摘要
本研究旨在建立犬血浆中米尔贝肟的LC-MS/MS检测方法,评价国产米尔贝肟片在犬体内的相对生物利用度。对12条比格犬采用开放、随机、交叉、单剂量给药,口服国产米尔贝肟片、进口米尔贝肟片。LC-MS/MS测定犬血浆中米尔贝肟的浓度,3p97药动学计算软件处理血浆药物-时间数据。该方法低浓度(5ng/mL)回收率高于85%,最低定量限为5ng/mL;健康犬口服进口和国产米尔贝肟片的药物动力学最佳数学模型均为一级吸收一室模型。本研究中建立的HPLC-MS/MS检测方法可用于口服给药后犬血浆中米尔贝肟含量的测定;口服国产米尔贝肟片与进口米尔贝肟片的相对生物利用度为99.07%。
The study was designed to develop a HPLC-MS/MS method for the determination of mllbe- mycin oxime in dog plasma and evaluate the bioavailability of milbemycin oxime in dogs by oral administrate. A single oral dose of 0.25 mg milbemycin oxime per tablet was given to 12 beagles in a random cross-over study. Concentrations of milbemycin oxime in plasma were determined by LC-MS/MS, and the concentration-time date was analyzed with 3pg7 computer program to get the pharmacokinetic parameters. Recoveries at low concentration（5 ng . mL-：） were higher than 85 %, and the limit of quantification was 5 ng . mL-1. The concentration-time data were fitted to a one-compartment model with Is＇ order absorptionafter oral milbemycin oxime tablet imported, and the main pharmacokinetic parameters were as follows： T1/2（ （1.07±0.03）h, V/F （2.65±0.08）L .kg-1 , CL/F （0. 155±0. 016）mL min-1 kg-1 , and AUC （1 614.61±186.32）ng .mL-1. h. The concentration-time data were fitted to a1 two-compartment model after oral milbemyein oxime tablet made in China, and the main pharmacokinetie parameters were as follows： T1/2（ka） （1.18±0.00）h, V/F （2.54±0.11）L. kg-1, CL/F （0. 156±0. 011）mL . rain. kg-1 , and AUC（1 599.64±122.79）ng .mL-1 .h-1. The method is suitable for the pharmaeokinetic study of milbemycin oxime after oral administration to dogs. The relative bioavailability of milbemycin oxime made in China and the imported one was 99.07 M.
出处
《中国兽医杂志》
CAS
北大核心
2012年第9期67-70,共4页
Chinese Journal of Veterinary Medicine
基金
"十一五"国家科技支撑计划项目(2006BAD31B02)
关键词
米尔贝肟
相对生物利用度
犬
milbemycin oxime
relative bioavailability
dog
