ArticleAntimicrobial agents and chemotherapy2009
Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 70 citations in OpenAlex.
- The Pharmacokinetics of CPZEN-45, a Novel Anti-Tuberculosis Drug, in Guinea Pigs.Pharmaceutics · 2023Article
- Inhalable Combination Powder Formulations for Treating Latent and Multidrug-Resistant Tuberculosis: Formulation and In Vitro Characterization.Pharmaceutics · 2023Article
- Fed- and Fasted-State Performance of Pretomanid Amorphous Solid Dispersions Formulated with an Enteric Polymer.Molecular pharmaceutics · 2023Article
- A review of formulations and preclinical studies of inhaled rifampicin for its clinical translation.Drug delivery and translational research · 2023Review
- Delamanid or pretomanid? A Solomonic judgement!The Journal of antimicrobial chemotherapy · 2022Article
- Pretomanid for tuberculosis treatment: an update for clinical purposes.Current research in pharmacology and drug discovery · 2022Review
- Disposable Dosators for Pulmonary Insufflation of Therapeutic Agents to Small Animals.Journal of visualized experiments : JoVE · 2017Article
- Pharmacokinetics of Ethionamide Delivered in Spray-Dried Microparticles to the Lungs of Guinea Pigs.Journal of pharmaceutical sciences · 2017Article
- Emerging strategies for the treatment of pulmonary tuberculosis: promise and limitations?The Korean journal of internal medicine · 2016Review
- Pharmacologic considerations in use and development of antituberculosis drugs.Cold Spring Harbor perspectives in medicine · 2014Review
- A rifapentine-containing inhaled triple antibiotic formulation for rapid treatment of tubercular infection.Pharmaceutical research · 2014Article
- Potent rifamycin-sparing regimen cures guinea pig tuberculosis as rapidly as the standard regimen.Antimicrobial agents and chemotherapy · 2013Article
- Pharmaceutical aerosols for the treatment and prevention of tuberculosis.Frontiers in cellular and infection microbiology · 2012Review
- Nanoparticle delivery of anti-tuberculosis chemotherapy as a potential mediator against drug-resistant tuberculosis.The Yale journal of biology and medicine · 2011Review
- Nitroimidazoles for the treatment of TB: past, present and future.Future medicinal chemistry · 2011Review
- Dry powder PA-824 aerosols for treatment of tuberculosis in guinea pigs.Antimicrobial agents and chemotherapy · 2010Article
- Inhaled drug delivery for tuberculosis therapy.Pharmaceutical research · 2009Review
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
We formulated PA-824, a nitroimidazopyran with promise for the treatment of tuberculosis, for efficient aerosol delivery to the lungs in a dry powder porous particle form. The objectives of this study were to prepare and characterize a particulate form of PA-824, assess the stability of this aerosol formulation under different environmental conditions, and determine the pharmacokinetic parameters for the powder after pulmonary administration. The drug was spray dried into porous particles containing a high drug load and possessing desirable aerosol properties for efficient deposition in the lungs. The physical, aerodynamic, and chemical properties of the dry powder were stable at room temperature for 6 months and under refrigerated conditions for at least 1 year. Pharmacokinetic parameters were determined in guinea pigs after the pulmonary administration of the PA-824 powder formulation at three doses (20, 40, and 60 mg/kg of body weight) and compared to those after the intravenous (20 mg/kg) and oral (40 mg/kg) delivery of the drug. Oral and inhaled delivery of PA-824 achieved equivalent systemic delivery at the same body dose within the first 12 h of dosing. However, animals dosed by the pulmonary route showed drug loads that remained locally in the lungs for 32 h postexposure, whereas those given the drug orally cleared the drug more rapidly. Therefore, we expect from these pharmacokinetic data that pulmonary delivery may achieve the same efficacy as oral delivery at the same body dose, with a potential improvement in efficacy related to pulmonary infection. This may translate into the ability to deliver lower body doses of this drug for the treatment of tuberculosis by aerosol.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.