The Pharmacokinetics of Ivermectin in Rabbit

E. Shu, P. Okonkwo
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Abstract

Objective: To establish the pharmacokinetics of ivermectin in the rabbit model as a basis for future screening of newly developed micro and macrofilaricides. Method: Pharmacokinetic parameters of ivermectin were investigated in 5 rabbits after a single subcutaneous dose (150ug/kg), as a basis for screening micro- and macro-filaricides. Plasma ivermectin levels were measured by a sensitive High Performance Liquid Chromatography (HPLC) with fluorometric detection method. Results: The mean ±SEM pharmacokinetic parameters were as follows: time taken from dosing to maximum concentration (T max ), 1.4 ±0.4 hrs; maximum concentration (C max ), 34.0 ±1.6ng/ml; volume of distribution (V), 4.8 ±1.3L/kg; area under the plasma concentration-time curve (AUC), 475.6 ±5.4ng.hr/ml; plasma clearance (CI), 9.2 ±1.8ml/min and elimination half life (t), 10.4 ±2.3hrs. Conclusion: The elimination phase of ivermectin pharmacokinetics reveals a secondary peak suggestive of an enterohepatic recycling. Key Words: HPLC, Pharmacokinetics, Ivermectin Orient Journal of Medicine Vol.15(3&4) 2003:42-45
伊维菌素在家兔体内的药动学
目的:建立伊维菌素在家兔体内的药动学,为今后新开发的微、大杀丝剂的筛选奠定基础。方法:研究伊维菌素单次皮下给药(150ug/kg) 5只家兔的药动学参数,作为筛选微、宏杀丝剂的依据。采用高效液相色谱荧光检测法测定血浆伊维菌素水平。结果:平均±SEM药代动力学参数为:给药至最大浓度时间(tmax)为1.4±0.4 hrs;最大浓度(C max), 34.0±1.6ng/ml;分布容积(V), 4.8±1.3L/kg;血浆浓度-时间曲线下面积(AUC): 475.6±5.4ng.hr/ml;血浆清除率(CI) 9.2±1.8ml/min,消除半衰期(t) 10.4±2.3hrs。结论:伊维菌素药代动力学消除期出现二次峰,提示肠肝循环。关键词:高效液相色谱,药代动力学,伊维菌素。东方医学杂志Vol.15(3&4) 2003:42-45
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