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Pulmonary pharmacokinetics

Feng Feng, Fulin Qiang, Aijun Shen, Donghui Shi, Aiyan Fu, Haiming Li, Mingzhu Zhang, Ganlin Xia, Peng Cao
Objective: To prospectively compare the discriminative capacity of dynamic contrast enhanced-magnetic resonance imaging (DCE-MRI) with that of18 F-fluorodeoxyglucose (18 F-FDG) positron emission tomography/computed tomography (PET/CT) in the differentiation of malignant and benign solitary pulmonary nodules (SPNs). Methods: Forty-nine patients with SPNs were included in this prospective study. Thirty-two of the patients had malignant SPNs, while the other 17 had benign SPNs...
February 2018: Chinese Journal of Cancer Research, Chung-kuo Yen Cheng Yen Chiu
Patrick Darken, Paolo DePetrillo, Colin Reisner, Earl St Rose, Paul Dorinsky
The budesonide/glycopyrronium/formoterol fumarate dihydrate metered dose inhaler (BGF MDI) is an inhaled corticosteroid/long-acting muscarinic antagonist/long-acting β2 -agonist fixed-dose combination formulated with innovative co-suspension delivery technology that is in clinical development for the treatment of chronic obstructive pulmonary disease (COPD). This randomized, Phase I, single-dose, six-treatment, four-period, crossover study (NCT01980615) examined the pharmacokinetic (PK) and safety profile of three doses of BGF MDI (320/14...
March 12, 2018: Pulmonary Pharmacology & Therapeutics
Glenn A Jacobson, Sharanne Raidal, Kate Robson, Christian K Narkowicz, David S Nichols, E Haydn Walters
BACKGROUND: Salmeterol (a long acting beta2-agonist) is a chiral molecule. (RR)-salmeterol is responsible for pharmacological effect, but basic knowledge of enantioselective pulmonary pharmacodynamics and pharmacokinetics of salmeterol remains unknown. There are safety concerns with (S)-enantiomers of beta2-agonists, with suggestions that these enantiomers may increase bronchial hyperresponsivneness in asthma patients. METHODOLOGY: Horses (n = 12) received racemic (rac-) salmeterol 250 μg via inhalation...
February 23, 2018: Journal of Pharmaceutical and Biomedical Analysis
Xiaobo Wang, Yinan Wang, Ronggang Xi, Yuanyuan Wang, Xiaobo Yang
The optimization of process parameters of spray-dried powder containing fanhuncaoin, a newly discovered antiinflammatorily active phenolic acid isolated from Chinese herb, was conducted using response surface methodology (RSM). The experimental results were fitted into partial cubic polynomial model to describe and predict the response quality in terms of the final angle of repose, aerodynamic diameter, respirable fraction (RF) and yield. The recommended optimum spray-drying parameters for development of fanhuncaoin powder with optimum quality were 110 °C inlet temperature, 0...
March 15, 2018: Drug Development and Industrial Pharmacy
Ziyu Zhao, Zhengwei Huang, Xuejuan Zhang, Ying Huang, Yingtong Cui, Cheng Ma, Guanlin Wang, Tim Freeman, Xiang-Yun Lu, Xin Pan, Chuanbin Wu
BACKGROUND: The hygroscopicity of raffinose carrier for dry powder inhaler (DPI) was the main obstacle for its further application. Hygroscopicity-induced agglomeration would cause deterioration of aerosolization performance of raffinose, undermining the delivery efficiency. METHODS: Cyclodextrin-raffinose binary carriers (CRBCs) were produced by spray-drying so as to surmount the above issue. Physicochemical attributes and formation mechanism of CRBCs were explored in detail...
March 13, 2018: Expert Opinion on Drug Delivery
Charlotte H Maden, David Fairman, Michelle Chalker, Maria J Costa, William A Fahy, Nadia Garman, Pauline T Lukey, Tim Mant, Simon Parry, Juliet K Simpson, Robert J Slack, Stuart Kendrick, Richard P Marshall
PURPOSE: Inhaled drug delivery is an attractive route by which to deliver drugs to lungs of patients with idiopathic pulmonary fibrosis (IPF). GSK3008348 is a potent and selective small molecule being developed as the first inhaled inhibitor of the αvβ6 integrin for the treatment of IPF. The phase 1 first-time-in-human clinical trial (NCT02612051) presented here was designed to investigate the safety, tolerability and pharmacokinetic (PK) profile of single doses of GSK3008348 in healthy participants...
March 12, 2018: European Journal of Clinical Pharmacology
Paul Gavra, André Y Denault, Yves Théoret, Louis P Perrault, France Varin
OBJECTIVES: Milrinone pulmonary administration is used currently for the treatment of pulmonary hypertension. Several methods are available: simple jet nebulization, vibrating mesh nebulization, intratracheal instillation, and intratracheal atomization. The aim of this study was to explore the concentration-effect relationship of milrinone for each of these methods. DESIGN: Observational open-label pharmacokinetic/pharmacodynamics cohort study. SETTING: Single-center, hospital animal laboratory...
January 31, 2018: Journal of Cardiothoracic and Vascular Anesthesia
Christine Sekaggya-Wiltshire, Mohammed Lamorde, Agnes N Kiragga, Kelly E Dooley, Moses R Kamya, Andrew Kambugu, Jan Fehr, Yukari C Manabe, Barbara Castelnuovo
Tuberculosis (TB) is a major public health problem. Many countries still fall below the minimum World Health Organization (WHO) TB treatment target success rate. There is conflicting evidence about whether concentrations of anti-tuberculosis drugs given at standard doses have an effect on treatment outcomes. The current data correlating anti-TB drug concentrations and treatment outcome is limited. This article summarized the existing literature and their utility in evaluating the association between each anti-TB drug's concentrations using current target concentrations and treatment outcomes in patients with pulmonary tuberculosis receiving standard WHO-recommended dosing...
January 2018: Tuberculosis
Cristina Lazzarini, Krupanandan Haranahalli, Robert Rieger, Hari Krishna Ananthula, Pankaj B Desai, Alan Ashbaugh, Michael J Linke, Melanie T Cushion, Bela Ruzsicska, John Haley, Iwao Ojima, Maurizio Del Poeta
The incidence of invasive fungal infections has risen dramatically in the past decades. Current antifungal drugs are either toxic, likely to interact with other drugs, have a narrow spectrum of activity or induce fungal resistance. Hence, there is a great need for new antifungals, possibly with novel mechanisms of action. Previously our group reported an acylhydrazone called BHBM that targeted the sphingolipid pathway, and showed strong antifungal activity against several fungi. In this study, we screened 19 derivatives of BHBM...
March 5, 2018: Antimicrobial Agents and Chemotherapy
Andreas Krause, Jochen Zisowsky, Jasper Dingemanse
BACKGROUND: Macitentan is the first endothelin receptor antagonist with demonstrated efficacy on morbidity and mortality in pulmonary arterial hypertension (PAH) in the pivotal study SERAPHIN. METHODS: The pharmacokinetics (PK) of macitentan and its active metabolite, ACT-132577, were characterized in a population model. Efficacy and hemodynamics (pharmacodynamics, PD) were related to PK based on PK/PD modeling. RESULTS: Sex, age, and body weight influenced the PK to a statistically significant extent...
February 28, 2018: Pulmonary Pharmacology & Therapeutics
Daniela Matei, Sharad Ghamande, Lynda D Roman, Angeles Alvarez Secord, John Nemunaitis, Merry Jennifer Markham, Kenneth P Nephew, Simone Jueliger, Aram Oganesian, Sue Naim, Xiang-Yao Su, Harold N Keer, Mohammad Azab, Gini Fleming
PURPOSE: Epigenetic changes are implicated in acquired resistance to platinum. Guadecitabine is a next-generation hypomethylating agent (HMA). Here we report the clinical results, along with pharmacokinetic (PK) and pharmacodynamic analyses of the phase 1 study of guadecitabine and carboplatin (G+C) in patients with recurrent, platinum resistant high-grade serous ovarian cancer (OC), primary peritoneal carcinoma (PPC), or fallopian tube cancer (FTC). EXPERIMENTAL DESIGN: Guadecitabine was administered once daily on Days 1-5 followed by carboplatin IV on Day 8 of a 28-day cycle...
March 2, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Merja Kirjavainen, Leena Mattila, Mikko Vahteristo, Jani Korhonen, Satu Lähelmä
BACKGROUND: Easyhaler® dry powder inhaler (DPI) containing salmeterol and fluticasone propionate was developed for the treatment of asthma and chronic obstructive pulmonary disease. Three different Salmeterol/fluticasone Easyhaler test products (Orion Pharma, Finland) were compared against the reference product Seretide® Diskus® DPI (GlaxoSmithKline, United Kingdom) to study whether any of the test products are bioequivalent with the reference. METHODS: Open and randomized pharmacokinetic four-period crossover study on 65 healthy volunteers was performed in a single center to compare the lung deposition and total systemic exposure of salmeterol and fluticasone propionate after administration of single doses (two inhalations of 50/500 μg/inhalation strength) in fasting conditions...
March 1, 2018: Journal of Aerosol Medicine and Pulmonary Drug Delivery
Ling Zhang, Fen Chen, Jiatong Zheng, Hongwei Wang, Xingjun Qin, Weisan Pan
Pingyangmycin (PYM) has been applied clinically for many years to treat vascular malformations (VM) in China. The major limitation of PYM injections is quick diffusion from the injection site, which increases side effects, especially the possibility of pulmonary injury. In this paper, chitosan/glycerophosphate disodium (CS/GP) thermogels containing liposomes for sustained and localized PYM delivery were prepared and optimized by a three-level three-factorial Box-Behnken experimental design to evaluate the effects of different variables (the PYM concentration, CS amount and GP content), on the selected responses (cumulative percentage PYM released in 1 day, 9 days and the rate constant k)...
November 2018: Drug Delivery
Robert Palmér, Jukka Mäenpää, Alexandra Jauhiainen, Bengt Larsson, John Mo, Muir Russell, James Root, Susanne Prothon, Ligia Chialda, Pablo Forte, Torbjörn Egelrud, Kristina Stenvall, Philip Gardiner
Neutrophil serine proteases (NSPs), such as neutrophil elastase (NE), are activated by dipeptidyl peptidase 1 (DPP1) during neutrophil maturation. High NSP levels can be detrimental, particularly in lung tissue, and inhibition of NSPs is therefore an interesting therapeutic opportunity in multiple lung diseases, including chronic obstructive pulmonary disease (COPD) and bronchiectasis. We conducted a randomized, placebo-controlled, first-in-man study to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of the DPP1 inhibitor AZD7986 in healthy subjects...
February 27, 2018: Clinical Pharmacology and Therapeutics
Marc Weiner, Jon Gelfond, Teresa L Johnson-Pais, Melissa Engle, Charles A Peloquin, John L Johnson, Erin E Sizemore, William R Mac Kenzie
Moxifloxacin exhibits concentration-dependent prolongation of human QTc intervals and bactericidal activity against Mycobacterium tuberculosis However, moxifloxacin plasma concentrations are variable between patients. We evaluated whether human gene polymorphisms affect moxifloxacin plasma concentrations in tuberculosis patients from two geographic regions. We enrolled a convenience sample of 49 adults with drug-sensitive pulmonary tuberculosis from Africa and the United State s enrolled in two treatment trials of moxifloxacin as part of multidrug therapy...
February 20, 2018: Antimicrobial Agents and Chemotherapy
Michel R Corboz, Jimin Zhang, Daniel LaSala, Keith DiPetrillo, Zhili Li, Vladimir Malinin, Jeremy Brower, Philip J Kuehl, Ted E Barrett, Walter R Perkins, Richard W Chapman
Idiopathic pulmonary fibrosis is a progressive and lethal disease and while there are now two approved drugs (Esbriet® and Ofev®) additional effective treatments are still needed. Recently, prostacyclin analogs such as iloprost and treprostinil (TRE) have been shown to exert some protection against bleomycin-induced pulmonary fibrosis in mice when administered in a prophylactic regimen. In this study, we evaluated the effect of the inhaled treprostinil prodrug hexadecyl-treprostinil (C16TR) formulated in a lipid nanoparticle (INS1009) administered therapeutically in a fibrotic rat model...
February 1, 2018: Pulmonary Pharmacology & Therapeutics
T W Felton, K Ogungbenro, E Boselli, W W Hope, K A Rodvold
Background: Severe infections of the respiratory tracts of critically ill patients are common and associated with excess morbidity and mortality. Piperacillin is commonly used to treat pulmonary infections in critically ill patients. Adequate antibiotic concentration in the epithelial lining fluid (ELF) of the lung is essential for successful treatment of pulmonary infection. Objectives: To compare piperacillin pharmacokinetics/pharmacodynamics in the serum and ELF of healthy volunteers and critically ill patients...
January 29, 2018: Journal of Antimicrobial Chemotherapy
Paramita Paul, Soma Sengupta, Biswajit Mukherjee, Tapan K Shaw, Raghuvir H Gaonkar, Mita Chatterjee Debnath
AIM: Chitosan-coated polylactic-co-glycolic acid nanoparticles of voriconazole (VChNP) were developed to increase residence time and provide sustained drug release locally to treat recurrent lung-fungal infection. MATERIALS & METHODS: VChNP has been developed using a simple, unique technique and characterized. Pharmacokinetics, lung deposition with time and gamma imaging were conducted with optimized formulations. RESULTS: The deposition of fluorescein isothiocyanate-labeled VChNP in lung was confirmed by confocal microscopy...
January 31, 2018: Nanomedicine
A Watteyn, S Croubels, S De Baere, P De Backer, M Devreese
Florfenicol (FF) is registered for treatment of bovine and swine respiratory diseases. Although, turkeys often suffer from bacterial respiratory tract infections, there is no registered formulation based on FF for poultry available in Europe. The aim of this study was to evaluate the pharmacokinetic behavior of FF in turkeys in plasma, lung tissue, and pulmonary epithelial lining fluid (PELF).The concentration and pharmacokinetic characteristics of FF in plasma, lung tissue, and PELF in turkeys were determined, either after a single oral bolus (30 mg/kg body weight, BW) or during and after continuous drinking water medication (30 mg/kg BW/d for 5 d)...
January 25, 2018: Poultry Science
Heewon Seo, Eun Jin Kwon, Young-Ah You, Yoomi Park, Byung Joo Min, Kyunghun Yoo, Han-Sung Hwang, Ju Han Kim, Young Ju Kim
BACKGROUND: Ritodrine is a commonly used tocolytic to prevent preterm labour. However, it can cause unexpected serious adverse reactions, such as pulmonary oedema, pulmonary congestion, and tachycardia. It is unknown whether such adverse reactions are associated with pharmacogenomic variants in patients. METHODS: Whole-exome sequencing of 13 subjects with serious ritodrine-induced cardiac and pulmonary side-effects was performed to identify causal genes and variants...
January 24, 2018: BMC Medical Genomics
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