氟氯苯菊酯在犬体内的药动学初步研究

Preliminary studies on pharmacokinetics of flumethrin in dogs

关键词:  氟氯苯菊酯  浇泼剂  药动学  犬

Key words:  flumethrin  transdermal delivery system  pharmacokinetics  dogs

摘要:

【目的】研究自制1%氟氯苯菊酯浇泼剂在健康家犬体内的药代动力学特征。【方法】选用6条健康犬，以2mg/kg单剂量沿背中线浇泼，采用反相高效液相色谱法(RP-HPLC)测定犬血浆中氟氯苯菊酯浓度，用3P97药动软件处理药时数据，计算药代动力学参数。【结果】氟氯苯菊酯的药时数据符合一级吸收二室开放模型，主要药动学参数为：T1/2α为3.622±1.079 h，T1/2β为22.654±0.417 h，T1/2Ka为1.684±0.240 h，AUC为47.385±1.709 μg·mL-1·h，Tpeak为4.165±0.187 h，Cmax为1.902±0.064 μg·mL-1，Lag time为0.489±0.002 h。【结论】健康家犬单次给予氟氯苯菊酯浇泼剂后，吸收、消除均缓慢，药物在动物体内作用时间较长。

Abstract:

[Objection]Pharmacokinetics of flumethrin pour-on preparation (1%) was studied in healthy dogs.[Method]Flumethrin pour-on preparation was dermal administrated in a dose of 2 mg/kg·bw in 6 healthy dogs and the plasma concentration of flumethrin was detected by RP-HPLC.The concentration-time date were analyzed with 3P97 computer program.[Results]The pharmacokinetics characteristics was fit to two-compartment model with first order absorption rate.The main pharmacokinetics parameters were as follows:T1/2α was 3.622±1.079 h,T1/2β was 22.654±0.417 h,T1/2Ka was 1.684±0.240 h,AUC was 47.385±1.709 μg·mL-1·h,Tpeak was 4.165±0.187 h,Cmax was 1.902±0.064 μg/mL,Lag-time was 0.489±0.002 h.[Conclusion]We concluded that flumethrin both been absorbed and eliminated slowly and had a long persistence time.