クレンチアゼム静脈内投与時のラットにおける体内動態: 組織内分布および血漿，脳ならびに肝臓中代謝物
1992 年 7 巻 6 号 p. 821-832
詳細
1992 年 7 巻 6 号 p. 821-832
The organ and tissue distribution of radioactivity, the concentration of acidic and basic metabolites in plasma, brain and liver were studied after intravenous administration of 14C-clentiazem at a dose of 3mg/kg to male and female rats. The plasma levels of radioactivity was higher in male rats than in female rats at any time examined. On the other hand, the radioactivity in the organs and tissues became higher in female rats than that in male rats with the lapse of time. The acidic metabolites which might be formed through oxidative deamination of clentiazem and the basic metabolites were higher in the plasma of male rats. The metabolites in the brain were mainly of basic character and the levels were higher in female rats. Few acidic metabolites were found in the brain of both male and female rats. One may expect that basic metabolites were easily transferred to the organs and tissues, while acidic metabolites were hardly transferred, due to their pKa values if the pH -partition theory is considered. Accordingly, it would be considered that plasma levels of radioactivity were higher in male rats while the organ and tissue levels of radioactivity were higher in female rats.
