二硫卡钠在小鼠体内的药代动力学和分布及在大鼠体内的排泄  

PHARMACOKINETICS AND DISTRIBUTION OF DITIOCARB SODIUM IN MOUSE AND ITS EXCRETION IN RAT AFTER INTRAVENOUS ADMINISTRATION

作　　者：陶学斌[1] 李万亥[1] 陈洁[1] 谈冶雄[1] 

机构地区：[1]第二军医大学药学院中西药研究室,上海200433

出　　处：《解放军药学学报》1997年第1期14-18,共5页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：本文研究了小鼠iv DTC100 mg·kg^(-1)的体内药代动力学和组织分布特征及大鼠iv DTC50mg·kg^(-1)的排泄情况。DTC及其代谢产物DTC-Me的药-时曲线分别符合二室开放式和一室线性动力学模型。DTC的主要药代动力学参数为:T_(1/2α)=3.07min;T_(1/2β)=9.0min;CL_b=0.053L·kg^(-1)·min^(-1);V_b=0.69L·kg^(-1)。DTC-Me体内滞留时间稍长,T_(1/2β)=21.6min。给药后5min,所有被考察的组织器官中均发现DTC,且达峰浓度,1.5h后降至检测限以下。脂肪,肌肉DTC分别于20,30min达峰,可检测时间分别长达7和4h。给药大鼠的粪便中未发现DTC或DTC-Me,尿液中也仅检测到DTC。累积尿药排泄量仅占给药剂量的0.89±0.03％。The pharmacokinetics and distribution of ditiocarb sodium intravenously injected with l00mg·kg-1 of DTC (DTC) in mice were studied. The excretion in rats after iv administra-tion of 50mg·kg-1 of DTC was also investigated. The concentration-time curves of DTC and its main metabolite methyl ester (DTC-Me) fitted an open two-compartment and a one-compartment kinetic model respectively. The main pharmacokinetic parameters were as followed: T1/2a=3. 07min, T1/2β=9.0min,Vb=0.69L·kg-1,and CLb=0. 053·kg-1·min-1 for DTC and T11/2β=21. 6min for DTC-Me. Both DTC and DTC-Me peaked at 20 and 30min in lipid and muscle re-spectively, but peaked within 5min in other tissues and organs investigated. The detectable times of DTC in muscle and lipid were 4 and 7h respectively, but those in other tissues were no more than 1.5h. DTC administered to rats rapidly appeared in urine, but it could not be detected in urine 12h after dosing during the whole observation. DTC-Me could not be found in urine or fe-ces. Only 0.89±0.03% of dose was recovered from urine as unchanged DTC.

关 键 词：二硫卡钠 药代动力学 分布 排泄 高压液相色谱 

分 类 号：R96[医药卫生—药理学]