Fundamental Pharmacokinetic Properties of Biperiden: Tissue Distribution and Elimination in Rabbits

Koichi Yokogawa, Emi Nakashima, Tsukinaka Yamana, Fujio Ichimura

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

The pharmacokinetics of biperiden in rabbits were examined at three doses (0.2, 0.8, and 3.2 mg/kg i.v.). The data were interpreted in terms of a three-compartment open model with a linear excretion rate. The serum unbound fraction and the blood-to-plasma concentration ratio were determined as 0.39 and 1.2, respectively, over a wide concentration range (25-10000 ng/ml). Rapid and complete absorption from the injection site in muscle to the systemic circulation was observed. The bioavailability of muscular injection was unity. The hepatic extraction ratio was 0.94, and the high plasma clearance could be explained in terms of hepatic blood flow rate-limited elimination. The major tissues in which iperiden was distributed were fat and muscle. The highest tissue-to-plasma partition coefficient in the steady-state was obtained for the lung. These three tissues comprised 56% of the total distribution volume.

Original languageEnglish
Pages (from-to)409-416
Number of pages8
JournalJournal of Pharmacobio-Dynamics
Volume9
Issue number4
DOIs
Publication statusPublished - 1986 Jan 1

Keywords

  • biperiden
  • blood-to-plasma concentration ratio
  • elimination
  • pharmacokinetics
  • protein binding
  • rabbit
  • tissue distribution
  • tissue-to-plasma partition coefficient (K)

ASJC Scopus subject areas

  • Pharmacology

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