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阿普拉霉素在肉鸡体内的动力学处置、全身生物利用度及组织分布

Kinetic disposition, systemic bioavailability and tissue distribution of apramycin in broiler chickens.

作者信息

Afifi N A, Ramadan A

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.

出版信息

Res Vet Sci. 1997 May-Jun;62(3):249-52. doi: 10.1016/s0034-5288(97)90199-5.

Abstract

Apramycin was administered to chickens orally, intramuscularly and intravenously to determine blood concentration, kinetic behaviour, bioavailability and tissue residues. Single doses of apramycin at the rate of 75 mg kg-1 body weight were given to broiler chickens by intracrop, i.m. and i.v. routes. The highest serum concentrations of apramycin were reached 0.20 and 0.76 hours after the oral and i.m. doses with an absorption half-life (t1/2(ab.)) of 0.10 and 0.19 hours and an elimination half life (t1/2(beta)) of 1.22 and 2.31 hours respectively. The systemic bioavailability was 2.0 and 58 per cent after intracrop and i.m. administration, respectively, indicating poor absorption of the drug when given orally. Following i.v. injection, the kinetics of apramycin was described by a two-compartment open model with a (t1/2(alpha)) of 1.5 hours, (t1/2(beta)) of 2.1 hours. Vd(ss) (volume of distribution) of 4.82 litre kg-1 and C1(B) (total body clearance) of 1.88 litre kg-1 hour-1. The serum protein-binding of apramycin was 26 per cent. The highest tissue concentrations of apramycin were present in the kidneys and liver. No apramycin residues were detected in tissues after six hours except in the liver and kidneys following intracrop dosing and kidneys following i.m. administration.

摘要

将阿普拉霉素经口、肌肉注射和静脉注射给予鸡,以测定其血药浓度、动力学行为、生物利用度和组织残留。按75 mg kg-1体重的剂量,通过嗉囊内、肌肉注射和静脉注射途径给肉鸡单剂量给予阿普拉霉素。口服和肌肉注射给药后,分别在0.20小时和0.76小时达到阿普拉霉素的最高血清浓度,吸收半衰期(t1/2(ab.))分别为0.10小时和0.19小时,消除半衰期(t1/2(beta))分别为1.22小时和2.31小时。嗉囊内给药和肌肉注射给药后的全身生物利用度分别为2.0%和58%,表明口服给药时药物吸收较差。静脉注射后,阿普拉霉素的动力学可用二室开放模型描述,α半衰期(t1/2(alpha))为1.5小时,β半衰期(t1/2(beta))为2.1小时,稳态分布容积(Vd(ss))为4.82 litre kg-1,全身清除率(C1(B))为1.88 litre kg-1 hour-1。阿普拉霉素的血清蛋白结合率为26%。阿普拉霉素在肾脏和肝脏中的组织浓度最高。除嗉囊内给药后肝脏和肾脏以及肌肉注射给药后肾脏外,6小时后在组织中未检测到阿普拉霉素残留。

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