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Cephradine antacids interaction studies.

M Saeed Arayne1, Najma Sultana, M Afzal

  • 1Department of Chemistry, University of Karachi, Karachi-75270, Pakistan. arayne@gawab.com

Pakistan Journal of Pharmaceutical Sciences
|June 5, 2007
PubMed
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Certain antacids, particularly those with polyvalent cations, significantly reduce cephradine availability. This interaction, involving strong adsorption, impacts the bioavailability of this first-generation cephalosporin antibiotic.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Interactions
  • Pharmacokinetics

Background:

  • Cephradine is a first-generation cephalosporin antibiotic effective against various Gram-positive and Gram-negative bacteria.
  • Antacids are frequently used for gastrointestinal issues, potentially leading to co-administration with antibiotics like cephradine.
  • Drug-complexing ligands can alter a drug's bioavailability, necessitating interaction studies.

Purpose of the Study:

  • To investigate the in vitro interaction between cephradine and seven common antacids.
  • To determine the effect of antacids on the dissolution and availability of cephradine.
  • To identify specific antacids that exhibit significant interactions with cephradine.

Main Methods:

  • Simulated physiological conditions to mimic natural environments for drug-antacid interactions.

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  • Utilized standard dissolution apparatus for in vitro testing.
  • Quantified cephradine levels using UV spectrophotometry and High-Performance Liquid Chromatography (HPLC).

    • Main Results:

    • Antacids containing polyvalent cations markedly reduced the in vitro availability of cephradine.
    • Cephradine demonstrated strong adsorption onto several antacid formulations.
    • Magnesium trisilicate and powdered simeco tablets showed the highest adsorption capacities for cephradine.

    Conclusions:

    • Co-administration of cephradine with polyvalent cation-containing antacids may impair its therapeutic efficacy due to reduced bioavailability.
    • The strong adsorption of cephradine onto specific antacids, like magnesium trisilicate, is a key factor in this interaction.
    • Clinical consideration is advised when prescribing cephradine to patients concurrently using these types of antacids.