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[环扁桃酯给药后健康受试者药物脑电图与药代动力学-药效学关系的证据]

[Evidence of a pharmacokinetic-pharmacodynamic relationship between pharmaco-EEG in healthy subjects after administration of cyclandelate].

作者信息

Dimpfel W, Schober F, Wedekind W, Kleinbloesem C, Coors C

机构信息

Pro Science Private Research Institute GmbHa, Linden.

出版信息

Arzneimittelforschung. 1994 Sep;44(9):999-1004.

PMID:7986255
Abstract

In an open randomized cross-over study 800 mg cyclandelate (Natil, CAS 456-59-7) was applicated to 24 young, male volunteers. Before and during 24 h after application of a single dose a 17-channel, quantitative topographical pharmaco-EEG was recorded. A significant increase of the spectral power density was observed in the alpha 2, beta 1 and beta 2 frequency bands starting 2 h after application until 4.5 h. The increase in beta 1 and beta 2 power was observed in the parietocentral area of the cortex. The difference between the circadian development of the EEG power and the development after medication was obvious after 3 until 4.5 h. For the beta frequencies only a weak statistical confirmation could be obtained, but for the alpha 2 frequency a significant difference between the circadian and the EEG power under cyclandelate was found using the sign test. Altogether a quantitative effect on brain activity was detected after oral application of cyclandelate, reaching its maximum before the blood concentration of the metabolites cyclandic glucuronide and mandelic acid reached their peak heights.

摘要

在一项开放性随机交叉研究中,将800毫克环扁桃酯(Natil,CAS 456-59-7)应用于24名年轻男性志愿者。在单次给药前及给药后24小时内,记录17通道定量脑电地形图。在给药后2小时至4.5小时期间,观察到α2、β1和β2频段的频谱功率密度显著增加。在皮质顶中央区域观察到β1和β2功率增加。在3至4.5小时后,脑电图功率的昼夜变化与用药后的变化之间的差异明显。对于β频率,仅获得了微弱的统计学证实,但对于α2频率,使用符号检验发现环扁桃酯作用下的昼夜节律与脑电图功率之间存在显著差异。总体而言,口服环扁桃酯后检测到对脑活动有定量影响,在代谢产物环扁桃酸葡糖醛酸和扁桃酸的血药浓度达到峰值之前,这种影响达到最大。

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