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[二甲基硅油对双香豆乙酯药代动力学和药效学的影响]

[Effect of dimethicone on pharmacokinetics and pharmacodynamics of ethyl biscoumacetate].

作者信息

Copie X, Pinquier J L, Letrait M, Paltiat M H, Pello J Y, Rey E, Chanteclair G, de Lauture D, Olive G, Strauch G

机构信息

Institut de Recherche Thérapeutique (IRT-Eclimed), Hôpital Cochin, Paris.

出版信息

Therapie. 1993 Mar-Apr;48(2):119-23.

PMID:8351679
Abstract

The influence of dimeticone (Gel de Polysilane Midy) on the pharmacokinetics and pharmacodynamics of oral ethyl biscoumacetate was studied in 6 healthy volunteers in a randomised single dose, two-way cross-over study. Each volunteer received at one week interval a single dose (300 mg) of ethyl biscoumacetate, either alone or with dimeticone. Ethyl biscoumacetate levels were measured in plasma for 24 hours. Pharmacodynamic parameters were measured for 96 hours. Ethyl biscoumacetate peak concentration was significantly higher when administered with dimeticone (40.3 +/- 25.3 mg/l vs 31.0 +/- 25.7 mg/l; p = 0.031), without significant change in the area under curve. Other pharmacokinetic and pharmacodynamic parameters did not differ significantly. The slight increase of the ethyl biscoumacetate bioavailability with dimeticone in repeated dosing might have pharmacodynamic consequence; a clinical trial should address this question.

摘要

在一项随机单剂量、双向交叉研究中,对6名健康志愿者研究了二甲基硅油(米迪聚硅氧烷凝胶)对口服双香豆乙酯药代动力学和药效学的影响。每位志愿者每隔一周接受一次单剂量(300毫克)的双香豆乙酯,单独服用或与二甲基硅油一起服用。在24小时内测定血浆中的双香豆乙酯水平。在96小时内测定药效学参数。与二甲基硅油一起给药时,双香豆乙酯的峰值浓度显著更高(40.3±25.3毫克/升对31.0±25.7毫克/升;p = 0.031),曲线下面积无显著变化。其他药代动力学和药效学参数无显著差异。重复给药时二甲基硅油使双香豆乙酯生物利用度略有增加可能具有药效学后果;一项临床试验应解决这个问题。

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