摘要
目的:研究人工合成胸腺素α1(sTα1)静脉注射或皮下注射在小鼠和大鼠体内的药动学特征。方法:取小鼠45只(sTα1,1mg·kg-1)、大鼠3只(sTα1,0.5mg·kg-1),尾静脉注射相应药物,分别于注射前及注射后6h内小鼠眼眶静脉采血和大鼠心脏采血;另取小鼠180只,随机分为高、中、低(sTα1,5、1、0.32mg·kg-1)剂量组,取大鼠9只,随机分为高、中、低(sTα1,2.5、0.5、0.16mg·kg-1)剂量组,皮下注射相应药物,分别于注射前及注射后10h内小鼠眼眶静脉采血和大鼠心脏采血,用酶联免疫吸附法检测各时间点的血药浓度,并计算其药动学参数。结果:sTα1静脉注射在小鼠体内的t1/2β为0.68h、AUC0～∞为554.32μg·h·L-1,在大鼠体内的t1/2β为(1.87±0.50)h、AUC0～∞为(1602.91±360.41)μg·h·L-1;sTα1高、中、低剂量组皮下注射在小鼠体内的t1/2分别为0.76、0.54、0.268h,AUC0～∞分别为3222.95、417.67、366.60μg·h·L-1,在大鼠体内的t1/2分别为(1.23±0.23)、(1.40±0.37)、(1.99±0.94)h,AUC0～∞分别为(22436.74±5641.94)、(1539.63±203.30)、(729.60±320.0)μg·h·L-1。结论:sTα1在大鼠和小鼠体内静脉注射的药动学过程属于一级二室开放模型,皮下注射的药动学过程属于一级一室开放模型。
OBJECTIVE：To study pharmacokinetic property of synthetic thymosin α1（sTα1） in mice and rats with intravenous（i.v.） and subcutaneous（s.c.） administration. METHODS：45 mice（sTα1,1 mg·kg-1） and 3 rats（sTα1,0.5 mg·kg-1） were given relevant medicine via tail vein. Blood samples were collected from orbit vein and heart before and within 6 h after administration. Another 180 mice were randomly divided into high-dose,medium-dose and low-dose groups（sTα1,5,1,0.32 mg·kg-1） . Another 9 rats were randomly divided into high-dose,medium-dose and low-dose groups（sTα1,2.5,0.5,0.16 mg·kg-1） . Six groups were given relevant medicine subcutaneously. Blood samples of orbit vein and heart were collected before and within 10 h after administration. ELISA was used to determine blood concentration of drugs at different time points and pharmacokinetic parameters were calculated. RESULTS：The main pharmacokinetic parameters of sTα1 in mice vs. rats after intravenous administration were as follows：t1/2β：0.68 h and AUC0～∞：554.32 μg·h·L-1;t1/2β and AUC0～∞ of sTα1 in rats after intravenous administration were（1.87±0.50） h and（1 602.91±360.41） μg·h·L-1. Pharmacokinetic parameters of sTα1 in mice in sTα1 high-dose,medium-dose and low-dose groups after subcutaneous administration were as follows：t1/2：0.76 h,0.54 h,0.268 h;AUC0～∞：3 222.95 μg·h·L-1,417.67 μg·h·L-1,366.60 μg·h·L-1,respectively. Pharmacokinetic parameters of sTα1 in rats in sTα1 high-dose,medium-dose and low-dose groups after subcutaneous administration were as follows：t1/2：（1.23±0.23） h,（1.40±0.37） h,（1.99±0.94） h;AUC0～∞：（22 436.74± 5 641.94） μg·h·L-1,（1 539.63±203.30） μg·h·L-1,（729.60±320.0） μg·h·L-1,respectively. CONCLUSION：Pharmacokinetic model of sTα1 in rats and mice with intravenous administration is first-order two-compartment model while that of sTα1 in rats and mice with subcutaneous administration is first-order one-compar
出处
《中国药房》
CAS
CSCD
北大核心
2011年第21期1935-1937,共3页
China Pharmacy
关键词
人工合成胸腺素α1
药动学
大鼠
小鼠
静脉注射
皮下注射
Synthetic thymosin α1
Pharmacokinetics
Rats
Mice
Intravenous administration
Subcutaneous administration
