陈伟,孟令阔,樊冬娇,唐星
CHEN Wei,MENG Ling-kuo,FAN Dong-jiao,TANG Xing(School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的研究盐酸小檗碱胶囊单次和多次给药后在Beagle犬体内的药动学。方法 6条Beagle犬按150 mg单次和多次口服盐酸小檗碱胶囊,多次给药每天1次,共7 d。采用UPLC-MS/MS色谱法测定犬血浆中盐酸小檗碱的浓度。用DAS 2.0药动学软件处理血药浓度数据。用SPSS统计软件对所得的药动学数据进行显著性差异分析。结果单次给药后主要药动学参数t1/2为(18.85±10.54)h,ρmax为(4.18±2.59)μg.L-1,AUC0-t为(110.04±70.22)μg.h.L-1,AUC0-∞为(121.51±74.19)μg.h.L-1,CL为(1 593.57±745.01)L.h-1,V为(44 509.1±34 995.4)L,tmax为(20.42±22.98)h;多次给药达稳态后主要药动学参数t1/2为(18.53±9.99)h,ρmax为(9.92±7.01)μg.L-1,AUC0-t为(164.51±119.70)μg.h.L-1,AUC0-∞为(172.34±125.03)μg.h.L-1,CL为(1 280.19±709.95)L.h-1,V为(33 655.7±27 632.2)L,tmax为(6.08±4.90)h。结论盐酸小檗碱单次和多次给药后在Beagle犬体内血药浓度均较低,盐酸小檗碱多次给药在Beagle犬体内无明显蓄积现象。
Objective To study the pharmacokinetics of berberine chloride after oral administration a single and multiple dose.Methods The pharmacokinetics was studied after single and multiple oral dose of 150 mg of berberine chloride in 6 Beagle dogs.The multiple dose regimen interval was 24 h for 7 d.The UPLC-MS/MS method was used to determine the berberine dog plasma concentrations.Pharmacokinetic parameters were obtained by the drug and statistics(DAS)version 2.0 software.Differences in pharmacokinetics were analyzed by the Student′s t-test using SPSS statistics software.Results The main pharmacokinetic parameters of berberine after a single dose were as follows:t1/2 was(18.85±10.54)h,ρmax was(4.18±2.59)μg · L-1,AUC0-t was(110.04±70.22)μg · h · L-1,AUC0-∞ was(121.51±74.19)μg · h · L-1,CL was(1 593.57±745.01)L · h-1,V was(44 509.1±34 995.4)L,tmax was(20.42±22.98)h;The main pharmacokinetic parameters of berberine after multiple dose were as follows:t1/2 was(18.53±9.99)h,ρmax was(9.92±7.01)μg · L-1,AUC0-t was(164.51±119.70)μg · h · L-1,AUC0-∞ was(172.34±125.03)μg · h · L-1,CL was(1280.19±709.95)L · h-1,V was(33 655.7±27 632.2)L,tmax was(6.08±4.90)h.Conclusions Berberine dog plasma concentrations are very low both after single and multiple dose.No accumulation of drug was found after repeated administration of berberine chloride.

关键词(KeyWords)： 盐酸小檗碱;单次和多次给药;药动学;UPLC-MS/MS色谱法
berberine chloride;single and multiple dose;pharmacokinetics;UPLC-MS/MS method

Abstract:

Keywords:

基金项目(Foundation):

作者(Author): 陈伟,孟令阔,樊冬娇,唐星
CHEN Wei,MENG Ling-kuo,FAN Dong-jiao,TANG Xing(School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2011.07.012

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