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氟甲喹在鳕鱼(大西洋鳕)和金鳍雀鲷中的单剂量药代动力学

Single-dose pharmacokinetics of flumequine in cod (Gadus morhua) and goldsinny wrasse (Ctenolabrus rupestris).

作者信息

Hansen M K, Horsberg T E

机构信息

Department of Pharmacology, Microbiology and Food Hygiene, Norwegian School of Veterinary Science, Oslo.

出版信息

J Vet Pharmacol Ther. 2000 Jun;23(3):163-8. doi: 10.1046/j.1365-2885.2000.00259.x.

Abstract

Knowledge of the pharmacokinetic properties of drugs to combat bacterial infections in cod (Gadus morhua) and wrasse (Ctenolabrus rupestris) is limited. One antimicrobial agent likely to be effective is flumequine. The aim of this study was to investigate the pharmacokinetic properties of flumequine in these two species. Flumequine was administered intravenously to cod (G. morhua) at a dose of 5 mg/kg bodyweight and wrasse (C. rupestris) at a dose of 10 mg/kg. Flumequine was also administered orally to both species at a dose of 10 mg/kg body weight, and as a bath treatment at a dose of 10 mg/L water for 2 h. Identical experimental designs were used otherwise. The study was performed in seawater with a salinity of 3.2% and a temperature of 8.0 +/- 0.2 degrees C (cod) and 14.5 +/- 0.4 degrees C (wrasse). Pharmacokinetic modelling of the data showed that flumequine had quite different pharmacokinetic properties in cod and wrasse. Following intravenous administration, the volumes of distribution at steady-state (Vss) were 2.41 L/kg (cod) and 2.15 L/kg (wrasse). Total body clearances (Cl) were 0.024 L/hxkg (cod) and 0.14 L/hxkg (wrasse) and the elimination half-lives (t1/2lambda z) were calculated to be 75 h (cod) and 31 h (wrasse). Mean residence times (MRT) were 99 h (cod) and 16 h (wrasse). Following oral administration, the t1/2 lambda z were 74 h (cod) and 41 h (wrasse). Maximal plasma concentrations (tmax) were 3.5 mg/L (cod) and 1.7 mg/L (wrasse), and were observed 24 h post-administration in cod and 1 h post-administration in wrasse. The oral bioavailabilities (F) were calculated to be 65% (cod) and 41% (wrasse). Following bath administration, maximal plasma concentrations were 0.13 mg/L (cod) and 0.09 mg/L (wrasse), and were observed immediately after the end of the bath.

摘要

对于鳕鱼(大西洋鳕)和隆头鱼(岩栖栉隆头鱼)体内用于对抗细菌感染的药物的药代动力学特性,人们了解有限。一种可能有效的抗菌剂是氟甲喹。本研究的目的是调查氟甲喹在这两个物种中的药代动力学特性。以5毫克/千克体重的剂量对鳕鱼(大西洋鳕)静脉注射氟甲喹,以10毫克/千克的剂量对隆头鱼(岩栖栉隆头鱼)静脉注射氟甲喹。还以10毫克/千克体重的剂量对这两个物种口服氟甲喹,并以10毫克/升水的剂量进行2小时的药浴处理。在其他方面采用相同的实验设计。该研究在盐度为3.2%、温度为8.0±0.2摄氏度(鳕鱼)和14.5±0.4摄氏度(隆头鱼)的海水中进行。对数据进行的药代动力学建模表明,氟甲喹在鳕鱼和隆头鱼中的药代动力学特性有很大不同。静脉注射后,稳态分布容积(Vss)分别为2.41升/千克(鳕鱼)和2.15升/千克(隆头鱼)。总体清除率(Cl)分别为0.024升/小时×千克(鳕鱼)和0.14升/小时×千克(隆头鱼),消除半衰期(t1/2λz)经计算分别为75小时(鳕鱼)和31小时(隆头鱼)。平均驻留时间(MRT)分别为99小时(鳕鱼)和16小时(隆头鱼)。口服给药后,t1/2λz分别为74小时(鳕鱼)和41小时(隆头鱼)。最大血浆浓度(tmax)分别为3.5毫克/升(鳕鱼)和1.7毫克/升(隆头鱼),在鳕鱼给药后24小时和隆头鱼给药后1小时观察到。口服生物利用度(F)经计算分别为65%(鳕鱼)和41%(隆头鱼)。药浴给药后,最大血浆浓度分别为0.13毫克/升(鳕鱼)和0.09毫克/升(隆头鱼),在药浴结束后立即观察到。

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