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长效头孢噻呋制剂(头孢噻呋晶体游离酸)在球蟒(球蟒)体内的药代动力学

Pharmacokinetics of a long-acting ceftiofur formulation (ceftiofur crystalline free acid) in the ball python (Python regius).

作者信息

Adkesson Michael J, Fernandez-Varon Emilio, Cox Sherry, Martín-Jiménez Tomás

机构信息

Saint Louis Zoo, 1 Government Drive, St. Louis, Missouri 63110, USA.

出版信息

J Zoo Wildl Med. 2011 Sep;42(3):444-50. doi: 10.1638/2011-0016.1.

Abstract

The objective of this study was to determine the pharmacokinetics of a long-acting formulation of ceftiofur crystalline-free acid (CCFA) following intramuscular injection in ball pythons (Python regius). Six adult ball pythons received an injection of CCFA (15 mg/kg) in the epaxial muscles. Blood samples were collected by cardiocentesis immediately prior to and at 0.5, 1, 2, 4, 8, 12, 18, 24, 48, 72, 96, 144, 192, 240, 288, 384, 480, 576, 720, and 864 hr after CCFA administration. Plasma ceftiofur concentrations were determined by high-performance liquid chromatography. A noncompartmental pharmacokinetic analysis was applied to the data. Maximum plasma concentration (Cmax) was 7.096 +/- 1.95 microg/ml and occurred at (Tmax) 2.17 +/- 0.98 hr. The area under the curve (0 to infinity) for ceftiofur was 74.59 +/- 13.05 microg x h/ml and the elimination half-life associated with the terminal slope of the concentration-time curve was 64.31 +/- 14.2 hr. Mean residence time (0 to infinity) was 46.85 +/- 13.53 hr. CCFA at 15 mg/kg was well tolerated in all the pythons. Minimum inhibitory concentration (MIC) data for bacterial isolates from snakes are not well established. For MIC values of < or =0.1 microg/ml, a single dose of CCFA (15 mg/kg) provides adequate plasma concentrations for at least 5 days in the ball python. For MICs > or =0.5 microg/ml, more frequent dosing or a higher dosage may be required.

摘要

本研究的目的是确定头孢噻呋无结晶游离酸(CCFA)长效制剂在球蟒(Python regius)肌肉注射后的药代动力学。六只成年球蟒在轴旁肌肉注射CCFA(15mg/kg)。在CCFA给药前及给药后0.5、1、2、4、8、12、18、24、48、72、96、144、192、240、288、384、480、576、720和864小时通过心脏穿刺采集血样。采用高效液相色谱法测定血浆头孢噻呋浓度。对数据进行非房室药代动力学分析。最大血浆浓度(Cmax)为7.096±1.95μg/ml,出现在(达峰时间)2.17±0.98小时。头孢噻呋的曲线下面积(0至无穷大)为74.59±13.05μg·h/ml,与浓度-时间曲线终末斜率相关的消除半衰期为64.31±14.2小时。平均驻留时间(0至无穷大)为46.85±13.53小时。所有球蟒对15mg/kg的CCFA耐受性良好。蛇类细菌分离株的最低抑菌浓度(MIC)数据尚不明确。对于MIC值≤0.1μg/ml,单剂量CCFA(15mg/kg)在球蟒体内可提供至少5天的足够血浆浓度。对于MIC≥0.5μg/ml,可能需要更频繁给药或更高剂量。

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