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Ceftriaxone Absorption Enhancement for Noninvasive Administration as an Alternative to Injectable Solutions.

Boubakar Ba1, Karen Gaudin1, Amélie Désiré1

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This summary is machine-generated.

Developing noninjectable ceftriaxone (antibiotic) formulations for neonatal sepsis is crucial. Rectal administration with absorption enhancers shows promise for reducing treatment delays in infants.

Keywords:
antibioticpediatricpediatric drug therapyrectal routethird-generation cephalosporins

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Area of Science:

  • Pharmacology
  • Neonatal Medicine
  • Drug Delivery Systems

Background:

  • Neonatal sepsis is a leading cause of infant mortality, particularly in developing nations.
  • Current injectable ceftriaxone treatment is hampered by delays in resource-limited settings.
  • Nonparenteral formulations are needed to improve accessibility and reduce treatment time.

Purpose of the Study:

  • To evaluate the nonparenteral absorption of ceftriaxone.
  • To explore the potential of noninjectable formulations for treating neonatal sepsis.
  • To present data supporting the development of noninvasive ceftriaxone treatments.

Main Methods:

  • Review of all available human and animal data on nonparenteral ceftriaxone absorption.
  • Preclinical studies using a rabbit model to assess rectal absorption.
  • Inclusion of historical unpublished data from F. Hoffmann-La Roche (Roche).

Main Results:

  • Rectal administration of ceftriaxone is feasible and can achieve adequate bioavailability.
  • A combination of 500 mg ceftriaxone and 125 mg Na-CDC (bile salt absorption enhancer) resulted in 24% rectal absorption in humans.
  • Maximal plasma concentration of 21 µg/ml was achieved with good tolerance in human subjects.

Conclusions:

  • Rectal ceftriaxone formulations are a viable option for treating neonatal sepsis.
  • Absorption enhancers like Na-CDC are effective in improving rectal bioavailability.
  • The developed rabbit model can screen future noninvasive drug formulations.