FUNDAMENTAL PHARMACOKINETIC PROPERTIES OF BIPERIDEN : TISSUE DISTRIBUTION AND ELIMINATION IN RABBITS

概要

論文の詳細を見る
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 mg/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 biperiden 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.
公益社団法人日本薬学会の論文