喹烯酮在鸡体内的代谢及药物动力学研究  

Preliminary Study on Metabolism and Pharmacokinetics of Quinocetone in Chickens

作　　者：张桂君[1] 贺利民[1] 颜丹丹[1] 王瑛莹[1] 方炳虎[1] 

机构地区：[1]华南农业大学兽医学院,广东广州510642

出　　处：《动物医学进展》2011年第6期64-67,共4页Progress In Veterinary Medicine

基　　金：国家重点基础研究发展计划项目(973计划)(2009CB118805)

摘　　要：以HPLC-MS/MS为定量手段,研究了喹烯酮经静脉注射(2.5 mg/kg)、口服(30 mg/kg)两种给药途径在鸡体内的代谢及药物动力学特征。鸡静脉注射喹烯酮后,血浆中检测到喹烯酮原药和1-脱氧喹烯酮;口服灌注喹烯酮后,血浆中检测到喹烯酮原药和3-甲基喹噁啉-2-羧酸(MQCA)。喹烯酮在鸡体内的药动学数据采用统计矩法处理。静脉注射给药的主要药动学参数为t1/2β2.93 h±0.76 h,AUC0.33(μg.h)/mL±0.06(μg.h)/mL,MRT 2.27 h±0.40 h,Clβ10.34 L/(h.kg)-1±1.89 L/(h.kg)-1,Vss22.69 L/kg±5.73 L/kg;口服给药的主要药动学参数为t1/2β6.54 h±1.60 h,AUC0.86(μg.h)/mL±0.15(μg.h)/mL,Cmax0.10μg/mL±0.02μg/mL,Tmax2.82 h±0.72 h,MRT8.38 h±1.37 h,F 21.47%。结果表明,喹烯酮在鸡体内的主要代谢途径可能为脱氧,最后氧化水解生成MQCA。药物动力学特征表现为喹烯酮在体内吸收迅速、体内分布广泛、消除较缓慢、生物利用度低。A high-performance liquid chromatography with electrospray ionization tandem mass spectrometry method was developed to detect the plasma concentration of quinocetone in studying the pharmacokinetics properties of quinocetone after intravenous and oral administration of the drug at a single dosage of 2.5 mg/kg body weight（i.v.） and 30 mg/kg body weight（oral）.After intravenous administration,quinocetone and de-monoxy-quinocetone were detected in chicken plasma;after oral administration,quinocetone and MQCA were detected.Pharmacokinetics was performed by non-compartmental method using WinNonlin.The main pharmacokinetic parameters were as follows： intravenous administration,t1/2β2.93±0.76 h,AUC 0.33±0.06 μg·h/mL,MRT 2.27±0.40 h,Clβ10.34±1.89 L/h/kg,Vss22.69±5.73 L/kg;oral administration,t1/2β6.54±1.60 h,AUC 0.86±0.15 μg·h/mL,Cmax0.10±0.02 μg/mL,Tmax2.82±0.72 h,MRT8.38±1.37 h,F 21.47%.The results showed that the major metabolic pathway of quinocetone may deoxidate,and the pharmacokinetic characteristics of the quinocetone in chickens were as follows：fast absorption,wide distribution,slow elimination and low bioavailablability.

关 键 词：喹烯酮 代谢 药动学 HPLC-MS/MS 鸡 

分 类 号：S811.5[农业科学—畜牧学]