Melt-Congealed Microspheres Enable Single Dose Antibiotic Therapy

摘要

A powder for oral suspension (POS) formulation of azithromycin was developed for single-dose oral antibiotic therapy. The formulation consists of drug-containing controlled-release microspheres manufactured by a melt-congealed process mixed with a vehicle blend which includes alkalizing agents. The formulation was designed to minimize GI side effects, allowing a sufficient dose of azithromycin, 2 grams, to be administered as a single oral dose therapy. To improve toleration, the azithromycin was released slowly from the microspheres, with more of the drug released further down the small intestine. However, to maintain bio-availability, essentially all of the azithromycin needed to be released in the small intestine since little azithromycin is absorbed from the colon. Several clinical studies have been conducted demonstrating efficacy and acceptable toleration of this single-dose oral antibiotic therapy.