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静脉注射和皮下注射莫西沙星后,哺乳期山羊的药代动力学及乳汁渗透情况

Pharmacokinetics and milk penetration of moxifloxacin after intravenous and subcutaneous administration to lactating goats.

作者信息

Fernández-Varón Emilio, Villamayor Lucia, Escudero Elisa, Espuny Alberto, Cárceles Carlos M

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Campus de Espinardo, 30.071-Murcia, Spain.

出版信息

Vet J. 2006 Sep;172(2):302-7. doi: 10.1016/j.tvjl.2005.04.017.

Abstract

The pharmacokinetics of moxifloxacin was studied following intravenous (IV) and subcutaneous (SC) administration of 5 mg/kg to healthy lactating goats (n = 6). Moxifloxacin concentrations were determined by high performance liquid chromatography assay with fluorescence detection. The moxifloxacin plasma concentration versus time data after IV administration could best be described by a two compartment open model. The disposition of SC administered moxifloxacin was best described by a one-compartment model. The plasma moxifloxacin clearance (Cl) for the IV route was 0.43 +/- 0.02 L/kg (mean +/- SE). The steady-state volume of distribution (Vss) was 0.79 +/- 0.08 L/kg. The terminal half-life (t1/2lambdaz) was 1.94 +/- 0.41 and 2.98 +/- 0.48 h after IV and SC administration, respectively. The absolute bioavailability was 96.87 +/- 10.27% after SC administration. Moxifloxacin penetration from blood to milk was quick for both routes of administration and the high AUCmilk/AUCplasma and Cmax-milk/Cmax-plasma ratios reached indicated a wide penetration of moxifloxacin into the milk. From these data, it appears that a 5 mg/kg SC dose of moxifloxacin would be effective in lactating goats against bacterial isolates with MIC < or = 0.20 microg/mL in plasma and MIC < or = 0.40 microg/mL in milk.

摘要

对6只健康泌乳山羊静脉注射(IV)和皮下注射(SC)5mg/kg莫西沙星后的药代动力学进行了研究。采用高效液相色谱荧光检测法测定莫西沙星浓度。静脉给药后莫西沙星血浆浓度-时间数据最适合用二室开放模型描述。皮下注射莫西沙星的处置情况最适合用一室模型描述。静脉给药途径的血浆莫西沙星清除率(Cl)为0.43±0.02L/kg(平均值±标准误)。稳态分布容积(Vss)为0.79±0.08L/kg。静脉注射和皮下注射后终末半衰期(t1/2λz)分别为1.94±0.41小时和2.98±0.48小时。皮下给药后的绝对生物利用度为96.87±10.27%。两种给药途径下莫西沙星从血液到乳汁的渗透都很快,较高的AUC乳汁/AUC血浆和Cmax-乳汁/Cmax-血浆比值表明莫西沙星在乳汁中的广泛渗透。从这些数据来看,5mg/kg皮下注射剂量的莫西沙星似乎对泌乳山羊体内血浆中MIC≤0.20μg/mL、乳汁中MIC≤0.40μg/mL的细菌分离株有效。

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