摘要
目的:研究参麦注射液活性成分人参皂苷Rg1、人参皂苷Re在正常和心肌缺血Beagle犬体内的药动学。方法:取6只Beagle犬sc盐酸异丙肾上腺素(1.1 mg/kg)以复制心肌缺血模型(模型组),另取6只犬sc等体积生理盐水(2.2 ml/kg)作为对照组。两组犬分别于第1天上午8:00、下午13:00和第2天上午8:00给药。第2天给药后1 h,各组犬iv参麦注射液(1.6 ml/kg),在1h左右滴注完成。各组犬于iv开始后0、0.25、0.5、0.75、1(iv结束)、1.5、2、3、4、6、8、12、24 h取血。采用液相色谱-质谱联用法测定人参皂苷Rg1、人参皂苷Re的血药浓度,Win Nonlin 6.3软件计算药动学参数并进行比较。结果:人参皂苷Re在模型组犬体内的t_(1/2)为(2.69±1.12)h,AUC_(0-24 h)为(2 060.78±812.18)h·μg/L,V_z为(46.16±20.98)ml,CL为(9.02±4.45)ml/h;与正常组比较,AUC_(0-24 h)显著升高,V_z、CL显著降低,差异均有统计学意义(P<0.05)。而两组犬人参皂苷Rg_1的药动学参数无显著性差异(P>0.05)。结论:心肌缺血会影响Beagle犬体内人参皂苷Re的消除,对人参皂苷Rg_1药动学过程无明显影响。
OBJECTIVE： To study the pharmacokinetics of the active ingredients of Shenmai injection, including ginsenoside Rg1 and ginsenoside Re, in normal Beagle dogs and those with myocardial ischemia. METHODS： 6 Beagle dogs were given isopro- terenol hydrochloride （1.1 mg/kg） sc to establish the model of myocardial ischemia （model group）. Another 6 Beagle dogs were given isometric normal saline （2.2 ml/kg） sc as controls group. The two groups of dogs respectively received corresponding drugs sc at 8：00 am and 13：00 pm on day 1 and at 8：00 am on day 2. Each group of dogs were given Shenmai injection （1.6 ml/kg） iv 1 h after administration on day 2, and such intravenous drip lasted for about 1 h. Blood was collected from each group 0, 0.25, 0.5, 0.75, 1 （the end of iv）, 1.5, 2, 3, 4, 6, 8, 12 and 24 h from the start of iv. Liquid chromatography-mass spectrometry was adopted to determine the concentrations of ginsenoside Rgl arid ginsenoside Re in blood, and WinNonlin 6.3 was used to calculate pharmacokinetic parameters for comparison. RESULTS： For ginsenoside Re in the dogs of the model group, t1/2 was （2.69 ± 1.12） h, AUC0-24h was （2 060.78 ± 812.18） h. μg/L, V2 was （46.16 ± 20.98） ml and CL was （9.02 ± 4.45） ml/h; compared to the normal control group, AUC0-24h was much greater and Vz and CL were significantly lower, showing a statistically significant difference （P〈 0.05）. No significant difference in the pharmacokinetic parameters of ginsenoside Rg1 was shown between 2 groups（P〉0.05）. CON- CLUSIONS ： Myocardial ischemia may affect the removal of ginsenoside Re in Beagle dogs, but has no effect on the pharmacoki- netic process of ginsenoside Rg1.
出处
《中国药房》
CAS
北大核心
2016年第25期3475-3477,共3页
China Pharmacy
基金
国家科技重大专项课题(No.2012ZX09303017)
临床重点专科建设项目资助(2013年)
国家中医药管理局临床中药学重点学科(2009年)
辽宁中医药大学杏林学者青蓝工程(2013年)
