The Mechanism of Release of Azithromycin

June 1, 2012

 

Lyon, D. K., "The Mechanism of Release of Azithromycin," Bulletin Technique Gattefossé 105(2012)106-112.

 

Zmax® is a single-dose antibiotic approved in the United States and Japan for treatment of acute bacterial sinusitis and community-acquired pneumonia. Zmax® is modifiedrelease azithromycin microspheres combined with sugar, flavors, and an alkalinizing compound in an oral formulation that is resuspended before dosing. This paper discusses the mechanism of azithromycin release from the modified-release microspheres, which contain Compritol® and a poloxamer. Based on azithromycin and poloxamer dissolution tests and microscopy, azithromycin is released from the microspheres after dissolving in liquid-filled pores that are formed following rapid dissolution of the poloxamer.