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头孢他啶在泌乳和非泌乳奶牛中的药代动力学。

The pharmacokinetics of ceftazidime in lactating and non-lactating cows.

作者信息

Rule R, Quiroga G H, Rubio M, Buschiazzo H O, Buschiazzo P M

机构信息

Comisión de Investigaciones Científicas, Provincia de Buenos Aires; Argentina.

出版信息

Vet Res Commun. 1996;20(6):543-50. doi: 10.1007/BF00396297.

Abstract

The pharmacokinetics of ceftazidime (CAZ) were studied in lactating (LTG) and non-lactating (NLTG) cows. Two groups (LTG and NLTG) of 5 healthy dairy cows were given ceftazidime (10 mg/ kg body weight) intravenously (i.v.) and intramuscularly (i.m.). Serum and milk (LTG) and serum samples (NLTG) were collected over a 24-h period post-administration. CAZ concentrations in serum and milk were determined by high-performance liquid chromatography, and an interactive and weighted-non-linear least-squares regression analysis was used to perform the pharmacokinetic analysis. The pharmacokinetic profiles in LTG and NLTG cows which had received CAZ i.v. fitted a three-compartment model and a two-compartment model, respectively. The CAZ concentration-time curves in serum and the area under the curve were greater and more sustained (p < 0.05) in the LTG cows by both routes, while the serum clearance (Cls = 72.5 +/- 18.1 ml/h per kg) was lower (p < 0.05) than that in the NLTG cows (Cls = 185.9 +/- 44.2 ml/h per kg). CAZ given i.v. exhibited a relatively long half-life of elimination (t1/2 beta (LTG) = 1.1 +/- 0.2 h; t1/2 beta (NLTG) = 1.4 +/- 0.3 h). Compared with other cephalosporins, CAZ had good penetration into the mammary gland (47.7 +/- 38.2% for CAZ i.v.; 51.1 +/- 39.0% for CAZ i.m.). Finally, the bioavailability of CAZ (F(LTG) = 98.9 +/- 36.8%; F(NLTG) = 77.1 +/- 25.3%) was suitable for its used by the i.m. route in lactating and non-lactating cows.

摘要

在泌乳奶牛(LTG)和非泌乳奶牛(NLTG)中研究了头孢他啶(CAZ)的药代动力学。将两组(LTG和NLTG)各5头健康奶牛分别静脉注射(i.v.)和肌肉注射(i.m.)头孢他啶(10 mg/kg体重)。给药后24小时内采集血清和乳汁(LTG)以及血清样本(NLTG)。通过高效液相色谱法测定血清和乳汁中的CAZ浓度,并采用交互式加权非线性最小二乘回归分析进行药代动力学分析。静脉注射CAZ的LTG和NLTG奶牛的药代动力学曲线分别拟合三室模型和二室模型。两种给药途径下,LTG奶牛血清中的CAZ浓度-时间曲线和曲线下面积均更大且更持久(p < 0.05),而血清清除率(Cls = 72.5 +/- 18.1 ml/h per kg)低于(p < 0.05)NLTG奶牛(Cls = 185.9 +/- 44.2 ml/h per kg)。静脉注射CAZ的消除半衰期相对较长(t1/2β(LTG) = 1.1 +/- 0.2 h;t1/2β(NLTG) = 1.4 +/- 0.3 h)。与其他头孢菌素相比,CAZ在乳腺中的渗透良好(静脉注射CAZ为47.7 +/- 38.2%;肌肉注射CAZ为51.1 +/- 39.0%)。最后,CAZ的生物利用度(F(LTG) = 98.9 +/- 36.8%;F(NLTG) = 77.1 +/- 25.3%)适合其在泌乳和非泌乳奶牛中通过肌肉注射途径使用。

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