Tina KaussAlexandra GaubertChantal BoyerBoubakar B. BaMuriel ManseStephane MassipJean Michel LégerFawaz FawazMartine LembegeJean Michel BoironXavier LafargeNiklas LindegardhNicholas J. WhitePiero OlliaroPascal MilletKaren GaudinDeveloppements Analytiques et Pharmaceutiques Appliques aux Maladies Negligees et Aux ContrefaconsUniversite de BordeauxEtablissement Francais du SangMahidol UniversityNuffield Department of Clinical MedicineOrganisation Mondiale de la Sante2018-10-192018-10-192013-01-30International Journal of Pharmaceutics. Vol.441, No.1-2 (2013), 218-22618733476037851732-s2.0-84872827650https://repository.li.mahidol.ac.th/handle/20.500.14594/32749Pharmaceutical development and manufacturing process optimization work was undertaken in order to propose a potential paediatric rectal formulation of azithromycin as an alternative to existing oral or injectable formulations. The target product profile was to be easy-to-use, cheap and stable in tropical conditions, with bioavailability comparable to oral forms, rapidly achieving and maintaining bactericidal concentrations. PEG solid solution suppositories were characterized in vitro using visual, HPLC, DSC, FTIR and XRD analyses. In vitro drug release and in vivo bioavailability were assessed; a study in rabbits compared the bioavailability of the optimized solid solution suppository to rectal solution and intra-venous product (as reference) and to the previous, non-optimized formulation (suspended azithromycin suppository). The bioavailability of azithromycin administered as solid solution suppositories relative to intra-venous was 43%, which compared well to the target of 38% (oral product in humans). The results of 3-month preliminary stability and feasibility studies were consistent with industrial production scale-up. This product has potential both as a classical antibiotic and as a product for use in severely ill children in rural areas. Industrial partners for further development are being sought. © 2012 Elsevier B.V. All rights reserved.Mahidol UniversityPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.1016/j.ijpharm.2012.11.040