Wilson R C, Whelan S C, Coulter D B, Mahaffey E A, Mahaffey M B, Huber T L
Am J Vet Res. 1981 Nov;42(11):1901-4.
Kinetics of gentamicin (2.2 mg/kg of body weight) were investigated in 7 sheep after IV bolus administration. The mean serum concentration profile could be described by a 2-compartment open model with a distribution rate constant (alpha) of 3.112 +/- 1.681 hour-1 [half-life, t1/2(alpha) = 17.22 +/- 8.63 minutes] and an overall elimination rate constant (beta) of 0.485 +/- 0.028 hour-1 [t1/2(beta) - 85.87 +/- 5.03 minutes]. The apparent volume of distribution was somewhat restricted [Vd(area) = 0.194 +/- 0.059 L/Kg], and the total body clearance was 1.559 +/- 0.400 ml/kg/min. Equal dosages of gentamicin (2.2 mg/kg) were also given IM and intratracheally (IT). after IM injection, gentamicin reached peak serum concentration at postinjection minutes (PIM) 45, surpassing concentrations after the IV injection for the remainder of the experiment. The IT injection produced detectable serum concentrations at PIM 5, with a peak concentration at PIM 60. The serum drug concentrations after IT injections remained well below concentrations after IV and IM injections. Radiographic analysis of an IT injection of a gentamicin-tantalum suspension revealed good distribution throughout the trachea and proximal bronchi, with physical clearance of the tantalum occurring after greater than or equal to 10 minutes. Aspiration biopsy of the tracheal wash 6 hours after IT gentamicin injection revealed no cytologic response to gentamicin in 6 of 7 sheep, with the single response that of a purulent exudate.
对7只绵羊静脉注射大剂量庆大霉素（2.2mg/kg体重）后的动力学进行了研究。平均血清浓度曲线可用二室开放模型描述，分布速率常数（α）为3.112±1.681小时-1[半衰期，t1/2(α)=17.22±8.63分钟]，总消除速率常数（β）为0.485±0.028小时-1[t1/2(β)=85.87±5.03分钟]。表观分布容积有所受限[Vd(area)=0.194±0.059L/Kg]，全身清除率为1.559±0.400ml/kg/min。还分别对绵羊进行了庆大霉素（2.2mg/kg）的肌肉注射和气管内注射。肌肉注射后，庆大霉素在注射后45分钟达到血清峰值浓度，在实验剩余时间内超过静脉注射后的浓度。气管内注射在注射后5分钟产生可检测到的血清浓度，在注射后60分钟达到峰值浓度。气管内注射后的血清药物浓度远低于静脉注射和肌肉注射后的浓度。对庆大霉素-钽混悬液气管内注射的影像学分析显示，药物在整个气管和近端支气管中分布良好，钽在大于或等于10分钟后出现物理清除。气管内注射庆大霉素6小时后对气管冲洗液进行抽吸活检，结果显示7只绵羊中有6只对庆大霉素无细胞学反应，唯一有反应的出现了脓性渗出物。
