KINETIC PROFILES OF TIANEPTINE AND ITS MC5 METABOLITE IN PLASMA, BLOOD AND BRAIN AFTER SINGLE AND CHRONIC INTRAPERITONEAL ADMINISTRATION IN THE RAT
KINETIC PROFILES OF TIANEPTINE AND ITS MC5 METABOLITE IN PLASMA, BLOOD AND BRAIN AFTER SINGLE AND CHRONIC INTRAPERITONEAL ADMINISTRATION IN THE RAT
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DOI：
10.1007/bf03190130
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发表时间：
1990-01-01
影响因子：
1.9
通讯作者：
FOURTILLAN, JB
中科院分区：
文献类型：
--
作者：
COUET, W;GIRAULT, J;FOURTILLAN, JB
进行本研究以测定单次（10 mg·kg-1）和慢性（10 mg·kg-1·d-1和2 × 10 - 1）给药后抗抑郁剂噻奈普汀及其主要代谢物（名为MC 5）在血浆、血液和脑中的动力学曲线。10 mg·kg-1，持续15天）。在血浆中，噻奈普汀和MC 5很快达到峰值（分别为给药后5和15 min）。达峰后，噻奈普汀的消失速度快于MC 5，终末半衰期分别接近2.5和6.5 h。长期给药期间，噻奈普汀的蓄积可忽略不计，MC 5的蓄积轻微，蓄积比为1.28（每日一次给药）和1.73（每日两次给药）。噻奈普汀和MC 5迅速出现在脑组织中，但浓度低于血浆中观察到的浓度。脑中噻奈普汀的峰值浓度高于MC 5。观察到噻奈普汀和MC 5进入红细胞的渗透率非常低。
This study was conducted to determine kinetic profiles of the antidepressant tianeptine and its main metabolite (name MC5) in plasma, blood and brain after single (10 mg.cntdot.kg-1) and chronic (10 mg.cntdot.kg-1.cntdot.day-1 and 2 .times. 10 mg.cntdot.kg-1 for 15 days) intraperitoneal administration in Wistar rats. In plasma, tianeptine and MC5 reached a peak very quickly (5 and 15 min post administration respectively). Following the peak, disappearance of tianeptine was faster than that of MC5 with terminal half-lives close to 2.5 and 6.5 h respectively. During chronic treatment, accumulation of tianeptine was negligible, that of MC5 was slight as indicated by accumulation ratios equal to 1.28 (once daily administration) and 1.73 (twice daily administration). Tianeptine and MC5 rapidly appeared in brain tissue but a concentrations less than those observed in plasma. Peak concentrations of tianeptine in brain were higher than those of MC5. A very low penetration of tianeptine and MC5 into erythrocytes was observed.