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Pulmonary pharmacokinetics

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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...
March 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28246425/influence-of-il-18-and-il-10-polymorphisms-on-tacrolimus-elimination-in-chinese-lung-transplant-patients
#9
Xiaoqing Zhang, Jiandong Xu, Junwei Fan, Tao Zhang, Yuping Li, Boxiong Xie, Wei Zhang, Shengtao Lin, Ling Ye, Yuan Liu, Gening Jiang
Aims. The influence of interleukin-10 (IL-10) and interleukin-18 (IL-18) polymorphisms on tacrolimus pharmacokinetics had been described in liver and kidney transplantation. The expression of cytokines varied in different kinds of transplantation. The influence of IL-10 and IL-18 genetic polymorphisms on the pharmacokinetic parameters of tacrolimus remains unclear in lung transplantation. Methods. 51 lung transplant patients at Shanghai Pulmonary Hospital were included. IL-18 polymorphisms (rs5744247 and rs1946518), IL-10 polymorphisms (rs1800896, rs1800872, and rs3021097), and CYP3A5 rs776746 were genotyped...
2017: Disease Markers
https://www.readbyqxmd.com/read/28223260/enhanced-pulmonary-absorption-of-poorly-soluble-itraconazole-by-micronized-cocrystal-dry-powder-formulations
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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