两种给药方式下伊维菌素在虹鳟体内的药物代谢动力学研究

研究旨在通过口灌和腹腔注射两种给药方式,研究伊维菌素在虹鳟体内的药动学特征。采用高效液相色谱-紫外检测法(HPLC-UV)研究了以0.3 mg/kg剂量分别单次口灌和腹腔注射伊维菌素后,药物在虹鳟体内的药代动力学特征。结果表明:口灌给药方式下,伊维菌素在虹鳟血浆、肌肉中的药物浓度和时间关系符合一级吸收二室开放模型,而在肝脏、肾脏中符合一级吸收一室开放模型;腹腔注射给药方式下,伊维菌素在虹鳟血浆、肌肉、肝脏和肾脏中的药时关系均符合一级吸收一室开放模型。口灌给药后,伊维菌素在血浆中主要的药动学参数:AUC为123.709 mg/(L?h)、Ka为3.749 h-1、t1/2ke为466.569 h、Tmax为0.454 h、Cmax为0.319 mg/L。腹腔注射给药后,伊维菌素在血浆中主要的药动学参数:AUC为52.560 mg/(L?h)、Ka为5.033 h-1、t1/2ke为103.236 h、Tmax为1.317 h、Cmax为0.350 mg/L。说明在两种给药方式下,伊维菌素在虹鳟体内的药动学特征存在明显的差异,伊维菌素在腹腔注射给药方式下吸收和消除速率均较口灌给要快。

Pharmacokinetics of Ivermectin in Oncorhynchus mykiss Following Two Ways of Administration

This experiment was conducted to study Pharmacokinetics of ivermectin in Oncorhynchus mykiss following a single oral administration or intraperitoneal injection. Pharmacokinetics of ivermectin in Oncorhynchus mykiss was studied following a single oral or intraperitoneal injection at dose of 0.3 mg/kg by high-performance liquid chromatography-ultraviolet detection(HPLC-UV). The results showed that: after oral administration, the concentrations versus time of ivermectin in plasma and muscle were well described by two-department open model with first-order absorption, while those in liver and kidney were well described by one-department open model with first-order absorption; after intraperitoneal injection , the concentrations versus time of ivermectin in plasma, muscle, liver and kidney were well described by one-department open model with first-order absorption. After oral administration, the pharmacokinetic parameters in plasma were as follows: AUC=123.709 mg/(L?h), Ka=3.749 h^-1, t_1?2ke=466.569 h, T_max=0.454 h, C_max=0.319 mg/L; After intraperitoneal injection, the pharmacokinetic parameters in plasma were as follows: AUC=52.560 mg/(L?h), Ka=5.033 h^-1, t_1?2ke=103.236 h, T_max=1.317 h, C_max=0.350 mg/L. It stated that pharmacokinetics of ivermectin in Oncorhynchus mykiss were differences between two different administration routes, and intraperitoneal injection led to more rapid absorption and elimination than oral administration.