单次给药研究后丙戊酸在志愿者体内的药代动力学。

Pharmacokinetics of valproic acid in volunteers after a single dose study.

作者信息

Bialer M, Hussein Z, Raz I, Abramsky O, Herishanu Y, Pachys F

出版信息

Biopharm Drug Dispos. 1985 Jan-Mar;6(1):33-42. doi: 10.1002/bdd.2510060105.

Abstract

The pharmacokinetics of valproic acid (VPA) was investigated in six healthy volunteers. This was done by monitoring total and free (unbound) valproic acid levels in the serum, and the amount of one of its metabolites, VPA glucuronide, in the urine as a function of time, after a single dose administration of the parent drug. VPA half-life calculated from the urine data of the metabolite was shorter than the half-life calculated from the blood data. About 15 to 20 per cent of the administered oral dose of VPA was excreted in the urine as VPA glucuronide. The average free fraction of VPA obtained in this study, by using the EMIT technique, ranged from 1.5 to 11.5 per cent with a mean value of 4.9 per cent.

摘要

在六名健康志愿者身上研究了丙戊酸（VPA）的药代动力学。这是通过监测单次给予母体药物后血清中总丙戊酸和游离（未结合）丙戊酸水平，以及尿液中其一种代谢物丙戊酸葡萄糖醛酸苷的量随时间的变化来进行的。根据代谢物的尿液数据计算出的VPA半衰期比根据血液数据计算出的半衰期短。给予的口服VPA剂量约有15%至20%以丙戊酸葡萄糖醛酸苷的形式经尿液排泄。在本研究中，通过使用EMIT技术获得的VPA平均游离分数范围为1.5%至11.5%，平均值为4.9%。