参麦注射液活性成分在正常和心肌缺血Beagle犬体内的药动学研究
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篇名: 参麦注射液活性成分在正常和心肌缺血Beagle犬体内的药动学研究
TITLE:
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1 h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,WinNonlin 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t1/2为(2.69±1.12) h,AUC0-24 h为(2 060.78±812.18) h·μg/L,Vz为(46.16±20.98) ml,CL为(9.02±4.45) ml/h;与正常组比较,AUC0-24 h显著升高,Vz、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Rg1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Rg1药动学过程无明显影响。
ABSTRACT: 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 isoproterenol 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 Rg1 and 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, AUC0-24 h was (2 060.78±812.18) h·μg/L, Vz was (46.16±20.98) ml and CL was (9.02±4.45) ml/h; compared to the normal control group, AUC0-24 h 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). CONCLUSIONS: Myocardial ischemia may affect the removal of ginsenoside Re in Beagle dogs, but has no effect on the pharmacokinetic process of ginsenoside Rg1.
期刊: 2016年第27卷第25期
作者: 唐思,杨瑞,张世良,董晓茜,李国信,夏素霞,朱婉玲
AUTHORS: TANG Si,YANG Rui,ZHANG Shiliang,DONG Xiaoqian,LI Guoxin,XIA Suxia,ZHU Wanling
关键字: 参麦注射液;心肌缺血模型;人参皂苷Rg1;人参皂苷Re;Beagle犬;药动学
KEYWORDS: Shenmai injection; Myocardial ischemia model; Ginsenoside Rg1; Ginsenoside Re; Beagle dogs; Pharmacokinetics
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