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芬苯达唑在斑点叉尾鮰体内的药代动力学与代谢

Pharmacokinetics and metabolism of fenbendazole in channel catfish.

作者信息

Kitzman J V, Holley J H, Huber W G, Koritz G D, Davis L E, Neff-Davis C A, Bevill R F, Short C R, Barker S A, Hsieh L C

机构信息

College of Veterinary Medicine, Mississippi State, MS 39762.

出版信息

Vet Res Commun. 1990;14(3):217-26. doi: 10.1007/BF00347741.

Abstract

Fenbendazole (FBZ) was administered intravenously (1 mg/kg) and orally (5 mg/kg) to catheterized, confined channel catfish. Blood samples were collected for 72 h, and resulting FBZ plasma concentrations were pharmacokinetically modelled. Following intravenous administration t 1/2 alpha was 0.51 h, t 1/2 beta was 16.8 h, body clearance (C1B) was 0.0598 L/kg/h, and Vd (area) was 1.45 L/kg. After oral administration the t 1/2 (abs) was 1.47 h, the t 1/2 beta was 20.1 h, and the tlag was 0.1 h. Following oral administration of 5 mg FBZ/kg body weight, the following tissues and body fluids were sampled for concentrations of FBZ, oxfendazole (FBZ-SO), sulphone metabolite (FBZ-SO2) and hydroxy metabolite (FBZ-OH): liver, posterior kidney, fat, muscle, bowel contents and urine. Fenbendazole was detected in the highest concentrations in abdominal fat, whereas oxfendazole was found primarily in the kidney, liver and abdominal fat. The sulphone metabolite was detected only in urine and bowel contents, while the hydroxy metabolite was found most often in the liver and abdominal fat samples.

摘要

将芬苯达唑(FBZ)以静脉注射(1毫克/千克)和口服(5毫克/千克)的方式给予插管饲养在受限水槽中的鲶鱼。采集血样72小时,并对所得的FBZ血浆浓度进行药代动力学建模。静脉给药后,α半衰期为0.51小时,β半衰期为16.8小时,机体清除率(C1B)为0.0598升/千克/小时,分布容积(Vd(area))为1.45升/千克。口服给药后,吸收半衰期为1.47小时,β半衰期为20.1小时,延迟时间为0.1小时。口服5毫克FBZ/千克体重后,采集以下组织和体液样本以检测FBZ、奥芬达唑(FBZ-SO)、砜代谢物(FBZ-SO2)和羟基代谢物(FBZ-OH)的浓度:肝脏、后肾、脂肪、肌肉、肠内容物和尿液。在腹部脂肪中检测到芬苯达唑的浓度最高,而奥芬达唑主要存在于肾脏、肝脏和腹部脂肪中。砜代谢物仅在尿液和肠内容物中检测到,而羟基代谢物最常出现在肝脏和腹部脂肪样本中。

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