~3H-茯苓素在大鼠体内的药代动力学研究  

PHARMACOKINETICS AND METABOLIC FATE OF ~3H-PORIATIN IN RATS

作　　者：张晶[1] 马瑜[1] 许津[1] 

机构地区：[1]中国医学科学院医药生物技术研究所,北京100050

出　　处：《中国抗生素杂志》1993年第2期149-153,共5页Chinese Journal of Antibiotics

摘　　要：本实验采用薄层层析与液体闪烁计数相结合的方法测定大鼠血液中同位素标记茯苓素浓度,该方法可将血液中原药与其它放射性物质相分离。静注(50mg/kg)后体内过程属于二房室模型,其主要参数:吸收相半衰期为0.323小时、消除相半衰期为1.443小时。口服给药达峰时间为1.214小时,峰浓度为5.149μg/ml,吸收速率常数0.779h^(-1),消除速率常数为0.592h^(-1)。肾脏为主要排泄器官,占全部放射剂量的56.72％,粪便排泄占33.10％,24小时内胆汁排泄占所给剂量的6.86％。通过胆管引流实验证明,茯苓素在动物体内存在肠肝循环,静注后组织中的放射剂量以肝、肾、肺含量最高。Poriatin is the physiologically active constituent of por-ia, a traditional Chinese herb,and consists of a group of tetracyclo trit- erpenes. The metabolism, and pharmacokinetics of ~3H-labeled poriatin in rats were studied in the experiments by iv and po administration routes. After oral single dose of ~3H-poriatin (50mg/kg) the PK constants were estimated: Tp=1.214h, Cp=5.149μg/ml, Ka=0.779h^(-1) Ke = 0.592h^(-1). In the experiment of adminstration by iv route, the data fitted to a two compartment open pharmacokinetic model, t_(1/2)= 0.32h, t_(1/2)=1.443h, V = 0.744 (mg·kg)/(μg/ml),CL= 0.743 (μg·kg)/h/(μg/ml).Tissue distribution of radioactivity for ~3H-poriatin was determined after 10min, 1h and 8h. The high level was found in the liver, kindney and lung. The bile of rats was continually collected through a biliary cannula for 24h.The amount of ~3H -poriatin excreted into the bile was about 6.3 percent of given dose. Enterhepatlc cycle of ~3H-poriatin in rats was demonstrated with two rats (A and B) linked by biliary cannula.About 56,7% of ~3H-poriatin excreted in urine and 33.1% in feces by rats during period of 5 days.P-arent drug and its metabolites in blood, urine and feces were seperated by TLC and determined by liquid scintillation.

关 键 词：茯苓素 药代动力学 茯苓 大鼠 

分 类 号：R282.710.5[医药卫生—中药学]