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恩拉霉素苯甲酸在鳕鱼(Gadus morhua L.)中的单剂量药代动力学研究,在 9°C 的海水中进行。

A single-dose pharmacokinetic study of emamectin benzoate in cod, Gadus morhua L., held in sea water at 9 degrees C.

机构信息

Institute of Marine Research, Nordnes, Bergen, Norway.

出版信息

J Fish Dis. 2010 Feb;33(2):137-42. doi: 10.1111/j.1365-2761.2009.01097.x. Epub 2009 Aug 30.

Abstract

The pharmacokinetic profile of the antiparasitic agent emamectin benzoate was studied in plasma after intravenous (i.v.) injection and in plasma, muscle and skin following oral (p.o.) administration to cod, Gadus morhua, held in sea water at 9 degrees C and weighing 100-200 g. Following i.v. injection, the plasma drug concentration-time profile showed two distinct phases. The plasma distribution half-life (t(1/2)alpha) was estimated as 2.5 h, the elimination half-life (t(1/2)beta) as 216 h, the total body clearance (Cl(T)) as 0.0059 L kg(-1) h(-1) and mean residence time (MRT) as 385 h. The volume of distribution at steady state, V(d(ss)), was calculated to be 1.839 L kg(-1). Following p.o. administration the peak plasma concentration (C(max)) was 15 ng mL(-1), the time to peak plasma concentration (T(max)) was 89 h and t(1/2)beta was 180 h. The highest concentration in muscle (21 ng g(-1)) was measured after 7 days and t(1/2)beta was calculated to be 247 h. For skin, a peak concentration of 28 ng g(-1) at 3 days was observed and a t(1/2)beta of 235 h was determined. The bioavailability following p.o. administration was calculated to be 38%.

摘要

抗寄生虫药埃玛菌素苯甲酸的药代动力学特征在静脉注射(i.v.)后以及在口服(p.o.)给予 9°C 海水环境下 100-200 克重的鳕鱼(Gadus morhua)后的血浆、肌肉和皮肤中进行了研究。静脉注射后,血浆药物浓度-时间曲线呈现两个明显的阶段。血浆分布半衰期(t(1/2)alpha)估计为 2.5 小时,消除半衰期(t(1/2)beta)为 216 小时,总体清除率(Cl(T))为 0.0059 L kg(-1) h(-1),平均驻留时间(MRT)为 385 小时。稳态分布容积(V(d(ss)))计算为 1.839 L kg(-1)。口服给药后,血浆峰浓度(C(max))为 15 ng mL(-1),达峰时间(T(max))为 89 小时,t(1/2)beta 为 180 小时。肌肉中(21 ng g(-1))的最高浓度在 7 天后测量,t(1/2)beta 计算为 247 小时。对于皮肤,在第 3 天观察到 28 ng g(-1)的峰值浓度,t(1/2)beta 为 235 小时。口服给药后的生物利用度计算为 38%。

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