Pharmacokinetics in the calf of a long-acting chloramphenicol formulation administered intravenously and intramuscularly.

E Bousquet
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Abstract

In a preliminary study, 3 different chloramphenicol doses were tested by intramuscular (im) route, the highest one (90 mg/kg) being selected, based upon the duration of therapeutic serum levels (41.7 h). Following intravenous (iv) administration at this dose rate, the main pharmacokinetic parameters were: half-life of 6.0 h; body clearance, 0.101 l.kg-1.h-1; steady-state volume of distribution, 0.864 l.kg-1. Following a single im administration at the same dose, a mean maximum serum concentration of 22.9 microgram.ml-1 (Cmax) was reached in a mean time of 8.9 h (Tmax), therapeutic serum levels were achieved in an average period of 41.3 h. The mean half-life of the terminal phase was 10.3 h. Absolute bioavailability calculated based on 3 calves was 70.9 +/- 23.3% by im route. Pharmacokinetics of the long-acting formulation were confirmed in a repeated-dose study using the dosage schedule selected (2 injections im of 90 mg/kg at a 48 h interval).

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静脉注射和肌肉注射长效氯霉素制剂在小牛体内的药代动力学。
在初步研究中,通过肌肉注射(im)途径测试了3种不同剂量的氯霉素,根据治疗血清水平的持续时间(41.7 h)选择了最高剂量(90 mg/kg)。以该剂量率静脉(iv)给药后,主要药代动力学参数为:半衰期6.0 h;机体清除率0.101 l.kg-1.h-1;稳态分布体积:0.864 l.kg-1。在同一剂量单次注射后,平均最高血清浓度为22.9微克。平均8.9 h (Tmax)达到ml-1 (Cmax),平均41.3 h达到治疗血清水平。终末期平均半衰期为10.3 h。通过im途径计算的3头小牛的绝对生物利用度为70.9±23.3%。长效制剂的药代动力学在重复给药研究中得到证实,使用所选择的给药方案(每次注射90 mg/kg,间隔48 h)。
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