ラットおよびイヌにおける塩酸キナプリルの薬物動態

抄録

After oral administration of quinapril hydrochloride (3 mg/kg) to rats and dogs, the unchanged drug, its active metabolite (quinaprilat) and the diastereomers of quinaprilat in plasma were simultaneously analyzed using the gas chromato graph-negative ion chemical ionization mass spectrometer.
The obtained results are as follows: (1) In rats, the plasma concentration of quinaprilat reached the maximum (C_max) of 2.48 μg/ml at 0.38 hr after oral administration, and then disappeared with the terminal half-life (t_1/2z) of 33.9 hr. The unchanged drug in plasma was not detected throughout all the time point examined. The bioavailability of quinaprilat was 63.4%.
(2) In dogs, the plasma concentration of unchanged drug reached the C_max of 0.41μg/ml at 0.42 hr and that of quinaprilat reached the C_max of 3.51 μg/ml at 0.92 hr after oral administration. The unchanged drug in plasma quickly disappeared and quinaprilat disappeared with the t_1/2z of 16.8 hr. The bioavailability of quinaprilat was 47.1%.
(3) There were no changes in the configuration of quinapril and quinaprilat after oral administration to rats and dogs.