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替米考星在马组织和血浆中的药代动力学。

Pharmacokinetics of tilmicosin in equine tissues and plasma.

作者信息

Clark C, Dowling P M, Ross S, Woodbury M, Boison J O

机构信息

Department of Biomedical Sciences, Western College of Veterinary Medicine, University of Saskatchewan, Saskatoon, SK, Canada.

出版信息

J Vet Pharmacol Ther. 2008 Feb;31(1):66-70. doi: 10.1111/j.1365-2885.2007.00909.x.

DOI:10.1111/j.1365-2885.2007.00909.x
PMID:18177321
Abstract

The macrolide antibiotic tilmicosin has potential for treating bacterial respiratory tract infections in horses. A pharmacokinetic study evaluated the disposition of tilmicosin in the horse after oral (4 mg/kg) or subcutaneous (s.c.) (10 mg/kg) administration. Tilmicosin was not detected in equine plasma or tissues after oral administration at this dose. With s.c. injection, tilmicosin concentrations reached a maximum concentration of approximately 200 ng/mL in the plasma of the horses. Tilmicosin concentrations in plasma persisted with a mean residence time (MRT) of 19 h. Maximum tissue residue concentrations (C(max)) of tilmicosin measured in equine lung, kidney, liver and muscle tissues after s.c. administration were 2784, 4877, 1398, and 881 ng/g, respectively. The MRT of tilmicosin in these tissues was approximately 27 h. Subcutaneous administration of tilmicosin resulted in severe reactions at the injection sites.

摘要

大环内酯类抗生素替米考星具有治疗马细菌性呼吸道感染的潜力。一项药代动力学研究评估了口服(4mg/kg)或皮下(s.c.)(10mg/kg)给药后替米考星在马体内的处置情况。在此剂量口服给药后,马的血浆或组织中未检测到替米考星。皮下注射后,替米考星浓度在马血浆中达到约200ng/mL的最大浓度。血浆中替米考星浓度持续存在,平均驻留时间(MRT)为19小时。皮下给药后,在马的肺、肾、肝和肌肉组织中测得的替米考星最大组织残留浓度(C(max))分别为2784、4877、1398和881ng/g。替米考星在这些组织中的MRT约为27小时。皮下注射替米考星导致注射部位出现严重反应。

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