Screening paediatric rectal forms of azithromycin as an alternative to oral or injectable treatment

• Main Authors: Tina Kauss, Karen Gaudin, Alexandra Gaubert, Boubakar Ba, Serena Tagliaferri, Fawaz Fawaz, Jean Louis Fabre, Jean Michel Boiron, Xavier Lafarge, Nicholas J. White, Piero L. Olliaro, Pascal Millet
• Other Authors: Developpements Analytiques et Pharmaceutiques Appliques aux Maladies Negligees et Aux Contrefacons
• Format: Article
• Published: 2018
• Subjects: Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://repository.li.mahidol.ac.th/handle/123456789/15155
• Institution: Mahidol University

The aim of this study was to identify a candidate formulation for further development of a home or near-home administrable paediatric rectal form of a broad-spectrum antibiotic - specially intended for (emergency) use in tropical rural settings, in particular for children who cannot take medications orally and far from health facilities where injectable treatments can be given. Azithromycin, a broad-spectrum macrolide used orally or intravenously for the treatment of respiratory tract, skin and soft tissue infections, was selected because of its pharmacokinetic and therapeutic properties. Azithromycin in vitro solubility and stability in physiologically relevant conditions were studied. Various pharmaceutical forms, i.e. rectal suspension, two different rectal gels, polyethylene glycol (PEG) suppository and hard gelatin capsule (HGC) were assessed for in vitro dissolution and in vivo bioavailability in the rabbit. Azithromycin PEG suppository appears to be a promising candidate. © 2012 Elsevier B.V. All rights reserved.