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替卡西林及替卡西林-丙磺舒在绵羊体内的药代动力学

Pharmacokinetics of ticarcillin and ticarcillin-probenecid in sheep.

作者信息

Errecalde J O, Lanusse C E, Mestorino O N, Landoni M F, Soraci A L

机构信息

Cátedra de Farmacología, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, Argentina.

出版信息

Zentralbl Veterinarmed A. 1991 May;38(4):255-60. doi: 10.1111/j.1439-0442.1991.tb01010.x.

Abstract

Serum concentrations of ticarcillin were measured serially over a period of 12h in a cross over trial involving 6 healthy adult ewes after intravenous and intramuscular (IM) administration of 40 mg ticarcillin per kg body weight. Probenecid (40 mg/kg) was also administered IM immediately before the IM administration of 40 mg/kg ticarcillin. Pharmacokinetic values after intravenous administration were: half-life of elimination (T 1/2 beta) = 0.90 +/- 0.09 h; volume of distribution at steady state (Vdss) = 456.8 +/- 106.6 ml/kg, total body clearance (CIB) = 614.5 +/- 81.2 ml/h/kg. Ticarcillin persisted in serum at greater than or equal to 1.5 micrograms/ml for 4 hours. Pharmacokinetic and bioavailability values after intramuscular administration were: half-life of absorption (T 1/2 ab) = 8.08 +/- 1.98 min; T 1/2 beta = 0.96 +/- 0.07 h. Peak serum concentration (Cmax) was 31.11 +/- 6.02 micrograms/ml at 0.50 h (Tmax), bioavailability (F) was 0.82 +/- 0.09. After ticarcillin was administered IM together with probenecid the T 1/2 ab was 33.9 +/- 13.7 min, the T 1/2 beta 2.66 +/- 0.65 h, Cmax = 44.87 +/- 5.58 at 1.33 +/- 0.44 h, and F = 1.25 +/- 0.23.

摘要

在一项交叉试验中,对6只健康成年母羊静脉注射和肌肉注射每千克体重40毫克替卡西林后,在12小时内连续测定血清中替卡西林的浓度。在肌肉注射40毫克/千克替卡西林之前,还立即肌肉注射丙磺舒(40毫克/千克)。静脉给药后的药代动力学值为:消除半衰期(T 1/2β)=0.90±0.09小时;稳态分布容积(Vdss)=456.8±106.6毫升/千克,总体清除率(CIB)=614.5±81.2毫升/小时/千克。替卡西林在血清中浓度大于或等于1.5微克/毫升的时间持续了4小时。肌肉注射后的药代动力学和生物利用度值为:吸收半衰期(T 1/2 ab)=8.08±1.98分钟;T 1/2β=0.96±0.07小时。在0.50小时(Tmax)时血清峰值浓度(Cmax)为31.11±6.02微克/毫升,生物利用度(F)为0.82±0.09。替卡西林与丙磺舒一起肌肉注射后,T 1/2 ab为33.9±13.7分钟,T 1/2β为2.66±0.65小时,在1.33±0.44小时时Cmax=44.87±5.58,F=1.25±0.23。

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