Aqueous acidic degradation of the carbacephalosporin loracarbef

J Pharm Sci. 1993 Oct;82(10):1010-7.

Abstract

The aqueous degradation of the carbacephalosporin loracarbef under moderately acidic conditions (pH range, 2.7-4.3) is described. Structures of a total of 10 compounds isolated by preparative reversed-phase HPLC have been proposed. Five of these 10 degradation compounds arose from hydrolysis of the beta-lactam ring followed by structural changes in the six-membered heterocyclic ring. Four compounds form from intermolecular reactions of loracarbef to form dimeric structures with peptide linkages. The remaining compound resulted from oxidation of the primary amine to a hydroxylamine. Pathways for the formation of these compounds from the parent loracarbef are proposed.

Publication types

  • Comparative Study

MeSH terms

  • Cefaclor / chemistry
  • Cephalosporins / chemistry*
  • Chromatography, High Pressure Liquid
  • Drug Stability
  • Hydrogen-Ion Concentration
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Structure
  • Solutions / chemistry

Substances

  • Cephalosporins
  • Solutions
  • loracarbef
  • Cefaclor