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https://www.readbyqxmd.com/read/29663288/in-vitro-in-vivo-predictive-dissolution-permeation-absorption-dynamics-of-highly-permeable-drug-extended-release-tablets-via-drug-dissolution-absorption-simulating-system-and-ph-alteration
#1
Zi-Qiang Li, Shuang Tian, Hui Gu, Zeng-Guang Wu, Makafui Nyagblordzro, Guo Feng, Xin He
Each of dissolution and permeation may be a rate-limiting factor in the absorption of oral drug delivery. But the current dissolution test rarely took into consideration of the permeation property. Drug dissolution/absorption simulating system (DDASS) valuably gave an insight into the combination of drug dissolution and permeation processes happening in human gastrointestinal tract. The simulated gastric/intestinal fluid of DDASS was improved in this study to realize the influence of dynamic pH change on the complete oral dosage form...
April 16, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29653073/a-zebrafish-heart-failure-model-for-assessing-therapeutic-agents
#2
Xiao-Yu Zhu, Si-Qi Wu, Sheng-Ya Guo, Hua Yang, Bo Xia, Ping Li, Chun-Qi Li
Heart failure is a leading cause of death and the development of effective and safe therapeutic agents for heart failure has been proven challenging. In this study, taking advantage of larval zebrafish, we developed a zebrafish heart failure model for drug screening and efficacy assessment. Zebrafish at 2 dpf (days postfertilization) were treated with verapamil at a concentration of 200 μM for 30 min, which were determined as optimum conditions for model development. Tested drugs were administered into zebrafish either by direct soaking or circulation microinjection...
March 20, 2018: Zebrafish
https://www.readbyqxmd.com/read/29651850/exploring-the-potential-of-a-global-emerging-contaminant-early-warning-network-through-the-use-of-retrospective-suspect-screening-with-high-resolution-mass-spectrometry
#3
Nikiforos A Alygizakis, Saer Samanipour, Juliane Hollender, María Ibáñez, Sarit Kaserzon, Varvara Kokkali, Jan A van Leerdam, Jochen F Mueller, Martijn Pijnappels, Malcolm J Reid, Emma L Schymanski, Jaroslav Slobodnik, Nikolaos S Thomaidis, Kevin V Thomas
A key challenge in the environmental and exposure sciences is to establish experimental evidence of the role of chemical exposure in human and environmental systems. High resolution and accurate tandem mass spectrometry (HRMS) is increasingly being used for the analysis of environmental samples. One lauded benefit of HRMS is the possibility to retrospectively process data for (previously omitted) compounds that has led to the archiving of HRMS data. Archived HRMS data affords the possibility of exploiting historical data to rapidly and effectively establish the temporal and spatial occurrence of newly identified contaminants through retrospective suspect screening...
April 13, 2018: Environmental Science & Technology
https://www.readbyqxmd.com/read/29618434/formulation-and-in-vitro-evaluation-of-directly-compressed-controlled-release-tablets-designed-from-the-co-precipitates
#4
Kamran Ahmad Khan, Gul Majid Khan, Syed Umer Jan, Asimur Rehman, Saifullah Mehsud
Controlled release dosage forms provide sustained therapeutics effects for prolonged period of time and improve patient compliance. In present study, controlled release co-precipitates of Metoprolol Tartrate and Losartan Potassium were prepared by solvent evaporation method using polymers such as Eudragit RL 100 and Carbopol 974PNF and controlled release tablets were directly compressed into tablets. In-vitro dissolution of controlled release co-precipitates were performed by USP Method-II (paddle method) and tablets were evaluated by USP Method-I (rotating basket method) in phosphate buffer (PH 6...
March 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29610608/pharmacotherapy-evaluation-and-utilization-in-coronary-artery-bypass-grafting-patients-in-kosovo-during-the-period-2016-2017
#5
Armond Daci, Adnan Bozalija, Raif Cavolli, Rame Alaj, Giangiacomo Beretta, Shaip Krasniqi
BACKGROUND: Coronary Artery Bypass Grafting (CABG) is realised in patients with critical or advanced disease of coronary arteries. There are different pharmacotherapeutic approaches which are used as management, treatment and preventive therapy in cardiovascular disease or related comorbidities. Performing a successful surgery, pharmacotherapy, and increase of bypass patency rate remains a serious challenge. AIM: This study aims to analyse the patient characteristics undergoing CABG and evaluation of their drug utilisation rate and daily dosages in the perioperative period...
March 15, 2018: Open Access Macedonian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29597876/ampk%C3%AE-2-deficiency-enhanced-susceptibility-to-ventricular-arrhythmias-in-mice-by-the-role-of-%C3%AE-adrenoceptor-signaling
#6
Hong Cao, Xin Wang, Shaozheng Ying, Congxin Huang
AMP-activated protein kinase-α2 is the main catalytic subunit of the heart, which is mainly located in cardiac myocytes. The effect of AMP-activated protein kinase-α2 on the cardiac electrophysiology is barely studied. From the previous study, it is possible that AMP-activated protein kinase-α2 may have some effect on the electrophysiology of the heart. To prove the hypothesis, we used the AMP-activated protein kinase-α2 knockout (AMPKα2-/- ) mice to estimate the electrophysiological characteristics of AMPKα2-/- mice and try to find the mechanism between them...
January 1, 2018: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/29582347/in-vitro-assessment-of-nasal-insufflation-of-comminuted-drug-products-designed-as-abuse-deterrent-using-the-vertical-diffusion-cell
#7
Heather Boyce, Dan Smith, Steve Byrn, Bhawana Saluja, Wen Qu, Vadim J Gurvich, Stephen W Hoag
In vitro evaluation of abuse deterrent formulations (ADFs) is a challenge since real abuse situations are variable and ADF technology is evolving. Specifically, an assessment of an ADF to deter nasal insufflation would be valuable. In this study, a vertical diffusion cell (VDC) was used to evaluate polyethylene oxide (PEO)-based tablets manipulated by three different forces. The commercially available products Oxycontin®, an ADF, Opana®, and metoprolol tartrate tablet formulations made in our laboratory were studied...
March 26, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29580170/comparison-of-therapeutic-triiodothyronine-versus-metoprolol-in-treatment-of-myocardial-infarction-in-rats
#8
Kuo Zhang, Yi-Da Tang, Youhua Zhang, Kaie Ojamaa, Ying Li, Amandeep Singh Saini, Maria Alicia Carrillo-Sepulveda, Viswanathan Rajagopalan, A Martin Gerdes
BACKGROUND: Beta blockers are standard therapy for myocardial infarction (MI). Preclinical studies have shown efficacy and safety of thyroid hormone (TH) treatment of cardiovascular disorders. Since THs interact with the sympathoadrenergic system, we aimed to compare triiodothyronine (T3) and metoprolol (Met) treatment of rats with MI on pathophysiology and TH-adrenergic signaling. METHODS: Female Sprague-Dawley rats aged 12 weeks underwent left anterior descending coronary artery ligation (MI) or sham surgeries...
March 26, 2018: Thyroid: Official Journal of the American Thyroid Association
https://www.readbyqxmd.com/read/29576700/combined-antihypertensive-effect-of-paeoniflorin-enriched-extract-and-metoprolol-in-spontaneously-hypertensive-rats
#9
Bo Li, Zheng-Biao Yang, Shan-Sha Lei, Jie Su, Ze-Wu Jin, Su-Hong Chen, Gui-Yuan Lv
Background: Hypertension is a great global health challenge and it mostly requires drug combination therapy with the various advantages. Metoprolol (MP) and paeoniflorin are both commonly used for the treatment of hypertension. However, whether they exert synergistic effects on antihypertension or not remains unclear, especially on vascular endothelial function. Objective: The purpose of the study is to investigate the advantages of the combined antihypertensive effects of paeoniflorin enriched extract from Radix Paeoniae Alba (RE) and MP in spontaneously hypertensive rats (SHR)...
January 2018: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29575226/discontinuation-and-dose-adjustment-of-metoprolol-after-metoprolol-paroxetine-fluoxetine-co-prescription-in-dutch-elderly
#10
Muh Akbar Bahar, Yuanyuan Wang, Jens H J Bos, Bob Wilffert, Eelko Hak
PURPOSE: Co-prescription of paroxetine/fluoxetine (a strong CYP2D6 inhibitor) in metoprolol (a CYP2D6 substrate) users is common, but data on the clinical consequences of this drug-drug interaction are limited and inconclusive. Therefore, we assessed the effect of paroxetine/fluoxetine initiation on the existing treatment with metoprolol on the discontinuation and dose adjustment of metoprolol among elderly. METHODS: We performed a cohort study using the University of Groningen IADB...
March 24, 2018: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29574456/modeling-short-qt-syndrome-using-human-induced-pluripotent-stem-cell-derived-cardiomyocytes
#11
Ibrahim El-Battrawy, Huan Lan, Lukas Cyganek, Zhihan Zhao, Xin Li, Fanis Buljubasic, Siegfried Lang, Gökhan Yücel, Katherine Sattler, Wolfram-Hubertus Zimmermann, Jochen Utikal, Thomas Wieland, Ursula Ravens, Martin Borggrefe, Xiao-Bo Zhou, Ibrahim Akin
BACKGROUND: Short QT syndrome (SQTS), a disorder associated with characteristic ECG QT-segment abbreviation, predisposes affected patients to sudden cardiac death. Despite some progress in assessing the organ-level pathophysiology and genetic changes of the disorder, the understanding of the human cellular phenotype and discovering of an optimal therapy has lagged because of a lack of appropriate human cellular models of the disorder. The objective of this study was to establish a cellular model of SQTS using human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs)...
March 24, 2018: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29574201/enhanced-pharmaceutical-removal-from-water-in-a-three-step-bio-ozone-bio-process
#12
Arnoud de Wilt, Koen van Gijn, Tom Verhoek, Amber Vergnes, Mirit Hoek, Huub Rijnaarts, Alette Langenhoff
Individual treatment processes like biological treatment or ozonation have their limitations for the removal of pharmaceuticals from secondary clarified effluents with high organic matter concentrations (i.e. 17 mg TOC/L). These limitations can be overcome by combining these two processes for a cost-effective pharmaceutical removal. A three-step biological-ozone-biological (BO3 B) treatment process was therefore designed for the enhanced pharmaceutical removal from wastewater effluent. The first biological step removed 38% of ozone scavenging TOC, thus proportionally reducing the absolute ozone input for the subsequent ozonation...
March 12, 2018: Water Research
https://www.readbyqxmd.com/read/29554753/effects-of-dissolved-organic-matter-and-nitrification-on-biodegradation-of-pharmaceuticals-in-aerobic-enrichment-cultures
#13
Yujie He, Alette A M Langenhoff, Rob N J Comans, Nora B Sutton, Huub H M Rijnaarts
Natural dissolved organic matter (DOM) and nitrification can play an important role in biodegradation of pharmaceutically active compounds (PhACs) in aerobic zones of constructed wetlands (CWs). This study used an enrichment culture originating from CW sediment to study the effect of DOM and nitrification on aerobic biodegradation of seven PhACs. The enriched culture degraded caffeine (CAF), metoprolol (MET), naproxen (NAP), and ibuprofen (IBP) with a consistent biodegradability order of CAF>MET>NAP>IBP...
March 2, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29552362/severe-hyperthyroidism-complicated-by-agranulocytosis-treated-with-therapeutic-plasma-exchange-case-report-and-review-of-the-literature
#14
Vishnu Garla, Karthik Kovvuru, Shradha Ahuja, Venkatataman Palabindala, Bharat Malhotra, Sohail Abdul Salim
Aim: To present a case of Graves' disease complicated by methimazole induced agranulocytosis treated with therapeutic plasma exchange (TPE) and review of the literature. Case Presentation: A 21-year-old patient with a history of Graves' disease presented to the endocrine clinic. His history was significant for heat intolerance, weight loss, and tremors. Upon examination he had tachycardia, smooth goiter, thyroid bruit, and hyperactive reflexes. He was started on methimazole and metoprolol and thyroidectomy was to be done once his thyroid function tests normalized...
2018: Case Reports in Endocrinology
https://www.readbyqxmd.com/read/29549925/the-association-of-adrb1-and-cyp2d6-polymorphisms-with-antihypertensive-effects-and-analysis-of-their-contribution-to-hypertension-risk
#15
Liping Chen, Ting Xiao, Liling Chen, Shanshan Xie, Maoqing Deng, Dingchang Wu
BACKGROUND: Genetic factors have a vital influence on the pathogenesis of hypertension. In this retrospective study, we aimed to evaluate the association of ADRB1 and CYP2D6 polymorphisms with antihypertensive effects and perform an analysis of their contribution to hypertension risk. METHODS: A total of 261 healthy individuals and 261 essential hypertension patients treated with metoprolol for 12 weeks were enrolled. ADRB1 and CYP2D6 genotypes were identified by xTAG liquid chip technology...
March 2018: American Journal of the Medical Sciences
https://www.readbyqxmd.com/read/29545006/risk-of-all-cause-mortality-in-diabetic-patients-taking-%C3%AE-blockers
#16
Tetsuro Tsujimoto, Hiroshi Kajio, Martin F Shapiro, Takehiro Sugiyama
OBJECTIVE: To assess the relationship between use of β-blockers and all-cause mortality in patients with and without diabetes. PATIENTS AND METHODS: Using data from the US National Health and Nutrition Examination Survey 1999-2010, we conducted a prospective cohort study. The study participants were followed-up from the survey participation date until December 31, 2011. We used a Cox proportional hazards model for all-cause mortality analysis. The multivariate-adjusted hazard ratios (HRs) of the participants taking β-blockers were compared with those of the participants not taking β-blockers...
March 9, 2018: Mayo Clinic Proceedings
https://www.readbyqxmd.com/read/29537909/effects-of-metoprolol-on-aquatic-invertebrates-in-artificial-indoor-streams
#17
Anna-Katharina Buchberger, Denise Brettschneider, Kristin Berg, Dirk Jungmann, Jörg Oehlmann, Marco Scheurer, Matthias Oetken
Aquatic organisms are impacted by various biotic and abiotic stressors such as current, inter- and intraspecific competition for food resources and habitat, neobiota as well as an increasing number of chemicals. The latter also include pharmaceuticals, which are increasingly being detected in surface waters due to their growing use. The aim of our study was to determine effect data for metoprolol as a model compound for beta-blockers under an environmentally realistic exposure scenario on aquatic invertebrates inhabiting lotic environments...
March 14, 2018: Journal of Environmental Science and Health. Part A, Toxic/hazardous Substances & Environmental Engineering
https://www.readbyqxmd.com/read/29524598/controlling-drug-release-from-mesoporous-silica-through-an-amorphous-nanoconfined-1-tetradecanol-layer
#18
Raul-Augustin Mitran, Cristian Matei, Daniela Berger, Laura Băjenaru, Mihaela G Moisescu
Mesoporous silica materials are promising nano-carriers for drug delivery systems. Even though there are many strategies for controlling the drug release kinetics, these must be adapted through trial and error on a case-by-case basis. Here we explore the possibility of tailoring the release kinetics of hydrophilic, water soluble therapeutic agents from mesoporous silica through addition of a hydrophobic excipient, 1-tetradecanol. In vitro drug release experiments performed at 37 °C, in phosphate buffer solution (pH 7...
March 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29524158/simultaneous-determination-of-14-oral-antihyperglycaemic-drugs-in-human-urine-by-liquid-chromatography-tandem-mass-spectrometry
#19
Quoc-Ky Truong, Xuan-Lan Mai, Jae-Yong Lee, Jongsook Rhee, Dinh Vinh, Jongki Hong, Kyeong Ho Kim
A simple, sensitive, and rapid assay based on hydrophilic interaction liquid chromatography (HILIC) with tandem mass spectrometry was developed and validated for the simultaneous determination of metformin and 13 other oral antihyperglycaemic drugs in human urine using metoprolol as an internal standard. A simple sample clean-up procedure using the "dilute and shoot" approach enabled fast and reliable analysis. Chromatographic separation was performed on a HILIC column using an elution gradient of mobile phase A, composed of 1 mM ammonium formate (pH 5), and mobile phase B, composed of acetonitrile, at a flow rate of 0...
March 9, 2018: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29523917/how-do-different-extracorporeal-circulation-systems-affect-metoprolol-bioavailability-in-coronary-artery-bypass-surgery-patients
#20
Hannu Kokki, Martin Maaroos, Sten Ellam, Jari Halonen, Ilkka Ojanperä, Merja Ranta, Veli-Pekka Ranta, Aleksandra Tolonen, Oscar Lindberg, Matias Viitala, Juha Hartikainen
PURPOSE: Cardiac surgery and conventional extracorporeal circulation (CECC) impair the bioavailability of drugs administered by mouth. It is not known whether miniaturized ECC (MECC) or off-pump surgery (OPCAB) affect the bioavailability in similar manner. We evaluated the metoprolol bioavailability in patients undergoing CABG surgery with CECC, MECC, or having OPCAB. METHODS: Thirty patients, ten in each group, aged 44-79 years, scheduled for CABG surgery were administered 50 mg metoprolol by mouth on the preoperative day at 8-10 a...
March 9, 2018: European Journal of Clinical Pharmacology
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