HPLC-MS/MS法测定犬体内盐酸苯环壬酯的血药浓度及其药动学研究  

Plasma Concentration of Phencynonate Hydrochloride in Dogs by HPLC-MS/MS and Its Pharmacokinetic Study

作　　者：曾媛[1,2] 郑露露[1,2] 熊磊[1] 刘辉[1] 段婷[2] 

机构地区：[1]广州军区武汉总医院药剂科,武汉430070 [2]湖北中医药大学药学院,武汉430065

出　　处：《中国药房》2015年第28期3912-3915,共4页China Pharmacy

基　　金：国家"十二五"科技重大专项课题(No.2013ZX09J13109-05C)

摘　　要：目的：测定犬体内盐酸苯环壬酯的血药浓度，计算药动学参数。方法：取Beagle犬6只，分别ig盐酸苯环壬酯片2 mg和4 mg，于给药前5 min和给药后0.17、0.25、0.5、0.75、1.0、1.25、1.5、2、3、4、6、8、10、12、14、16、18、24、36 h时各取血2 ml，采用高效液相色谱-质谱联用法，以盐酸戊乙奎醚为内标，测定盐酸苯环壬酯的血药浓度；2周后交叉给药，同法测定。利用DAS2.0软件计算药动学参数。结果：盐酸苯环壬酯检测质量浓度的线性范围为0.1～15 ng/ml（r＝0.9996），定量限为0.1 ng/ml，方法回收率为97.30％～103.20％，提取回收率为52.30％～60.11％，RSD均小于11％（n＝5）；低、高剂量的药动学参数t1/2α分别为（0.678±0.525）、（0.405±0.465）h，tmax分别为（1.042±0.401）、（0.900±0.418）h，cmax分别为（14.063±6.29）、（31.580±9.673）mg/L，AUC0-36 h分别为（48.186±14.776）、（79.269±34.649）mg·h/L。结论：本法操作简单、灵敏度高、专属性强，可用于盐酸苯环壬酯在犬体内的药动学研究。OBJECTIVE：To determine the plasma concentration of Phencynonate hydrochloride（PCH）in dogs,and to calcu-late pharmacokinetic parameters. METHODS：6 Beagle dogs were given PCH tablets（2 mg and 4 mg）intragastrically. The blood samples were collected 5 min before medication and 0.17,0.25,0.5,0.75,1.0,1.25,1.5,2,3,4,6,8,10,12,14,16,18, 24 and 36 h after medication,2 ml each time. Using penehyclidine hydrochloride as internal standard,HPLC-MS/MS method was adopted to determine the plasma concentration of PCH. The medication plans were interchanged 2 weeks later. The pharmacokinetic parameters were calculated using DAS 2.0 software. RESULTS：The linear range of PCH was 0.1-15 ng/ml（r=0.999 6）;the low-est limit of quantification was 0.1 ng/ml;the methodology recovery were 97.30%-103.20%;the extraction recovery were 52.30%-60.11%（RSD〈11%,n=5）. The main pharmacokinetic parameters of low and high doses were as follows as t1/2α of （0.678±0.525）and（0.405±0.465）h,tmax of（1.042±0.401）and（0.900±0.418）h,cmax of（14.063±6.29）and（31.580±9.673） mg/L,AUC0-36 h of（48.186±14.776）and（79.269±34.649）mg＆#183;h/L. CONCLUSIONS：The method is simple,sensitive and speci-fic,and can be used for pharmacokinetic study of PCH in dogs.

关 键 词：盐酸苯环壬酯 盐酸戊乙奎醚 高效液相色谱-质谱联用法 BEAGLE犬 

分 类 号：R965[医药卫生—药理学]