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Interactions between sparfloxacin and antacids - dissolution and adsorption studies.

Fida Hussain1, M Saeed Arayne, Najma Sultana

  • 1Department of Chemistry, University of Karachi, Karachi-75270, Pakistan.

Pakistan Journal of Pharmaceutical Sciences
|April 25, 2006
PubMed
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Concurrent use of antacids significantly reduces sparfloxacin absorption, potentially leading to treatment failure. This study investigated how common antacids affect sparfloxacin availability, finding varied impacts on dissolution rates.

Area of Science:

  • Pharmacology
  • Drug Interactions
  • Pharmaceutical Sciences

Background:

  • Sparfloxacin is a broad-spectrum fluoroquinolone antibiotic with a long half-life.
  • Concurrent administration with antacids can decrease sparfloxacin gastrointestinal absorption, risking therapeutic failure.

Purpose of the Study:

  • To evaluate the influence of common antacids on the in vitro availability of sparfloxacin.
  • To assess the impact of various antacids on sparfloxacin dissolution rates.

Main Methods:

  • Dissolution testing of sparfloxacin tablets was performed using a BP 2003 apparatus.
  • Studies were conducted in simulated gastric and intestinal juices at 37°C for three hours.
  • The effects of sodium bicarbonate, calcium hydroxide, calcium carbonate, aluminum hydroxide, magnesium hydroxide, magnesium carbonate, magnesium trisilicate, and magaldrate were examined.

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Main Results:

  • All tested antacids markedly retarded the dissolution rate of sparfloxacin tablets.
  • Magaldrate and calcium carbonate showed higher adsorption capacities in simulated gastric juice.
  • Magnesium trisilicate and calcium hydroxide demonstrated higher adsorption capacities in simulated intestinal juice.

Conclusions:

  • The co-administration of sparfloxacin with common antacids significantly impacts its dissolution and, consequently, its bioavailability.
  • Different antacids exhibit varying degrees of interaction with sparfloxacin, influencing its release profile in simulated gastric and intestinal environments.