注射用益气复脉(冻干)对非洛地平在大鼠体内药动学的影响  

Effects of Yiqi Fumai for Injection(Lyophilized)on Pharmacokinetics of Felodipine in Rats

作　　者：胡冰[1,2] 岳洁皓[2] 段超慧[2] 叶正良[1] 周大铮[1] 李德坤[1] 马英丽[2] 

机构地区：[1]天津天士力之骄药业有限公司,天津300410 [2]黑龙江中医药大学药学院,哈尔滨150040

出　　处：《中国药房》2012年第45期4230-4232,共3页China Pharmacy

基　　金："重大新药创制"科技重大专项(2010ZX09502-004)

摘　　要：目的:考察注射用益气复脉(冻干)(YQFM)对非洛地平在大鼠体内药动学的影响。方法:将大鼠分为高、中、低剂量(1625、542、181mg·kg-1)YQFM组和空白对照(生理盐水)组,每组10只,尾静脉连续注射给药8d,第8天给药后各组均立即灌胃给予非洛地平0.5mg.kg-1,灌胃后0、0.5、0.75、1、2、2.5、3、3.5、4、5、8、12、24、48h于眼底静脉丛取血,以液质联用检测非洛地平在各组大鼠血浆中的浓度,利用TopFit2.0软件拟合并计算其药动学参数。结果:空白对照组和高、中、低剂量YQFM组非洛地平的药动学参数分别为:cmax为(50.67±8.99)、(37.78±7.74)、(40.31±6.03)、(45.24±8.03)μg·L-1,AUC0～48h为(532.21±102.15)、(395.75±85.85)、(424.80±77.53)、(489.87±94.81)μg.h.L-1,t1/2为(17.47±4.31)、(17.04±3.20)、(16.75±4.04)、(16.59±3.52)h,CL为(0.19±0.04)、(0.27±0.03)、(0.26±0.03)、(0.22±0.04)L·h-1;非洛地平药动学参数符合一室模型,与空白对照组比较,中、高剂量YQFM组cmax、AUC0～48h明显减小,CL明显增加(P<0.05或P<0.01),3个剂量YQFM组间药动学参数差异无统计学意义(P>0.05)。结论:YQFM高、中剂量能明显加快非洛地平在大鼠体内的代谢和清除。OBJECTIVE：To investigate the effect of Yiqi fumai（YQFM）for injection（lyophilized）on the pharmacokinetics of felodipine in rats.METHODS：Rats were divided into high-dose,medium-dose and low-dose YQFM groups（1 625,542 and 181 mg.kg-1）and blank control group（normal saline）with 10 rats in each group.They were given medicine via the caudal vein for consecutive 8 d,and were lavaged felodipine 0.5 mg·kg-1 immediately after medication on 8th day.The blood samples were collected via the retinal vein plexus 0,0.5,0.75,1,2,2.5,3,3.5,4,5,8,12,24 and 48 h after,i.g.administration.LC-MS method was used to detect the plasma concentration of felodipine in rats,and the TopFit software was used to calculate its pharmacokinetic parameters.RESULTS：Pharmacokinetics parameters of blank control group,high-dose,midium-dose and low-dose YQFM groups were as follow：c max：（50.67±8.99）,（37.78±7.74）,（40.31±6.03）and（45.24±8.03）μg·L-1 ;AUC 0～48 h：（532.21±102.15）,（395.75±85.85）,（424.80±77.53）and（489.87±94.81）μg·h·L-1 ;t 1/2：（17.47±4.31）,（17.04±3.20）,（16.75±4.04）,（16.59± 3.52）h;CL：（0.19±0.04）,（0.27±0.03）,（0.26±0.03）and（0.22±0.04）L.h-1.Pharmacokinetics parameters of felodipine were in line with one-compartment model.Compared with blank control group,c max and AUC 0～48 h of medium-dose and high-dose YQFM groups decreased significantly,while CL increased significantly（P0.05 or P0.01）.There was no significant difference of pharmacokinetics parameters among YQFM groups（P0.05）.CONCLUSION：The high-dose and medium-dose of YQFM may promote metabolism and clearance of felodipine in rats.

关 键 词：注射用益气复脉(冻干) 非洛地平 大鼠 药动学 液质联用 

分 类 号：R965[医药卫生—药理学]