人参四逆注射剂在大鼠及小鼠体内的药物动力学  

Pharmacokinetics of Renshensini injection in mice and rats

作　　者：赵镭[1] 柳玉石[1] 杨昊[1] 唐星[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2008年第7期524-529,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的通过药物累积法研究人参四逆注射剂在小鼠体内药物动力学过程,与大鼠体内血样质量浓度法测定结果进行比较。方法将人参四逆汤剂中四味药材分别精制成提取物,按照一定顺序混合,制备人参四逆注射剂。采用药物累积法,以小鼠急性死亡率为指标,测定药物动力学参数。以甘草酸为指标性成分,采用血药浓度法考察复方制剂中甘草酸在大鼠体内的药动学行为。结果人参四逆注射剂在小鼠和大鼠体内的药动学参数分别是：ke为0.44 h^-1和0.59 h^-1,t1/2为1.57 h和1.25 h,AUC0-t为2267.59μg.h和728.11 mg·h·L^-1,Vss为9.20 mL和13.28 mL,CL为6.15 h^-1和6.90 mL·h^-1。药物在小鼠体内的体存量随时间间隔增加而显著降低,间隔时间为1 h时,体存量存在反跳点,大鼠体内血样的质量浓度在1.5～2 h时存在同样的跳点。结论人参四逆注射剂在小鼠和大鼠体内药物动力学模型均为二室模型,体内分布、消除速度快。血样质量浓度法与药物累积法测定结果具有一定相关性,相互补充说明复方制剂配伍后的整体疗效。Objective To study the pharmacokinetics of compound preparation Renshensini （traditional Chinese medicine）injection in mice with drug accumulation method （DAM）, and compare the result with that from blood drug level method （BDLM）in rats. Methods Renshensini injection was prepared with the four refine extracts, which were refined from the herbal material and combined in a certain sequence. Pharmacokinetic parameters were determined with DAM, taking the mortality of mice as index. Pharmacokinetics of compound preparation was studied based on the GA in rats. Results The pharmacokinetic parameters of Renshensini injection determined by DAM and BDLM were as follows： k e was 0.44 h^-1 and 0.59 h^-1 ; t 1/2 was 1.57 h and 1.25 h;AUC0→t was 2 267.59 μg·h and 728.11 （mg·h）·L^-1; Vss was 9.20 mL and 13.28 mL;CL was 6.15 mL·h^-1 and 6.90 mL·h^-1. The residue drug in the mice decreased significantly with the increase of interval time. However the rudimentary drug existed jump-point in one hour during administration, the same phenomenon occurred in the BDLM. Conclusions The pharmacokinetics of Renshensini injection in mice and rats after i. v. fits with two-compartment model. It distributes rapidly after entry into the body, and is also eliminated quickly from the plasma. DAM and BDLM additionally demonstrate the whole curative effect of compound preparation and provide actual value in clinical practice.

关 键 词：人参四逆注射剂 药物累积法 血药浓度法 药物动力学 

分 类 号：R94[医药卫生—药剂学]