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Pulmonary pharmacokinetics

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https://www.readbyqxmd.com/read/28431781/clenbuterol-hydrochloride
#1
Abdulrahman A Al-Majed, Nasr Y Khalil, Ibraheem Khbrani, Hatem A Abdel-Aziz
Clenbuterol (Broncodil and trade) is a direct-acting sympathomimetic agent with mainly beta-adrenergic activity and a selective action on β2 receptors (a β2 agonist). It has properties similar to those of salbutamol. It is used as a bronchodilator in the management of reversible airways obstruction, as in asthma and in certain patients with chronic obstructive pulmonary disease. The uses, applications, and the synthetic pathways of this drug are outlined. Physical characteristics including: ionization constant, solubility, X-ray powder diffraction pattern, thermal methods of analysis, UV spectrum, IR spectrum, mass spectrum are all produced...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28416418/current-progress-toward-a-better-understanding-of-drug-disposition-within-the-lungs-summary-proceedings-of-the-1-st-workshop-on-drug-transporters-in-the-lungs
#2
REVIEW
Carsten Ehrhardt, Per Bäckman, William Couet, Chris Edwards, Ben Forbes, Markus Fridén, Mark Gumbleton, Ken-Ichi Hosoya, Yukio Kato, Takeo Nakanishi, Mikihisa Takano, Tetsuya Terasaki, Ryoko Yumoto
The School of Pharmacy and Pharmaceutical Sciences at Trinity College Dublin hosted the 1(st)Workshop on Drug Transporters in the Lungs in September 2016 to discuss the impact of transporters on pulmonary drug disposition and their roles as drug targets in lung disease. The workshop brought together about 30 scientists from academia and pharmaceutical industry from Europe and Japan and addressed the primary questions: What do we know today, and what do we need to know tomorrow about transporters in the lung? The three themes of the workshop were: (1) techniques to study drug transporter expression and actions in the lungs; (2) drug transporter effects on pulmonary pharmacokinetics - case studies; and (3) transporters as drug targets in lung disease...
April 14, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28415455/heparin-modified-graphene-oxide-for-ph-sensitive-sustained-release-of-doxorubicin-hydrochloride
#3
Baomei Zhang, Xiaoye Yang, Yang Wang, Guangxi Zhai
A novel nanocarrier of heparin (Hep) modified graphene oxide (GO) was fabricated via a linker (adipic dihydrazide) and used as a pH-sensitive drug delivery system for controlling the release of anticancer drug doxorubicin (DOX) for anti-tumor therapy. The finally obtained nanocarrier was GO-ADH-Hep with better stability, blood compatibility and biocompatibility confirmed by the hemolytic test and in vitro cytotoxicity study. Its safety issue was greatly improved via Hep modification. The amount of DOX loaded onto GO-ADH-Hep was significantly high and dependent on pH value...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28415011/design-and-synthesis-of-novel-xanthine-derivatives-as-potent-and-selective-a2b-adenosine-receptor-antagonists-for-the-treatment-of-chronic-inflammatory-airway-diseases
#4
Sujay Basu, Dinesh A Barawkar, Vidya Ramdas, Meena Patel, Yogesh Waman, Anil Panmand, Santosh Kumar, Sachin Thorat, Minakshi Naykodi, Arnab Goswami, B Srinivasa Reddy, Vandna Prasad, Sandhya Chaturvedi, Azfar Quraishi, Suraj Menon, Shalini Paliwal, Abhay Kulkarni, Vikas Karande, Indraneel Ghosh, Syed Mustafa, Siddhartha De, Vaibhav Jain, Ena Ray Banerjee, Sreekanth R Rouduri, Venkata P Palle, Anita Chugh, Kasim A Mookhtiar
Adenosine induces bronchial hyperresponsiveness and inflammation in asthmatics through activation of A2B adenosine receptor (A2BAdoR). Selective antagonists have been shown to attenuate airway reactivity and improve inflammatory conditions in pre-clinical studies. Hence, the identification of novel, potent and selective A2BAdoR antagonist may be beneficial for the potential treatment of asthma and Chronic Obstructive Pulmonary Disease (COPD). Towards this effort, we explored several prop-2-ynylated C8-aryl or heteroaryl substitutions on xanthine chemotype and found that 1-prop-2-ynyl-1H-pyrazol-4-yl moiety was better tolerated at the C8 position...
April 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28414242/discovery-of-2-2-ethyl-6-4-2-3-hydroxyazetidin-1-yl-2-oxo-ethyl-piperazin-1-yl-8-methyl-imidazo-1-2-a-pyridin-3-yl-methyl-amino-4-4-fluorophenyl-thiazole-5-carbonitrile-glpg1690-a-first-in-class-autotaxin-inhibitor-undergoing-clinical-evaluation-for-the-treatment
#5
Nicolas Desroy, Christopher Housseman, Xavier Bock, Agnès Joncour, Natacha Bienvenu, Laëtitia Cherel, Virginie Labeguere, Emilie Rondet, Christophe Peixoto, Jean-Marie Joël Grassot, Olivier Picolet, Denis Annoot, Nicolas Triballeau, Alain Monjardet, Emanuelle Wakselman, Veronique Roncoroni, Sandrine Le Tallec, Roland Blanque, Celine Cottereaux, Nele Vandervoort, Thierry Christophe, Patrick Mollat, Marieke B A C Lamers, Marielle Auberval, Boska Hrvacic, Jovica Ralic, Line Oste, Ellen Van der Aar, Reginald Brys, Bertrand Heckmann
Autotaxin is a circulating enzyme with a major role in the production of lysophosphatic acid (LPA) species in blood. A role for the autotaxin/LPA axis has been suggested in many disease areas including pulmonary fibrosis. Structural modifications of the known autotaxin inhibitor lead compound 1, to attenuate hERG inhibition, remove CYP3A4 time-dependent inhibition and improve pharmacokinetic properties, led to the identification of clinical candidate GLPG1690 (11). Compound 11 was able to cause a sustained reduction of LPA levels in plasma in vivo and was shown to be efficacious in a bleomycin-induced pulmonary fibrosis model in mice, and in reducing extra-cellular matrix deposition in the lung whilst also reducing LPA 18:2 content in bronchoalveolar lavage fluid...
April 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28394614/a-synthetic-macromolecular-antibiotic-platform-for-inhalable-therapy-against-aerosolized-intracellular-alveolar-infections
#6
Debobrato Das, Jasmin Chen, Selvi Srinivasan, Abby Michelle Kelly, Brian Lee, Hye-Nam Son, Frank Radella, Timothy E West, Daniel M Ratner, Anthony J Convertine, Shawn J Skerrett, Patrick S Stayton
Lung-based intracellular bacterial infections remain one of the most challenging infectious disease settings. For example, the current standard for treating Franciscella tularensis pneumonia (tularemia) relies on prolonged administration of oral and intravenous antibiotics that poorly achieve and sustain pulmonary drug bioavailability. Inhalable antibiotic formulations are approved and in clinical development for upper respiratory infections, but sustained drug dosing from inhaled antibiotics against alveolar intracellular infections remains a current unmet need...
April 10, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28389258/role-of-dual-bronchodilators-in-copd-a-review-of-the-current-evidence-for-indacaterol-glycopyrronium
#7
REVIEW
Joachim H Ficker, Klaus F Rabe, Tobias Welte
In this review, we summarize the rationale for combining long-acting bronchodilators in the management of chronic obstructive pulmonary disease (COPD), and the evidence for the long-acting bronchodilator combination indacaterol/glycopyrronium (IND/GLY). Clinical practice guidelines generally recommend the use of long-acting bronchodilators in the treatment of patients with all severities of COPD, either as a first-choice or alternative-choice therapy. Combining classes of long-acting bronchodilators can result in superior improvements in lung function and clinical outcomes compared with bronchodilator monotherapy, as observed in studies of free combinations of long-acting β2-agonists (LABAs) and long-acting muscarinic antagonists (LAMAs)...
April 4, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28385615/identification-and-characterisation-of-a-salt-form-of-danirixin-with-reduced-pharmacokinetic-variability-in-patient-populations
#8
Jackie C Bloomer, Claire Ambery, Bruce E Miller, Paul Connolly, Helen Garden, Nick Henley, Neil Hodnett, Sarah Keel, James L Kreindler, Richard S Lloyd, Wayne Matthews, John Yonchuk, Aili L Lazaar
The natural variability of gastric pH or gastric acid reducing medications can result in lower and more variable clinical pharmacokinetics for basic compounds in patient populations. Progressing alternative salt forms with improved solubility and dissolution properties can minimise this concern. This manuscript outlines a nonclinical approach comprising multiple biopharmaceutical, in vitro and physiologically based pharmacokinetic model (PBPK) modelling studies to enable selection of an alternative salt form for danirixin (DNX, GSK1325756), a pharmaceutical agent being developed for chronic obstructive pulmonary disease (COPD)...
April 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28378883/pharmacokinetics-of-macitentan-in-patients-with-pulmonary-arterial-hypertension-and-comparison-with-healthy-subjects
#9
Milena Issac, Jasper Dingemanse, Patricia N Sidharta
Macitentan is a worldwide approved dual endothelin receptor antagonist that has demonstrated efficacy in the treatment of pulmonary arterial hypertension (PAH) in a phase 3 clinical trial, SERAPHIN, at a dose of 10 mg once daily. During this trial, trough plasma concentrations (Ctrough ) of macitentan and its active metabolite,  ACT-132577,  were obtained at steady state in 242 patients, indicating that mean Ctrough of both analytes was about 2-fold higher in PAH patients than in healthy subjects. To further investigate the pharmacokinetics (PK) of macitentan and its active metabolite, ACT-132577,  a 24-hour PK profile was recorded at steady state in 20 PAH patients in the open-label extension of SERAPHIN...
April 5, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28374512/pharmacokinetic-analysis-of-inhaled-salmeterol-in-asthma-patients-evidence-from-two-dry-powder-inhalers
#10
Konstantina Soulele, Panos Macheras, Vangelis Karalis
Salmeterol (SAL) is a long-acting β2-adrenergic agonist, which is widely used in the asthma therapy. The aim of this study was to investigate the pharmacokinetics (PK) of inhaled SAL in asthma patients using two different dry powder inhalers. This analysis was based on data from 45 subjects who participated in a two-sequence, four period crossover bioequivalence (BE) study after single administration of the test (T) and reference (R) products. In order to mimic more closely the real treatment conditions, activated charcoal was not co-administered...
April 3, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28369685/isorhapontigenin-a-bioavailable-dietary-polyphenol-suppresses-airway-epithelial-cell-inflammation-through-a-corticosteroid-independent-mechanism
#11
Samuel Chao Ming Yeo, Peter S Fenwick, Peter J Barnes, Hai Shu Lin, Louise E Donnelly
BACKGROUND AND PURPOSE: Chronic obstructive pulmonary disease (COPD) is a corticosteroid-resistant airway inflammatory condition. Resveratrol has exhibited anti-inflammatory activities in COPD but has weak potency and poor pharmacokinetics. This study aims to evaluate the potential of isorhapontigenin, another dietary polyphenol, as a novel anti-inflammatory agent for COPD by examining its effects in vitro and its pharmacokinetics in vivo. EXPERIMENTAL APPROACH: Primary human airway epithelial cells derived from healthy and COPD subjects and A549 epithelial cells were incubated with isorhapontigenin or resveratrol and stimulated with IL-1β in the presence or absence of cigarette smoke extract...
March 30, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28346048/mabdelivery-administration-routes-for-antibody-therapy-third-labex-mabimprove-industrial-workshop-july-2-2015-tours-france
#12
Elsa Bodier-Montagutelli, Renaud Respaud, Hervé Watier, Audrey Guillon-Munos
The annual "LabEx MAbImprove Industrial Workshops" are primarily intended to provide a comprehensive view about topics of interest for the pharmaceutical industry to scientists involved in research on therapeutic antibodies. The third workshop in this series, held July 2, 2015 in Tours, was dedicated to the optimization of delivery, namely all processes leading monoclonal antibodies to reach their target site. The commonly used intravenous (IV) route, although advantageous in terms of pharmacokinetics and pharmacodynamics, presents some disadvantages in terms of patients' convenience, therapeutic target access or treatment cost...
February 28, 2017: MAbs
https://www.readbyqxmd.com/read/28322599/dissolvit-an-in-vitro-method-for-simulating-the-dissolution-and-absorption-of-inhaled-dry-powder-drugs-in-the-lungs
#13
Per Gerde, Maria Malmlöf, Lina Havsborn, Carl-Olof Sjöberg, Pär Ewing, Stefan Eirefelt, Katarina Ekelund
The main purpose of this work was to develop an in vitro method for simulating the dissolution and absorption of inhaled dry powder drugs that also mimics systemic pharmacokinetic data. A second purpose was to evaluate this method. DissolvIt(®) was developed as a simulation of the air-blood barrier of the upper airways, constituting: "airborne" particles deposited on a glass cover slip, a mucus simulant, a polycarbonate (basal) membrane, and a pumped albumin buffer simulating the pulmonary blood flow. The PreciseInhale(®) exposure system was used to aerosolize and deposit test formulations onto cover slips...
February 2017: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/28317153/pharmacokinetics-and-pulmonary-distribution-of-gamithromycin-after-intravenous-administration-in-foals
#14
S Berlin, T Randow, E Scheuch, M Grube, M Venner, W Siegmund
The long-acting azalide antibiotic gamithromycin is marketed for intramuscular treatment of bovine and swine infections. Off-label use in foals leads to severe local lesions likely caused by hyperosmolality of the injected solution. We provide evidence from a pharmacokinetic study in 10 warm-blooded healthy foals for intravenous bolus injection of gamithromycin diluted in distilled water to be a safe and well tolerated alternative. By intravenous dosing, markedly higher plasma exposure and better penetration into bronchoalveolar lavage cells but lower distribution into epithelial lining fluid are achieved as after intramuscular or subcutaneous administration...
March 19, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28314480/airways-antiallergic-effect-and-pharmacokinetics-of-alkaloids-from-alstonia-scholaris
#15
Yun-Li Zhao, Jing Cao, Jian-Hua Shang, Ya-Ping Liu, Afsar Khan, Heng-Shan Wang, Yi Qian, Lu Liu, Min Ye, Xiao-Dong Luo
BACKGROUND: Alstonia scholaris (L.) R. Br. (Apocynaceae), an important herbal medicine, has been widely used to treat respiratory tract diseases, such as cough, asthma, phlegm, and chronic obstructive pulmonary disease. PURPOSE: To evaluate pharmacological effect of alkaloids from A. scholaris on ovalbumin induced airways allergic inflammatory model, and explore whether the dosing frequency is related to pharmacokinetics. STUDY DESIGN: After oral administration of total alkaloids, the pharmacokinetic study of it was investigated...
April 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28302764/-18-f-gp1-a-novel-fluorine-18-labeled-tracer-designed-for-pet-imaging-of-thrombi-with-high-detection-sensitivity-and-low-background
#16
Jessica Lohrke, Holger Siebeneicher, Markus Berger, Michael Reinhardt, Mathias Berndt, Andre Mueller, Marion Zerna, Norman Koglin, Felix Oden, Marcus Bauser, Matthias Friebe, Ludger M Dinkelborg, Joachim Huetter, Andrew W Stephens
Thromboembolic diseases such as myocardial infarction, stroke, transient ischemic attacks and pulmonary embolism are major causes of morbidity and mortality worldwide. GPIIb/IIIa is the key receptor involved in platelet aggregation and is a validated target for therapeutic approaches and diagnostic imaging. The aim of this study was to develop and characterize a specific small molecule tracer for positron emission tomography (PET) imaging that binds with high affinity to GPIIb/IIIa receptors and has suitable pharmacokinetic properties to overcome limitations of previous approaches...
March 16, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28281196/pharmacokinetics-of-the-inhaled-selective-glucocorticoid-receptor-modulator-azd5423-following-inhalation-using-different-devices
#17
Johanna Melin, Susanne Prothon, Charlotte Kloft, Adriaan Cleton, Carl Amilon, Carin Jorup, Per Bäckman, Bo Olsson, Ulrika Wählby Hamrén
AZD5423 is a non-steroidal glucocorticoid receptor modulator, with low aqueous solubility, developed for treatment of asthma and COPD. In this work, we aim to evaluate and compare the absorption pharmacokinetics (PK) of AZD5423 after inhalation via four devices, (Spira®, I-neb®, Turbuhaler® and a new dry powder inhaler (new DPI)) with two formulations using differently sized primary particles, and to compare the pulmonary bioavailability with the predicted lung deposited dose. Plasma concentration-time data after intravenous, oral and inhaled administration via four devices were available from two clinical studies in healthy and asthmatic subjects...
March 9, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28267480/the-safety-and-efficacy-of-full-versus-reduced-dose-betrixaban-in-the-acute-medically-ill-vte-venous-thromboembolism-prevention-with-extended-duration-betrixaban-apex-trial
#18
C Michael Gibson, Rim Halaby, Serge Korjian, Yazan Daaboul, Douglas F Arbetter, Megan K Yee, Samuel Z Goldhaber, Russel Hull, Adrian F Hernandez, Shiao-Ping Lu, Olga Bandman, Janet M Leeds, Alex Gold, Robert A Harrington, Alexander T Cohen
BACKGROUND: The APEX trial assessed the safety and efficacy of extended-duration thromboprophylaxis using betrixaban versus standard dosing of enoxaparin among hospitalized, acutely ill medical patients. The 80-mg betrixaban dose was halved to 40 mg among subjects with severe renal insufficiency and those receiving a concomitant strong P-glycoprotein inhibitor. METHODS: This analysis assessed the pharmacokinetics, efficacy, and safety of full- (80 mg) and reduced-dose (40 mg) betrixaban relative to enoxaparin in the APEX trial...
March 2017: American Heart Journal
https://www.readbyqxmd.com/read/28264853/pharmacokinetics-and-pharmacodynamics-of-minocycline-against-acinetobacter-baumannii-in-a-neutropenic-murine-pneumonia-model
#19
Jian Zhou, Kimberly R Ledesma, Kai-Tai Chang, Henrietta Abodakpi, Song Gao, Vincent H Tam
Multi-drug resistant (MDR) Acinetobacter baumannii is increasingly more prevalent in nosocomial infections. Although in vitro susceptibility of A. baumannii to minocycline is promising, the in vivo efficacy of minocycline has not been well established. In this study, the in vivo activity of minocycline was evaluated in a neutropenic murine pneumonia model. Specifically, we investigated the relationship between minocycline exposure and bactericidal activity using 5 A. baumannii isolates with a broad range of susceptibility (MIC ranged from 0...
March 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28263078/pharmacokinetics-metabolism-and-partial-biodistribution-of-pincer-therapeutic-nitazoxanide-in-mice-following-pulmonary-delivery-of-inhalable-particles
#20
Anuradha Gupta, Sachin L Tulsankar, Rabi S Bhatta, Amit Misra
Nitazoxanide (NTZ) induces autophagy in mammalian cells and also has mycobactericidal activity, displaying a two-pronged therapeutic effect, on the host as well as the pathogen. The pharmacokinetics and biodistribution of inhaled NTZ were investigated. Particles containing NTZ in a matrix of PLGA were prepared by spray drying. HPLC and LC-MS/MS methods were developed and validated. Particles were administered as inhalations to mice. Drug concentrations in plasma and tissues were estimated at different time points...
April 3, 2017: Molecular Pharmaceutics
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