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[Pharmacokinetics of m-nifedipine in Beagle dogs]

Zhi-fu Yang1, Si-yuan Zhou, Tie-hong Yang

  • 1Department of Pharmacology, The Fourth Military Medical University, Xi'an 710032, China. yang_zf@hotmail.com

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|November 26, 2004
PubMed
Abstract

Insights

The pharmacokinetics of m-nifedipine (m-Nif) in Beagle dogs revealed rapid elimination. Oral administration of m-Nif resulted in very low absolute bioavailability, indicating limited absorption in this model.

Area of Science:

  • Pharmacology
  • Drug Metabolism and Pharmacokinetics

Background:

  • Nifedipine analogs are crucial in cardiovascular research.
  • Understanding the pharmacokinetic profile of m-nifedipine is essential for potential therapeutic applications.

Purpose of the Study:

  • To investigate the pharmacokinetic properties of m-nifedipine in Beagle dogs.
  • To determine the elimination rate and bioavailability of m-nifedipine following intravenous and oral administration.

Main Methods:

  • Beagle dogs were administered m-nifedipine intravenously (0.288 mg/kg) or orally (1.152, 3.456, 10.370 mg/kg).
  • Plasma concentrations of m-nifedipine were quantified using reversed-phase high-performance liquid chromatography.
  • Pharmacokinetic parameters were calculated using 3P97 software.

Main Results:

  • Intravenous administration followed a two-compartment model with a T1/2beta of 117 min.
  • Oral administration followed a one-compartment model.
  • Oral bioavailability was found to be very low, with dose-dependent Cmax values observed.

Conclusions:

  • m-Nifedipine exhibits a high elimination rate in Beagle dogs.
  • The absolute oral bioavailability of m-nifedipine is significantly low, suggesting poor absorption or extensive first-pass metabolism.

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