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.
Copyright © 2012 Elsevier B.V. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acrylates / administration & dosage
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Acrylates / chemistry
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Acrylates / pharmacokinetics
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Administration, Rectal
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Animals
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Anti-Bacterial Agents / administration & dosage
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacokinetics
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Azithromycin / administration & dosage
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Azithromycin / chemistry*
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Azithromycin / pharmacokinetics
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Gelatin / administration & dosage
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Gelatin / chemistry
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Gelatin / pharmacokinetics
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Hydrogels / administration & dosage
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Hydrogels / chemistry
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Hydrogels / pharmacokinetics
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Hydrogen-Ion Concentration
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Hypromellose Derivatives
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Methylcellulose / administration & dosage
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Methylcellulose / analogs & derivatives
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Methylcellulose / chemistry
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Methylcellulose / pharmacokinetics
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Polyethylene Glycols / administration & dosage
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Polyethylene Glycols / chemistry
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Polyethylene Glycols / pharmacokinetics
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Rabbits
Substances
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Acrylates
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Anti-Bacterial Agents
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Hydrogels
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carbopol 974P NF
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Hypromellose Derivatives
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Polyethylene Glycols
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Azithromycin
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Gelatin
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Methylcellulose