces (98...
March 20, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Baixue Yang, Chen Wei, Yang Yang, Qifang Wang, Sanming Li
OBJECTIVE: To evaluate parameters about wettability, water absorption or swelling of excipients in forms of powders or dosage through various methods systematically and explore its correlation with tablet disintegration. MATERIALS AND METHODS: The water penetration and swelling of powders with different proportions of excipients including microcrystalline cellulose (MCC), mannitol, low-substituted hydroxypropyl cellulose (L-HPC), crospolyvinylpyrrolidone (PVPP), carboxymethyl starch sodium (CMS-Na), croscarmellose sodium (CCMC-Na) and magnesium stearate (MgSt) were determined by Washburn capillary rise...
March 20, 2018: Drug Development and Industrial Pharmacy
M Angeles Tejero Hernández, Elena García Martínez, M José Arroyo Marin, Elena Gómez Guzmán
The cardiorenal syndrome has been defined as a situation in which therapy to relieve congestive symptoms of heart failure is limited by a decreased renal function. The resistance to conventional diuretic treatment makes difficult managing these patients. Tolvaptan, a selective vasopressin-2 receptor antagonist, has been used successfully in adults with this pathology but the experience with children is very limited. A five-year-old girl with renal failure waiting for a heart transplant is presented. Tolvaptan (0...
April 1, 2018: Archivos Argentinos de Pediatría
Kengran Yang, V Ongun Özçelik, Nishant Garg, Kai Gong, Claire E White
Conventional drying of colloidal materials and gels (including cement) can lead to detrimental effects due to the buildup of internal stresses as water evaporates from the nano/microscopic pores. However, for these gel materials the underlying nanoscopic alterations that are, in part, responsible for macroscopically-measured strain values (especially at low relative humidity) remain a topic of open debate in the literature. In this study, sodium-based calcium-alumino-silicate-hydrate (C-(N)-A-S-H) gel, the major binding phase of silicate-activated blast furnace slag (one type of low-CO2 cement), is investigated from a drying perspective, since it is known to suffer extensively from drying-induced microcracking...
March 20, 2018: Physical Chemistry Chemical Physics: PCCP
Tomotaka Ando, Yoshitaka Okuhara, Yoshiyuki Orihara, Koichi Nishimura, Kyoko Yamamoto, Tohru Masuyama, Shinichi Hirotani
Recently, we and other group have reported that furosemide administration along with hypertonic saline solution enhanced diuretic efficiency of furosemide. However, little is known about factors which associated with high diuretic efficiency by hypertonic saline solution with furosemide therapy. To identify predictors of diuretic efficiency in the hypertonic saline solution with furosemide therapy, we recruited 30 consecutive hospitalized heart failure (HF) patients with volume overload (77 ± 10 years, systolic blood pressure > 90 mmHg, and estimated glomerular filtration rate > 15 ml/min/1...
March 19, 2018: Heart and Vessels
Yuan Cheng, Haiying Song, Xiaoqing Pan, Hong Xue, Yifei Wan, Tao Wang, Zhongmin Tian, Entai Hou, Ian R Lanza, Pengyuan Liu, Yong Liu, Purushottam W Laud, Kristie Usa, Yongcheng He, Mingyu Liang
Dietary salt intake has significant effects on arterial blood pressure and the development of hypertension. Mechanisms underlying salt-dependent changes in blood pressure remain poorly understood, and it is difficult to assess blood pressure salt-sensitivity clinically. Methods: We examined urinary levels of metabolites in 103 participants of the Dietary Approaches to Stop Hypertension (DASH)-Sodium trial after nearly 30 days on a defined diet containing high sodium (targeting 150 mmol sodium intake per day) or low sodium (50 mmol per day)...
2018: Theranostics
Tetsuya Suzuki, Kyomu Matsumoto, Masamitsu Honma, Takehiko Nohmi
In regulatory genetic toxicology, it is an axiom that there is no threshold for genotoxicity of chemicals, such that genotoxic chemicals may impose carcinogenic risk on humans even at very low doses. This paradigm is counterintuitive, however, because humans possess a number of self-defense mechanisms that may suppress the genotoxicity at these low doses and therefore manifest a practical threshold. DNA polymerase zeta (Pol ζ) is a specialized Pol that plays an important role in DNA synthesis across DNA damage, thereby modulating cell survival and genotoxicity...
April 2018: Mutation Research
Payal Malhotra, Sandeep Jain, Gauri Kapoor
BACKGROUND: Cerebral sinovenous thrombosis (CSVT) is a rare, yet important complication of acute lymphoblastic leukemia (ALL) therapy, associated with significant morbidity and mortality. Paucity of data from India prompted us to report our experience with CSVT over a period of 17 years. MATERIALS AND METHODS: This is a retrospective analysis of 500 consecutive ALL patients, below 18 year of age, treated between January 1998 and December 2014, who developed symptomatic CVST...
March 16, 2018: Journal of Pediatric Hematology/oncology
Lebogang P Mokotedi, Frederic S Michel, Angela J Woodiwiss, Gavin R Norton, Aletta Me Millen
Sodium (Na)-intake increases vascular reactivity. Whether low potassium (K)-intake affects vascular reactivity associated blood pressure (BP) changes is uncertain. This study aimed to determine whether Na-induced increases in BP and vascular reactivity are altered by low K-intake. Male Sprague-Dawley rats were assigned to three dietary groups for six weeks: a standard Na-K diet (Control, n=12), a high Na-normal K diet (HS-NormK, n=12) and a high Na-low K diet (HS-LowK, n=12). BP was measured at baseline and after the dietary intervention...
March 12, 2018: Journal of Cardiovascular Pharmacology
Le Kang, Mingsan Miao, Ming Bai, Shuo Tian
Objective: To study the protective effect of total flavonoid in rabdosia rubescens on BIT model by brain ischemic tolerance (hereinafter BIT) model of mice. Method: BIT model is used to block bilateral common carotid arteries and to copy BIT model of mice. After 10 min of transient ischemia for rats in preconditioning group, the mice in the nimodipine group and naoluotong capsule group were given the total flavonoid in rabdosia rubescens (300 mg/kg, 150 mg/kg, 75 mg/kg) for gavage, sham operation group, ischemia/reperfusion injury (hereinafter IRI) group and BIT group were fed with the same volume of 0...
December 2017: Saudi Journal of Biological Sciences
Geeta Kumari Wasupalli, Devendra Verma
We report here the self-assembled structures of polyelectrolyte complexes (PECs) of polyanionic sodium alginate with the polycationic chitosan at room temperature. The PECs prepared at different pH values exhibited two distinct morphologies. The chitosan-alginate PECs self-assembled into the fibrous structure in a low pH range of pH 3 to 7. The PECs obtained at high pH series around pH 8 and above resulted in the formation of colloidal nanoparticles in the range of 120 ± 9.48 nm to 46.02 ± 16...
March 15, 2018: International Journal of Biological Macromolecules
M I Maiorino, G Bellastella, D Giugliano, K Esposito
Metabolic diseases are associated with chronic low-grade inflammation, which has been indicated as a potential mediator of endothelial dysfunction and cardiovascular disease. Visceral adiposity is thought to be the starting condition of the inflammatory state through the release of inflammatory cytokines, including TNF-alpha, CRP, and IL-6, which in turn promote endothelial dysfunction, endothelial expression of chemokines (IL-1) and adhesion molecules (ICAM-1, VCAM-1, and P-selectin), and the inhibition of anti-atherogenic factors (adiponectin)...
March 16, 2018: Journal of Endocrinological Investigation
Leah J Mische, Ellen M Mowry
PURPOSE OF REVIEW: This review aims to critically evaluate published studies examining diets and nutritional supplements (excepting vitamin D) for the impact on prevention and prognosis of multiple sclerosis (MS). RECENT FINDINGS: There is a negative relationship between the Mediterranean diet and vascular disease, and vascular co-morbidities are associated with a worse MS prognosis. Low-fat, fish-based diets, sodium-restricted diets, calorie restriction, the paleo diet, and gluten-free diets have been examined, mostly in observational studies; results are inconclusive...
March 17, 2018: Current Treatment Options in Neurology
Nahid Rafie, Sahar Golpour Hamedani, Noushin Mohammadifard, Awat Feizi, Sayyed Morteza Safavi
PURPOSE: There are epidemiologic studies indicating a positive correlation between high sodium and low potassium intake and body mass index. Therefore, this study was conducted in a cross-sectional sample of Iranian children and adolescents to evaluate the link between 24-h urinary Na:K ratio and risk of obesity. METHODS: In this cross-sectional study, 374 participants aged 11-18 years were included. One 24-h urine sample was collected by each participant to estimate Na:K ratio...
March 16, 2018: European Journal of Nutrition
Theresa Stolle, Freya Grondinger, Andreas Dunkel, Thomas Hofmann
Recently, studies on human salt taste sensitivity demonstrated that sodium chloride (NaCl) sensitive and non-sensitive subjects differed in their salivary proteome and, in particular, in endopeptidase activity. In order to investigate individual's NaCl sensitivity and the role of endoprotease activity in salt taste perception, 20 panellists were classified according to NaCl sensitivity and saliva samples collected. A targeted protein quantitation by means of selected-reaction-monitoring (SRM) mass spectrometry and stable-isotope incorporation revealed the joint abundance of lysozyme C and lipocalin-1 to be indicative for non-sensitive subjects...
July 15, 2018: Food Chemistry
Melissa Palmer, Lee Jennings, Debra G Silberg, Caleb Bliss, Patrick Martin
BACKGROUND: Accumulation of toxic free cholesterol in hepatocytes may cause hepatic inflammation and fibrosis. Volixibat inhibits bile acid reuptake via the apical sodium bile acid transporter located on the luminal surface of the ileum. The resulting increase in bile acid synthesis from cholesterol could be beneficial in patients with non-alcoholic steatohepatitis. This adaptive dose-finding study investigated the safety, tolerability, pharmacodynamics, and pharmacokinetics of volixibat...
March 16, 2018: BMC Pharmacology & Toxicology
Frederik Flenner, Nicole Arlt, Mahtab Nasib, Sophie Schobesberger, Thea Koch, Ursula Ravens, Felix Friedrich, Viacheslav Nikolaev, Torsten Christ, Sebastian N Stehr
BACKGROUND: Systemic toxicity of local anesthetics is predominantly complicated by their myocardial toxicity. Especially long-acting local anesthetics exert a negative inotropic effect that has been described at lower concentrations than defined for blockade of myocardial ion channels. We evaluated the negative inotropic effect of bupivacaine at a concentration described for clinical toxicity testing the hypothesis that negative inotropy is a result of reduced Ca sensitivity rather than blockade of ion channels...
March 16, 2018: Anesthesiology
Min-Seob Seo, Sumin Jang, Hyunwoo Kim
A chiral aluminum solvating agent (CASA) was demonstrated to be a general and efficient reagent for 1H NMR chiral analysis of alcohols. The sodium salt of the CASA (CASA-Na) showed a complete baseline peak separation of the hydroxyl group for various chiral alcohols including primary, secondary, and tertiary alcohols with alkyl and aryl substituents in CD3CN. Due to the weak intermolecular interaction, 1H NMR measurement at low temperature (-40 to 10 °C) was required.
March 16, 2018: Chemical Communications: Chem Comm
Firas Sbeih, Florian Christov, Michael B Gluth
OBJECTIVE: To describe the course of Meniere's disease with noninvasive treatment during the first few years after initial diagnosis. METHODS: A retrospective review of consecutive patients with newly diagnosed definite Meniere's disease between 2013 and 2016 and a minimum follow-up of 1 year. Patients received a written plan for low sodium, water therapy, and treatment with a diuretic and/or betahistine. Subjects were screened and treated for vestibular migraine as needed...
March 1, 2018: Annals of Otology, Rhinology, and Laryngology
Zhen-Yue Wu, Chao Ma, Yu-Lin Bai, Yu-Si Liu, Shi-Feng Wang, Xiao Wei, Kai-Xue Wang, Jie-Sheng Chen
The development of sustainable and low cost electrode materials for sodium-ion batteries has attracted considerable attention. In this work, a carbon composite material decorated with in situ generated ZnS nanoparticles has been prepared via a simple pyrolysis of the rubber powder from dumped tires. Upon being used as an anode material for sodium-ion batteries, the carbon composite shows a high reversible capacity and rate capability. A capacity as high as 267 mA h g-1 is still retained after 100 cycles at a current density of 50 mA g-1...
March 16, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
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