Cátedra de Farmacología, Facultad de Ciencias Veterinarias, Universidad de Buenos Aires, Chorroarín 280 (1427), Buenos Aires, Argentina.
Vet J. 2011 Jan;187(1):129-32. doi: 10.1016/j.tvjl.2009.09.019. Epub 2009 Oct 24.
The aim of this study was to characterise the pharmacokinetic properties of different formulations of erythromycin in cats. Erythromycin was administered as lactobionate (4 mg/kg intravenously (IV)), base (10mg/kg, intramuscularly (IM)) and ethylsuccinate tablets or suspension (15 mg/kg orally (PO)). After IV administration, the major pharmacokinetic parameters were (mean ± SD): area under the curve (AUC)((0-∞)) 2.61 ± 1.52 microgh/mL; volume of distribution (V(z)) 2.34 ± 1.76L/kg; total body clearance (Cl(t)) 2.1 0 ± 1.37 L/hkg; elimination half-life (t(½)(λ)) 0.75 ± 0.09 h and mean residence time (MRT) 0.88 ± 0.13 h. After IM administration, the principal pharmacokinetic parameters were (mean ± DS): peak concentration (C(max)), 3.54 ± 2.16 microg/mL; time of peak (T(max)), 1.22 ± 0.67 h; t(½)(λ), 1.94 ± 0.21 h and MRT, 3.50 ± 0.82 h. The administration of erythromycin ethylsuccinate (tablets and suspension) did not result in measurable serum concentrations. After IM and IV administrations, erythromycin serum concentrations were above minimum inhibitory concentration (MIC)(90)=0.5 microg/mL for 7 and 1.5h, respectively. However, these results should be interpreted cautiously since tissue erythromycin concentrations have not been measured and can reach much higher concentrations than in blood, which may be associated with enhanced clinical efficacy.
本研究旨在描述不同剂型红霉素在猫体内的药代动力学特性。给予乳糖酸红霉素(4mg/kg,静脉内(IV))、碱(10mg/kg,肌内(IM))和琥珀酸乙酯片或混悬剂(15mg/kg,口服(PO))。IV 给药后,主要药代动力学参数为:(均值±SD):曲线下面积(AUC)(0-∞)2.61±1.52μg·h/mL;分布容积(V(z))2.34±1.76L/kg;总体清除率(Cl(t))2.10±1.37L/h/kg;消除半衰期(t(½)(λ))0.75±0.09h和平均驻留时间(MRT)0.88±0.13h。IM 给药后,主要药代动力学参数为:峰浓度(C(max))3.54±2.16μg/mL;达峰时间(T(max))1.22±0.67h;t(½)(λ)1.94±0.21h和 MRT3.50±0.82h。给予红霉素琥珀酸乙酯(片剂和混悬剂)并未导致可测量的血清浓度。IM 和 IV 给药后,红霉素血清浓度分别超过最低抑菌浓度(MIC)(90)=0.5μg/mL 7h 和 1.5h。然而,这些结果应谨慎解释,因为尚未测量组织中的红霉素浓度,且组织中的浓度可能比血液中高得多,这可能与增强的临床疗效相关。