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Pulmonary pharmacokinetics

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https://www.readbyqxmd.com/read/28223260/enhanced-pulmonary-absorption-of-poorly-soluble-itraconazole-by-micronized-cocrystal-dry-powder-formulations
#1
Masatoshi Karashima, Noriyasu Sano, Syunsuke Yamamoto, Yuta Arai, Katsuhiko Yamamoto, Nobuyuki Amano, Yukihiro Ikeda
Micronized cocrystal powders and amorphous spray-dried formulations were prepared and evaluated in vivo and in vitro as pulmonary absorption enhancement formulations of poorly soluble itraconazole (ITZ). ITZ cocrystals with succinic acid (SA) or l-tartaric acid (TA) with a particle size diameter of < 2 µm were successfully micronized using the jet-milling system. The cocrystal crystalline morphologies observed using scanning electron microscopy (SEM) suggested particle shapes that differed from those of the crystalline or spray-dried amorphous ITZ...
February 18, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28219073/relationship-between-pulmonary-adverse-events-and-everolimus-exposure-in-japanese-and-non-japanese-patients-a-meta-analysis-of-oncology-trials
#2
Shinzaburo Noguchi, Nobuo Shinohara, Tetsuhide Ito, Atsushi Ohtsu, Alain Ravaud, Guy Jerusalem, Nobutsugu Ohno, Jorge Gallo, Emmanuel Bouillaud, Jenna Fan, Norio Nonomura
AIMS: This meta-analysis explores the relationship between the everolimus minimum (Cmin) and maximum (Cmax) exposure and the risk for pulmonary adverse events (AEs) in Japanese versus non-Japanese patients. METHODS: Patient-level data from patients treated with daily everolimus in advanced solid tumor trials were evaluated using a Cox regression model, stratified by cancer type or treatment arm, with log-transformed time-averaged Cmin or Cmax as a time-varying covariate...
February 21, 2017: Oncology
https://www.readbyqxmd.com/read/28213957/a-bosentan-pharmacokinetic-study-to-investigate-dosing-regimens-in-paediatric-patients-with-pulmonary-arterial-hypertension-future-3
#3
R M F Berger, M Gehin, M Beghetti, D Ivy, A Kusic-Pajic, P Cornelisse, S Grill, D Bonnet
AIM: To investigate whether increasing bosentan dosing frequency from 2 mg/kg twice daily (b.i.d.) to 2 mg/kg three times daily (t.i.d.) in children with pulmonary arterial hypertension (PAH) (from ≥3 months to <12 years of age) would increase exposure. METHODS: An open-label, prospective, randomised, multicentre, multiple-dose, Phase 3 study was conducted. Patients (n = 64) were randomised 1:1 to receive oral doses of bosentan of 2 mg/kg b.i...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28196344/identification-characterization-and-in-silico-admet-prediction-of-roflumilast-degradation-products
#4
Mariana S Pinheiro, Gil M Viana, Bárbara de A Abrahim Vieira, Alessandra Mendonça Teles de Souza, Carlos Rangel Rodrigues, Rita de Cássia E E Marins, Lúcio M Cabral, Valéria P de Sousa
The present study reports the degradation behavior of roflumilast (RFL), a new drug developed for the treatment of chronic obstructive pulmonary disease. The degradation of RFL was tested under various stress conditions as per the guidelines of the International Conference on Harmonization. The degradation products (DPs) of RFL were identified, characterized and in silico predictions were made of their pharmacokinetic properties, absorption, distribution, metabolism, excretion and toxicity (ADMET). RFL was subjected to various stress conditions including photodegradation, alkaline and acidic hydrolysis, oxidative and metallic degradation...
February 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28195061/overview-of-the-preclinical-pharmacological-properties-of-nigella-sativa-black-seeds-a-complementary-drug-with-historical-and-clinical-significance
#5
E Z Dajani, T G Shahwan, N E Dajani
Nigella sativa (N. sativa, black seeds; or sometimes known by many other names such as the blessed seed by the Arabs, black cumin in the Holy Bible, black caraway and Kalonji in South Asia) has been traditionally used for many years not only as a food but also as complementary drug. It is the objective of this communication to review the evidence-based pre-clinical pharmacological actions of N. sativa as a basis of its existing and potential new human clinical uses. Primary PubMed literature searches and secondary Medline searches were conducted to define N...
December 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28170282/pharmacokinetics-of-salbutamol-delivered-from-the-unit-dose-dry-powder-inhaler-comparison-with-the-metered-dose-inhaler-and-diskus-dry-powder-inhaler
#6
Alison Moore, Kylie Riddell, Shashidhar Joshi, Robert Chan, Rashmi Mehta
AIM: To compare the systemic exposure of salbutamol following delivery from the unit dose dry powder inhaler (UD-DPI) system with that from the Diskus(®) and metered dose inhaler (MDI). MATERIALS AND METHODS: This open-label, two-part, six-way crossover, randomized single-dose study in healthy subjects evaluated salbutamol systemic exposure of three dose strengths (using three inhalations: 3 × 150 μg [450 μg], 3 × 200 μg [600 μg], and 3 × 250 μg [750 μg]) and 2% of drug in lactose blends (1...
February 7, 2017: Journal of Aerosol Medicine and Pulmonary Drug Delivery
https://www.readbyqxmd.com/read/28167229/population-pharmacokinetics-model-of-thc-used-by-pulmonary-route-in-occasional-cannabis-smokers
#7
A Marsot, C Audebert, L Attolini, B Lacarelle, J Micallef, O Blin
Cannabis is the most widely used illegal drug in the world. Delta-9-tetrahydrocannabinol (THC) is the main source of the pharmacological effect. Some studies have been carried out and showed significant variability in the described models as the values of the estimated pharmacokinetic parameters. The objective of this study was to develop a population pharmacokinetic model for THC in occasional cannabis smokers. Twelve male volunteers (age: 20-28years, body weight: 62.5-91.0kg), tobacco (3-8 cigarette per day) and cannabis occasional smokers were recruited from the local community...
February 4, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28156176/respirable-controlled-release-polymeric-colloid-rcrpc-of-bosentan-for-the-management-of-pulmonary-hypertension-in-vitro-aerosolization-histological-examination-and-in-vivo-pulmonary-absorption
#8
COMPARATIVE STUDY
Lydia A Hanna, Emad B Basalious, Omaima N ELGazayerly
Bosentan is an endothelin receptor antagonist (ERA) prescribed for patients with pulmonary arterial hypertension (PAH). The oral delivery of bosentan possesses several drawbacks such as low bioavailability (about 50%), short duration of action, frequent administration, hepatotoxicity and systemic hypotension. The pulmonary administration would circumvent the pre-systemic metabolism thus improving the bioavailability and avoids the systemic adverse effects of oral bosentan. However, the short duration of action and the frequent administration are the major drawbacks of inhalation therapy...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28156170/passive-targeting-and-lung-tolerability-of-enoxaparin-microspheres-for-a-sustained-antithrombotic-activity-in-rats
#9
Shaimaa S Ibrahim, Rihab Osman, Nahed D Mortada, Ahmed-Shawky Geneidy, Gehanne A S Awad
Pulmonary bed can retain microparticles (MP) larger than their capillaries' diameter, hence we offer a promising way for lung passive targeting following intravenous (IV) administration. In this study, enoxaparin (Enox)-albumin microspheres (Enox-Alb MS) were, optimally, developed as lung targeted sustained release MP for IV use. Lung tolerability and targeting efficiency of Enox-Alb MS were tested, and the pharmacokinetic profile following IV administration to albino rats was constructed. In vivo studies confirmed high lung targeting efficiency of Enox-Alb MS with lack of potential tissue toxicity...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28124478/defining-the-optimal-dose-of-rifapentine-for-pulmonary-tuberculosis-exposure-response-relations-from-two-phase-2-clinical-trials
#10
Radojka M Savic, Marc Weiner, William R Mac Kenzie, Melissa Engle, William C Whitworth, John L Johnson, Pheona Nsubuga, Payam Nahid, Nhung Viet Nguyen, Charles A Peloquin, Kelly E Dooley, Susan E Dorman
Rifapentine is a highly active antituberculosis antibiotic with treatment-shortening potential; however, exposure-response relations and the dose needed for maximal bactericidal activity have not been established. We used pharmacokinetic/pharmacodynamic data from 657 adults with pulmonary tuberculosis participating in treatment trials to compare rifapentine (n = 405) with rifampin (n = 252) as part of intensive-phase therapy. Population pharmacokinetic/pharmacodynamic analyses were performed with nonlinear mixed-effects modeling...
January 25, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28122892/safety-efficacy-and-pharmacokinetics-of-humanized-anti-cd52-monoclonal-antibody-alemtuzumab-in-japanese-patients-with-relapsed-or-refractory-b-cell-chronic-lymphocytic-leukemia
#11
Kenichi Ishizawa, Noriko Fukuhara, Chiaki Nakaseko, Shigeru Chiba, Michinori Ogura, Akihiko Okamoto, Yoshinori Sunaga, Kensei Tobinai
OBJECTIVE: To evaluate the safety, efficacy and pharmacokinetics of alemtuzumab in Japanese patients, we conducted a phase I study in patients with relapsed or refractory B-cell chronic lymphocytic leukemia. METHODS: Six patients received alemtuzumab by intravenous infusion every other day three times a week for 12 weeks. The dose was gradually escalated on daily basis (3, 10 and then 30 mg) until the patient tolerated. The primary objective was to evaluate the safety of alemtuzumab in Japanese patients and the secondary objectives were to evaluate the overall response rate and the pharmacokinetics...
January 2017: Japanese Journal of Clinical Oncology
https://www.readbyqxmd.com/read/28099979/milrinone-pharmacokinetics-and-pharmacodynamics-in-neonates-with-persistent-pulmonary-hypertension-of-the-newborn
#12
Annie Giaccone, Athena F Zuppa, Beena Sood, Meryl S Cohen, Michael L O'Byrne, Ganesh Moorthy, Amit Mathur, Haresh Kirpalani
Objective To describe the pharmacokinetics and pharmacodynamics of milrinone in infants with persistent pulmonary hypertension of the newborn (PPHN) and to explore the impact of age on milrinone disposition. Design Randomized, open label pilot study. Setting Multicenter; level 3 and level 4 neonatal intensive care units. Patients Six infants ≥34 weeks' gestational age and <10 days of life with persistent hypoxemia receiving inhaled nitric oxide. Intervention Intravenous milrinone lactate in one of two dosing regimens: (1) low dose, 20 mcg/kg bolus followed by 0...
January 18, 2017: American Journal of Perinatology
https://www.readbyqxmd.com/read/28095918/anti-staphylococcal-activity-resulting-from-epithelial-lining-fluid-elf-concentrations-of-amikacin-inhale-administered-via-the-pulmonary-drug-delivery-system
#13
Islam M Ghazi, Mordechai Grupper, David P Nicolau
BACKGROUND: Amikacin inhale (BAY41-6551), a unique drug-device combination of a specially formulated drug solution and a pulmonary drug delivery system device (AMK-I) is currently under phase III study as an adjunctive therapy to IV antibiotics for the treatment of Gram-negative pneumonia in mechanically ventilated patients. While the epidemiology of nosocomial pneumonia is predominated by Gram-negative pathogens such as Pseudomonas aeruginosa and the Enterobacteriaceae, Staphylococcus aureus is increasingly recognized as a pathogen of concern for these pulmonary based infections...
January 17, 2017: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/28092695/absorption-distribution-and-excretion-of-the-anti-tuberculosis-drug-delamanid-in-rats-extensive-tissue-distribution-suggests-potential-therapeutic-value-for-extrapulmonary-tuberculosis
#14
Masakazu Shibata, Yoshihiko Shimokawa, Katsunori Sasahara, Noriaki Yoda, Hiroyuki Sasabe, Mitsunari Suzuki, Ken Umehara
Delamanid (OPC-67683, Deltyba(TM) , nitro-dihydro-imidazooxazoles derivative) is approved for the treatment of adult pulmonary multidrug-resistant tuberculosis. The absorption, distribution, and excretion of delamanid-derived radioactivity were investigated after a single oral administration of (14) C-delamanid at 3 mg/kg to rats. In both male and female rats, radioactivity in blood and all tissues reached peak levels by 8 or 24 hours postdose, and thereafter decreased slowly. Radioactivity levels were 3- to 5-fold higher in lung tissue at time to maximum concentration compared with plasma...
January 16, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28089914/arachidonic-acid-with-taurine-enhances-pulmonary-absorption-of-macromolecules-without-any-serious-histopathological-damages
#15
Masateru Miyake, Takanori Minami, Hiroyuki Yamazaki, Chie Emoto, Tadashi Mukai, Hajime Toguchi
Therapeutic peptides and protein are being used in several indications; however, their poor permeability still remains to be solved. This study focused on the pulmonary route of macromolecules. First, the effects of arachidonic acid (AA) as an absorption enhancer on drug serum concentration, after intratracheal administration, were investigated in rats. Second, the safety of AA was assessed in rats in an acute toxicity study for 7 days. AA enhanced the exposure of both interferon-α (IFN-α) and fluorescein isothiocyanate 4000 (FD-4)...
January 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28078552/pediatric-development-of-bosentan-facilitated-by-modeling-and-simulation
#16
Jochen Zisowsky, Martine Géhin, Andjela Kusic-Pajic, Andreas Krause, Maurice Beghetti, Jasper Dingemanse
BACKGROUND: Bosentan is approved for use in adult patients with pulmonary arterial hypertension. The primary aim of the pharmacokinetic modeling was the provision of a systematic guidance for study design and enhanced understanding of pharmacokinetics across the entire pediatric age range. METHODS: A physiologically based pharmacokinetic model was developed for the pediatric population; starting from an adult model, the effects of body weight, age, and maturation of relevant metabolizing enzymes were incorporated to extrapolate the pharmacokinetics to children...
January 11, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28074294/-procedures-on-patients-receiving-noacs-what-s-possible
#17
A Polzin, M Kelm, P Horn
Non-vitamin K antagonist oral anticoagulants (NOACs) are increasingly used in patients with deep vein thrombosis (DVT), pulmonary embolism (PE) and atrial fibrillation (AF). However, there is insufficient data concerning the periinterventional, perioperative, and intensive care management of patients on NOACs. Therefore, the recommendations regarding this management rely on pharmacokinetics of the particular NOAC in combination with the individual patient's characteristics, bleeding risk of the planned intervention/surgery, and urgency of the procedure...
January 10, 2017: Medizinische Klinik, Intensivmedizin und Notfallmedizin
https://www.readbyqxmd.com/read/28063154/pharmacological-indices-and-pulmonary-distribution-of-rifampicin-after-repeated-oral-administration-in-healthy-foals
#18
S Berlin, A Kirschbaum, L Spieckermann, S Oswald, M Keiser, M Grube, M Venner, W Siegmund
BACKGROUND: The treatment of equine lung infections by Rhodococcus equi with rifampicin is empirically based because pharmacokinetic/pharmacodynamic (PK/PD) indices and pivotal clinical outcome data are not available. OBJECTIVES: To evaluate the pharmacokinetics and pulmonary distribution of rifampicin into epithelial lining fluid (ELF) and bronchoalveolar lavage cells (BALC) to predict antimicrobial activity in the lung using PK/PD indices. STUDY DESIGN: Controlled, randomised, two-period, crossover, repeated-dose study with an initial arm to measure disposition after i...
January 7, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/28061907/a-randomized-seven-day-study-to-assess-the-efficacy-and-safety-of-a-glycopyrrolate-formoterol-fumarate-fixed-dose-combination-metered-dose-inhaler-using-novel-co-suspension%C3%A2-delivery-technology-in-patients-with-moderate-to-very-severe-chronic-obstructive-pulmonary
#19
Colin Reisner, Leonardo M Fabbri, Edward M Kerwin, Charles Fogarty, Selwyn Spangenthal, Klaus F Rabe, Gary T Ferguson, Fernando J Martinez, James F Donohue, Patrick Darken, Earl St Rose, Chad Orevillo, Shannon Strom, Tracy Fischer, Michael Golden, Sarvajna Dwivedi
BACKGROUND: Long-acting muscarinic antagonist/long-acting β2-agonist combinations are recommended for patients whose chronic obstructive pulmonary disease (COPD) is not managed with monotherapy. We assessed the efficacy and safety of glycopyrrolate (GP)/formoterol fumarate (FF) fixed-dose combination delivered via a Co-Suspension™ Delivery Technology-based metered dose inhaler (MDI) (GFF MDI). METHODS: This was a Phase IIb randomized, multicenter, placebo-controlled, double-blind, chronic-dosing (7 days), crossover study in patients with moderate-to-very severe COPD ( NCT01085045 )...
January 6, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28061018/bronchopulmonary-pharmacokinetics-of-r-salbutamol-and-s-salbutamol-enantiomers-in-pulmonary-epithelial-lining-fluid-and-lung-tissue-of-horses
#20
Glenn A Jacobson, Sharanne Raidal, Kate Robson, Christian K Narkowicz, David S Nichols, E Haydn Walters
AIMS: Salbutamol is usually administered as a racemic mixture but little is known about the enantioselectivity of salbutamol pharmacokinetics in the lung. This study was designed to investigate enantiomer concentrations in lung tissue after inhaled dosing. METHODS: Horses (n = 12) received racemic salbutamol 1000 μg via inhalation. Enantioselective ultra performance liquid chromatography-tandem mass spectrometry was used to determine salbutamol concentrations in pulmonary epithelial lining fluid (PELF) sampled 2, 5, 10 and 15 min after administration, in central lung (endoscopic bronchial biopsy) and peripheral lung (percutaneous pulmonary biopsy) tissues (at 20 and 25 min respectively), and in plasma samples...
January 6, 2017: British Journal of Clinical Pharmacology
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