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某些对取代乙酰苯胺在单独存在以及在泊洛沙姆存在的情况下对金鱼的生物有效性。

Biological effectiveness, in goldfish, of some p-substituted acetanilides alone and in the presence of poloxamers.

作者信息

Collett J H, Tobin E A

出版信息

J Pharm Pharmacol. 1979 Aug;31(8):517-20. doi: 10.1111/j.2042-7158.1979.tb13575.x.

Abstract

The death times of goldfish have been measured in aqueous solutions containing different concentrations of p-substituted acetanilides alone or in the presence of poloxamers. Plots of reciprocal death time versus concentration were linear with a positive concentration intercept, the minimum effective concentration (MEC). The MEC values were directly related to the pi value (hydrophobic-lipophilic constant) of the functional group on the acetanilide indicating that activity is directly related to lipophilicity. Slopes of reciprocal death time versus drug concentration were linearly related to pi values but there was no direct dependence. The presence of poloxamers in aqueous acetanilide solutions reduced the goldfish death time. The effect of the poloxamers is believed to be one of rendering the goldfish membrane more permeable to drugs.

摘要

已测定了金鱼在单独含有不同浓度对取代乙酰苯胺或含有泊洛沙姆的水溶液中的死亡时间。倒数死亡时间与浓度的关系图呈线性,具有正的浓度截距,即最低有效浓度(MEC)。MEC值与乙酰苯胺上官能团的π值(疏水亲脂常数)直接相关,表明活性与亲脂性直接相关。倒数死亡时间与药物浓度关系图的斜率与π值呈线性相关,但没有直接相关性。在乙酰苯胺水溶液中加入泊洛沙姆会缩短金鱼的死亡时间。据信,泊洛沙姆的作用是使金鱼膜对药物更具渗透性。

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