截短侧耳素衍生物BC-7013在鸡体内的药物动力学和生物利用度研究  

Research on pharmacokinetics and bioavailability of pleuromutilin derivative BC-7013 in chickens

作　　者：杨德学[1] 陈良柱[2] 赖丽虹 任妙贤 张桂君[2] 潘志坤 方炳虎[1] 

机构地区：[1]华南农业大学兽医学院,广东广州510642 [2]广东大华农动物保健品股份有限公司,广东新兴527439

出　　处：《华南农业大学学报》2015年第4期26-31,共6页Journal of South China Agricultural University

基　　金：国家自然科学基金(31172359)

摘　　要：【目的】研究截短侧耳素衍生物BC-7013在鸡体内的药物动力学(简称药动学)特征及生物利用度.【方法】6周龄健康白羽肉鸡20只随机分为2组,雌雄各半,分别进行单剂量静脉注射(简称静注,2.5 mg·kg-1)和单剂量口服(15 mg·kg-1)截短侧耳素衍生物BC-7013.以高效液相色谱-串联质谱(HPLC-MS/MS)内标法定量测定血浆中衍生物BC-7013的浓度,采用Win Nonlin 5.2药动学软件的非房室模型统计矩原理分析药物浓度-时间数据,并计算其药动学参数.【结果和结论】鸡静注给药后药动学参数为:t1/2β=(1.37±0.14)h,Vd=(1.87±0.25)L·kg-1,AUC(0→∞)=(2.83±0.56)μg·m L-1·h,CL=(1.14±0.28)L·h-1·kg-1;鸡口服给药后药动学参数为:tmax=(1.94±0.26)h,Cmax=(126.18±6.54)ng·m L-1,AUC(0→∞)=(1.38±0.21)μg·m L-1·h,MRT=(9.49±0.57)h,F=(10.37±1.48)%.截短侧耳素衍生物BC-7013在鸡体内的药动学特征表现为:静注给药后分布广,消除快;口服给药后吸收较快但不完全,生物利用度较低.【Objective】The pharmacokinetical characteristics and bioavailability of pleuromutilin derivative BC-7013 in chickens were investigated. 【Method 】 Twenty chickens were randomly divided into two groups for pharmacokinelical experiments after a single intravenous（ 2. 5 mg·kg^- 1） and oral administration（ 15 mg·kg^- 1）. Blood samples were collected at different intervals after the administration of derivative BC-7013. The concentrations of derivative BC-7013 in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry（ HPLC-MS/MS） with internal standard method. Plasma concentration-time profiles of derivative BC-7013 were analyzed by using non-compartmental analysis Win Nonlin 5. 2 software. 【Result and conclusion】The main pharmacokinetical parameters of i. v. administration were as follows： t1 /2β=（ 1. 37 ± 0. 14） h,Vd =（ 1. 87 ± 0. 25） L·kg- 1,AUC（ 0→∞）=（ 2. 83 ±0. 56） μg·L^- 1·h,CL =（ 1. 14 ± 0. 28） L·h- 1·kg- 1. The major pharmacokinetical parameters of oral administration were as follows： tmax=（ 1. 94 ± 0. 26） h,Cmax=（ 126. 18 ± 6. 54） ng·m L- 1,AUC（ 0→∞）=（ 1. 38 ± 0. 21） μg·m L- 1·h,MRT =（ 9. 49 ± 0. 57） h,F =（ 10. 37 ± 1. 48） %. The results show that the pharmacokinetical characteristics of pleuromutilin derivative BC-7013 in healthy chicken manifest wide distribution,rapid elimination as well as incomplete absorption and low oral bioavailability.

关 键 词：衍生物BC-7013 药物动力学 生物利用度 HPLC-MS/MS 鸡 

分 类 号：S859.7[农业科学—临床兽医学]