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水牛犊单次静脉注射林可霉素后的药代动力学

Pharmacokinetics of lincomycin following single intravenous administration in buffalo calves.

作者信息

Sreeshitha Gouri Sreedharan, Venkatachalam Dinakaran, Dumka Vinod Kumar

机构信息

Department of Veterinary Pharmacology and Toxicology, Guru Angad Dev Veterinary and Animal Sciences University, Ludhiana, 141004, India.

出版信息

Trop Anim Health Prod. 2014 Aug;46(6):1099-102. doi: 10.1007/s11250-014-0595-4. Epub 2014 May 4.

Abstract

Lincomycin 10 mg kg(-1), IV in buffalo calves followed two-compartment open model with high distribution rate constant α (11.2 ± 0.42 h(-1)) and K 12/K 21 ratio (4.40 ± 0.10). Distribution half-life was 0.06 ± 0.01 h and AUC was 41.6 ± 1.73 μg mL(-1) h. Large Vdarea (1.15 ± 0.03 L kg(-1)) indicated good distribution of lincomycin in various body fluids and tissues. Peak plasma level of lincomycin (71.8 ± 1.83 μg mL(-1)) was observed at 1 min as expected by IV route. The elimination half-life and MRT of lincomycin were short (3.30 ± 0.08 and 4.32 ± 0.11 h, respectively). Lincomycin 10 mg kg(-1) IV at 12-h interval would be sufficient to maintain T > MIC above 60 % for bacteria with minimum inhibitory concentrations (MIC) values ≤1.6 μg mL(-1). Favourable pharmacokinetic profile in buffalo calves and a convenient dosing interval suggest that lincomycin may be an appropriate antibacterial in buffalo species for gram-positive and anaerobic bacterial pathogens susceptible to lincomycin.

摘要

在水牛犊牛中静脉注射10 mg/kg的林可霉素,其药代动力学符合二室开放模型,分布速率常数α较高(11.2±0.42 h⁻¹),K₁₂/K₂₁比值为(4.40±0.10)。分布半衰期为0.06±0.01 h,药时曲线下面积(AUC)为41.6±1.73 μg·mL⁻¹·h。较大的表观分布容积(1.15±0.03 L/kg)表明林可霉素在各种体液和组织中分布良好。正如静脉注射途径所预期的那样,在1分钟时观察到林可霉素的血浆峰值水平(71.8±1.83 μg·mL⁻¹)。林可霉素的消除半衰期和平均滞留时间较短(分别为3.30±0.08 h和4.32±0.11 h)。对于最低抑菌浓度(MIC)值≤1.6 μg·mL⁻¹的细菌,每隔12小时静脉注射10 mg/kg的林可霉素足以使T>MIC维持在60%以上。水牛犊牛具有良好的药代动力学特征和方便的给药间隔,这表明林可霉素可能是水牛物种中针对对林可霉素敏感的革兰氏阳性菌和厌氧菌病原体的合适抗菌药物。

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