A Physiologically Based Pharmacokinetic Model for Biperiden in Animals and Its Extrapolation to Humans

Emi Nakashima, Koichi Yokogawa, Fujio Ichimura, Tsukinaka Yamana, Kouichi Kurata, Hideki Kido, Nariyoshi Yamaguchi

研究成果: Article査読

19 被引用数 (Scopus)

抄録

The disposition characteristics of biperiden were investigated in rats, rabbits, beagles, and humans, and a physiologically based pharmacokinetic model was established by using the hepatic intrinsic clearance of unbound drug concentration and the tissue-to-plasma unbound concentration ratios. Protein-binding parameters and blood-to-plasma concentration ratios were determined, and linear parameters were obtained in beagles and humans over a wide concentration range. The hepatic intrinsic clearance of humans was predicted from the animal data. The coincidence of each tissue-to-plasma Unbound concentration ratio between rats and rabbits was confirmed in the steady state, and the mean tissue-to-plasma unbound concentration ratios were used for the prediction of the plasma concentration-time courses of beagles and humans. The predicted lines fitted the observed plasma concentrations of beagles and a patient well after a single intravenous injection and repeated intramuscular administrations, respectively.

本文言語English
ページ(範囲)718-725
ページ数8
ジャーナルChemical and Pharmaceutical Bulletin
35
2
DOI
出版ステータスPublished - 1987

ASJC Scopus subject areas

  • 化学 (全般)
  • 創薬

フィンガープリント

「A Physiologically Based Pharmacokinetic Model for Biperiden in Animals and Its Extrapolation to Humans」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル