不同剂量二硫卡钠在小鼠体内的药动学  

Pharmacokinetics of ditiocarb sodium in mice after intravenous administration of various doses

作　　者：陶学斌[1,2] 李万亥[1,2] 陈幸福 

机构地区：[1]第二军医大学药学院中西药研究室 [2]解放军八五医院药械科

出　　处：《中国药学杂志》1997年第12期758-760,共3页Chinese Pharmaceutical Journal

摘　　要：目的：研究小鼠分别ｉｖ不同剂量的二硫卡钠（ＤＴＣ）后，ＤＴＣ及其甲酯（ＤＴＣＭｅ）体内药动学特征。方法：小鼠分别ｉｖＤＴＣ２５，５０，１００ｍｇ·ｋｇ－１后，于各时间点摘眼球获取血浆。用柱切换高压液相色谱法分别测定ＤＴＣ及ＤＴＣＭｅ的浓度，所得血药浓度时间数据用ＭＣＰＫＰ药动学软件处理，求得药动学参数。结果：ＤＴＣ药时曲线均符合二室开放模型，ｔ１／２α分别为（１．３６±０．１１）ｍｉｎ、（３．０±０．５）ｍｉｎ、（３．１±０．６）ｍｉｎ；ｔ１／２β分别为（１７．２±２．３）ｍｉｎ、（１１±３）ｍｉｎ、（９．１±０．９）ｍｉｎ；ＣＬｂ分别为（０．１０６±０．０１７）Ｌ·ｋｇ－１·ｍｉｎ－１、（０．１０４±０．０２４）Ｌ·ｋｇ－１·ｍｉｎ－１、（０．０５３±０．０２１）Ｌ·ｋｇ－１·ｍｉｎ－１；ＡＵＣ分别为（２３５±１８）μｇ·ｍｉｎ·ｍｌ－１、（４８０±７９）μｇ·ｍｉｎ·ｍｌ－１、（１１８４±１０７）μｇ·ｍｉｎ·ｍｌ－１。ＤＴＣＭｅ均符合一室线性动力学模型，ｔ１／２β分别为（１４１±２１）ｍｉｎ、（３０±５）ｍｉｎ、（２２±３２）ｍｉｎ；ｔ１／２Ｋａ分别为（８．５±０．９）ｍｉｎ、（４．３±０．?OBJECTIVE: To investigate the pharmacokinetics of ditiocarb sodium (DTC) and its Smethyl ester (DTCMe) in mice after intravenous injection with DTC. METHODS: Plasma was collected from mice by pick of eyeball, which has been intravenously injected with DTC 25,50,100 mg·kg-1, respectively. The concentration of DTC and DTCMe were determined by columnswitching high performance liquid chromatography, and the date were analysed with the programe of MCPKP on computer to get the pharmacokinetic parameters. RESULTS: The concentrationtime curves of DTC and DTCMe fitted an open twocompartment and a onecompartment kinetic model, respectively. The main pharmacokinetic parameters of DTC after iv DTC 25, 50, 100 mg·kg-1 were as follows: t1/2α was (1.36±0.11)min, (3.0±0.5)min, (3.1±0.6)min; t1/2β was (17.2±2.3)min, (11±3)min, (9.1±0.9)min; CLb was (0.106±0.017)L·kg-1·min-1, (0.104±0.024)L·kg-1·min-1, (0.053±0.021)L·kg-1·min-1; and AUC was (235±18)μg·min·ml-1, (480±79)μg·min·ml-1, (1 184±107)μg·min·ml-1, reslpectively.t1/2β of DTCMe was (141±21)min, (30±5)min, (22±32)min; and t1/2Ka of DTCMe was (8.5±0.9)min, (4.3±0.8)min, (1.3±0.4)min for 25, 50, and 100 mg·kg-1, respectively. CONCLUSION: The distribution and elimination of either DTC or DTCMe were rapid, and their pharmacokinetics were linear.

关 键 词：二硫卡钠 药物动力学 剂量 

分 类 号：R979.5[医药卫生—药品]