title: Screening paediatric rectal forms of azithromycin as an alternative to oral or injectable treatment.
abstract: 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.
authors.affiliation: Univ. Bordeaux, EA 4575 Analytical and Pharmaceutical Developments Applied to Neglected Diseases and Counterfeits, Bordeaux, France. tina.kauss@u-bordeaux2.fr
authors.forename: Tina
authors.initials: T
authors.lastname: Kauss
authors.forename: Karen
authors.initials: K
authors.lastname: Gaudin
authors.forename: Alexandra
authors.initials: A
authors.lastname: Gaubert
authors.forename: Boubakar
authors.initials: B
authors.lastname: Ba
authors.forename: Serena
authors.initials: S
authors.lastname: Tagliaferri
authors.forename: Fawaz
authors.initials: F
authors.lastname: Fawaz
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Fabre
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Boiron
authors.forename: Xavier
authors.initials: X
authors.lastname: Lafarge
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: White
authors.forename: Piero L
authors.initials: PL
authors.lastname: Olliaro
authors.forename: Pascal
authors.initials: P
authors.lastname: Millet
mesh_terms: D000179:Acrylates / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000285:Administration, Rectal; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D017963:Azithromycin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D005780:Gelatin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D020100:Hydrogels / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011817:Rabbits
chemical_list: D000179:Acrylates; D000900:Anti-Bacterial Agents; D020100:Hydrogels; C117167:carbopol 974P NF; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols; D017963:Azithromycin; D005780:Gelatin; D008747:Methylcellulose