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: 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
• Journal: International journal of pharmaceutics (Int J Pharm) Vol. 436 Issue 1-2 Pg. 624-30 (Oct 15 2012) ISSN: 1873-3476 [Electronic] Netherlands
• PMID: 22868232 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier B.V. All rights reserved.

Chemical References

• Acrylates
• Anti-Bacterial Agents
• Hydrogels
• carbopol 974P NF
• Hypromellose Derivatives
• Polyethylene Glycols
• Azithromycin
• Gelatin
• Methylcellulose

Topics

• Acrylates (administration & dosage, chemistry, pharmacokinetics)
• Administration, Rectal
• Animals
• Anti-Bacterial Agents (administration & dosage, chemistry, pharmacokinetics)
• Azithromycin (administration & dosage, chemistry, pharmacokinetics)
• Gelatin (administration & dosage, chemistry, pharmacokinetics)
• Hydrogels (administration & dosage, chemistry, pharmacokinetics)
• Hydrogen-Ion Concentration
• Hypromellose Derivatives
• Methylcellulose (administration & dosage, analogs & derivatives, chemistry, pharmacokinetics)
• Polyethylene Glycols (administration & dosage, chemistry, pharmacokinetics)
• Rabbits