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Single-dose azithromycin microsphere formulation: a novel delivery system for antibiotics
1Department of Internal Medicine, University of South Carolina School of Medicine, Columbia, SC 29203, USA. damrol@sc.edu
Abstract:
Azithromycin extended release (Zmax, Pfizer Inc) is a novel single-dose administration formulation of azithromycin which won FDA approval in June 2005 and is currently approved for the treatment of community acquired pneumonia and acute bacterial sinusitis. Azitromycin is incorporated into sustained-release microspheres which release the drug slowly through 200 microm pores. Because of this sustained release mechanism, most of the drug is released into the lower gastrointestinal tract, reducing gastrointestinal side-effects, and allowing for a higher dose to be administered. The unique pharmacological properties and extremely long half-life of azithromycin make this drug well suited to single-dose administration but gastrointestinal side effects have previously hampered single-dose therapy.
Insights
Azithromycin extended release (Zmax) offers a novel single-dose treatment for pneumonia and sinusitis. Its sustained-release microspheres reduce gastrointestinal side effects, improving tolerability for single-dose azithromycin therapy.
Area of Science:
- Pharmacology
- Drug Delivery Systems
Background:
- Azithromycin is an effective antibiotic for bacterial infections.
- Previous single-dose azithromycin formulations were limited by gastrointestinal side effects.
- Community-acquired pneumonia and acute bacterial sinusitis are common infections.
Purpose of the Study:
- To evaluate the novel single-dose azithromycin extended-release formulation (Zmax).
- To assess the efficacy and tolerability of Zmax for treating community-acquired pneumonia and acute bacterial sinusitis.
Main Methods:
- Development of azithromycin incorporated into sustained-release microspheres.
- Utilizing 200-micrometer pores for slow drug release.
- Administration as a single dose.
Main Results:
- The extended-release formulation directs most of the azithromycin to the lower gastrointestinal tract.
- This sustained release mechanism reduces gastrointestinal side effects.
- Enables administration of a higher azithromycin dose, improving suitability for single-dose therapy.
Conclusions:
- Azithromycin extended release (Zmax) provides an improved option for single-dose antibiotic therapy.
- The formulation overcomes previous limitations of gastrointestinal side effects associated with single-dose azithromycin.
- Zmax is approved for treating community-acquired pneumonia and acute bacterial sinusitis.
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