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大菱鲆(Scophthalmus maximus)单次口服给药后,恶喹酸的非连续吸收过程的药代动力学。

Pharmacokinetics of a discontinuous absorption process of oxolinic acid in turbot, Scophthalmus maximus, after a single oral administration.

作者信息

Poher I, Blanc G

机构信息

Equipe Associée INRA/ENVN, Chimiothérapie Aquacole et Environnement, Ecole Nationale Vétérinaire de Nantes, France.

出版信息

Xenobiotica. 1998 Nov;28(11):1061-73. doi: 10.1080/004982598238958.

Abstract
  1. The pharmacokinetics of oxolinic acid have been studied in 500 g turbot (Scophthalmus maximus). The fish were kept in seawater at 16 degrees C with a 15 h/9 h photoperiod. Oxolinic acid was administered orally via a stomach tube at a single dose of 10 mg/kg of body weight. Serum concentrations of oxolinic acid were determined by a (HPLC) using liquid phase extraction with an internal standard and a fluorescence detection. 2. The pharmacokinetic process was not significantly sex-influenced. The short elimination phase of the oxolinic acid in turbot after oral administration was similar to the elimination after intravascular administration. The serum concentration profile of oxolinic acid was better described by a discontinuous absorption model than by compartment models using continuous absorption processes. The absorption of oxolinic acid in turbot was characterized by two distinct phases after a lag time of about 2 h. A time (Tmax) of 12 h was necessary to reach the peak serum concentration (Cmax) of 1.41 microg/ml. The oral bioavailability was 27.9%. 3. Based on the minimum inhibitory concentration for susceptible strains, and especially Vibrio anguillarum, the oxolinic acid could be effective in turbot after an oral treatment of 10 mg/kg/day.
摘要
  1. 已在500克大菱鲆(Scophthalmus maximus)中研究了恶喹酸的药代动力学。将鱼饲养在16摄氏度的海水中,光照周期为15小时/9小时。通过胃管以10毫克/千克体重的单剂量口服给予恶喹酸。使用内标和荧光检测的液相萃取通过高效液相色谱法(HPLC)测定血清中恶喹酸的浓度。2. 药代动力学过程没有受到显著的性别影响。口服给药后,大菱鲆体内恶喹酸的消除期较短,这与血管内给药后的消除情况相似。与使用连续吸收过程的房室模型相比,用不连续吸收模型能更好地描述恶喹酸的血清浓度曲线。大菱鲆对恶喹酸的吸收在约2小时的滞后时间后表现为两个不同的阶段。达到1.41微克/毫升的血清峰值浓度(Cmax)需要12小时(Tmax)。口服生物利用度为27.9%。3. 根据对敏感菌株,尤其是鳗弧菌的最低抑菌浓度,口服10毫克/千克/天的剂量后,恶喹酸对大菱鲆可能有效。

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