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Pharmacokinetics of A40926 in rats after single intravenous and subcutaneous doses

A Bernareggi1, A Danese, L Cavenaghi

  • 1Merrell-Dow Research Institute, Lepetit Center, Gerenzano (VA), Italy.

Antimicrobial Agents and Chemotherapy
|February 1, 1988
PubMed

Insights

The glycopeptide antibiotic A40926 exhibits prolonged high plasma concentrations in rats after intravenous or subcutaneous administration. Its elimination is slow, with a terminal half-life of 61.22 hours, indicating extensive distribution.

Area of Science:

  • Pharmacology
  • Microbiology
  • Drug Development

Background:

  • A40926 is a novel glycopeptide antibiotic demonstrating unique efficacy against Neisseria gonorrhoeae.
  • Previous studies indicated high and sustained drug levels in mouse blood.

Purpose of the Study:

  • To investigate the pharmacokinetics of A40926 in rats following single intravenous and subcutaneous doses.
  • To determine drug concentrations in plasma and urine over time.

Main Methods:

  • Rats received a single 10-mg/kg intravenous or subcutaneous dose of A40926.
  • Plasma and urine samples were collected at various time points.
  • Antibiotic concentrations were quantified using microbiological assays.

Main Results:

  • Following intravenous administration, plasma concentrations ranged from 132 mg/L at 3 minutes to 0.7 mg/L at 96 hours.
  • A three-exponential decay was observed, reflecting prolonged biphasic distribution and slow elimination with a terminal half-life of 61.22 hours.
  • Subcutaneous administration showed rapid absorption with nearly 90% bioavailability, and 35.9% of the dose was excreted in urine within 120 hours.

Conclusions:

  • A40926 exhibits a pharmacokinetic profile characterized by extensive distribution and slow elimination in rats.
  • The slow return from deep tissue compartments appears to be the rate-limiting factor for A40926 elimination.
  • The drug demonstrates favorable absorption and bioavailability following subcutaneous administration.

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