Haddad N S, Ravis W R, Pedersoli W M, Carson R L
Am J Vet Res. 1986 Apr;47(4):808-13.
Healthy mature lactating cows (n = 6) were given gentamicin (5 mg/kg of body weight) by IV route and another dose 19 days later by IM route. Serum gentamicin concentrations were determined over a period of 48 hours after each drug dosing, using radioimmunoassay. With the aid of a nonlinear least-square regression analysis program, the combined data of the IV and IM treatments were best fitted by a 2-compartment open model, as indicated by residual trends and improvements in the sum of squares by F test and the SD of the estimated values. The distribution phase half-life was 0.25 +/- 0.12 hour, and postdistribution half-life was 1.83 +/- 0.18 hours. The volume of the central compartment was 0.10 +/- 0.02 L/kg, volume of distribution at steady state was 0.16 +/- 0.03 L/kg, and the total body clearance was 1.32 +/- 0.17 ml/min/kg. Intramuscular absorption was rapid, with a half-life for absorption of 0.63 +/- 0.28 hour. The extent of IM absorption was 92% +/- 15%. The percentage of the IM dose eliminated in the urine during the first 8 hours was 83 +/- 8. Gentamicin was detected in milk for 48 hours. Kinetic calculations predicted that IM injection of gentamicin at a dosage of 3.5 mg/kg of body weight every 8 hours would provide average steady-state serum drug concentrations of 5.08 micrograms/ml, with minimum and maximum steady-state concentrations of 1.03 and 12.05 micrograms/ml, respectively, whereas an IM injection of a 5 mg/kg dosage every 8 hours would provide average steady-state serum concentrations of 7.26 micrograms/ml, with minimum and maximum steady-state serum concentrations of 1.47 and 17.21 micrograms/ml, respectively.
选用6头健康的成年泌乳奶牛,静脉注射庆大霉素(5毫克/千克体重),19天后再肌肉注射另一剂量。每次给药后48小时内,采用放射免疫分析法测定血清庆大霉素浓度。借助非线性最小二乘回归分析程序,静脉注射和肌肉注射治疗的合并数据通过二室开放模型得到最佳拟合,残差趋势以及F检验的平方和改善情况和估计值的标准差均表明了这一点。分布相半衰期为0.25±0.12小时,分布后半衰期为1.83±0.18小时。中央室容积为0.10±0.02升/千克,稳态分布容积为0.16±0.03升/千克,全身清除率为1.32±0.17毫升/分钟/千克。肌肉吸收迅速,吸收半衰期为0.63±0.28小时。肌肉注射的吸收程度为92%±15%。在最初8小时内,尿液中排出的肌肉注射剂量百分比为83±8。在牛奶中检测到庆大霉素的时间为48小时。动力学计算预测,每8小时肌肉注射3.5毫克/千克体重的庆大霉素,平均稳态血清药物浓度将达到5.08微克/毫升,最小和最大稳态浓度分别为1.03和12.05微克/毫升,而每8小时肌肉注射5毫克/千克剂量,平均稳态血清浓度将达到7.26微克/毫升,最小和最大稳态血清浓度分别为1.47和17.21微克/毫升。