富马酸喹硫平在大鼠体内的药动学研究  

Pharmacokinetic Study of Quetiapine Fumarate in Rats

作　　者：张文静[1] 李见春[1] 朱娜[1] 王秀[1] 张劲[1] 

机构地区：[1]蚌埠医学院药学系,安徽蚌埠233030

出　　处：《中国药房》2014年第37期3478-3480,共3页China Pharmacy

摘　　要：目的:测定富马酸喹硫平在大鼠体内的血药浓度,并研究其药动学特征。方法:取6只大鼠灌胃给予富马酸喹硫平40mg/kg,与给药前和给药后5、15、30、45 min和1、1.5、2、4、6、8、12、24 h静脉采血0.5 ml,离心后取血浆,用乙腈沉淀蛋白后直接进样,以卡马西平为内标物,反相高效液相色谱法测定血药浓度,采用DAS2.0软件分析药动学参数。结果:富马酸喹硫平在大鼠体内的药动学特征呈二室模型,主要药动学参数t1/2α为(20.132±1.198)min、t1/2β为(62.883±11.120)min、tmax为(40.00±8.66)min、cmax为(2.21±0.066)μg/ml、AUC0-24 h为(687.453±12.026)mg·min/L、V1/F为(8.244±0.679)L/kg、K10为(0.183±0.028)min-1、K12为(1.764±0.161)min-1、K21为(0.189±0.018)min-1。结论:富马酸喹硫平在大鼠体内的分布和消除均比较快,且分布不广泛。OBJECTIVE： To determine plasma concentration of quetiapine fumarate in rats, and to study the pharmacokinetic characteristics of it. METHODS： 6 rats were given quetiapine fumarate 40 mg/kg intragastrically. Blood samples 0.5 ml were collected from vein before medication, 5, 15, 30, 45 min and 1, 1.5, 2, 4, 6, 8, 12, 24 h after medication. The plasma sample was collected after centrifugation. After deproteinized with acetonitrile, plasma sample was directly injected. Using carbamazepine as internal standard, RP-HPLC was used. DAS 2.0 software was adopted to analyze pharmacokinetic parameters. RESULTS： The pharmacokinetics of quetiapine fumarate was in line with two-compartment model. Main pharmacokinetic parameters were as follows： t1/2α （20.132 ± 1.198） min; t1/2β （62.883 ± 11.120） min; tmax （40.00 ± 8.66） min; cmax （2.21 ± 0.066） μg/ml; AUC024 h （687.453 ± 12.026） mg.min/L; V1/F （8.244 ± 0.679） L/kg; K10 （0.183± 0.028） min^-1; K12 （1.764 ± 0.161） min^-1; K21 （0.189 ± 0.018） min^-1. CONCLUSIONS： Quetiapine fumarate is distributed and eliminated rapidly, but isn＇t widely distributed.

关 键 词：富马酸喹硫平 反相高效液相色谱法 药动学 大鼠 

分 类 号：R965[医药卫生—药理学]