恩其明醋酸盐的药代动力学研究  

Pharmacokinetics of ungeremine acetate in rats

作　　者：梁罡[1] 徐永平[1] 胥彬[1] 

机构地区：[1]中国科学院上海药物研究所

出　　处：《中国药理学通报》1997年第1期30-32,共3页Chinese Pharmacological Bulletin

基　　金：中国科学院八.五重大课题

摘　　要：目的：研究恩其明醋酸盐（ＡＴ１８４０）在大鼠体内的药代动力学。方法：荧光检测法。结果：大鼠静注后，其体内的血药浓度－时间曲线符合二室开放模型。其分布相Ｔ１２α为０．５７ｍｉｎ，消除相Ｔ１２β为５．５１ｍｉｎ。大鼠ｉｖＡＴ１８４０后，组织中的药物浓度，以肺、肾浓度最高，肝、卵巢、心、脾、胃次之，肌肉、脂肪、脑中最低。尿中排泄量２４ｈ内占总给药量的２３．２８％；胆汁和粪中分别约为给药量的３６．４６％和１．７９％。ＡＴ１８４０与血浆蛋白的结合率６８．５％～７３．９％。结论：ＡＴ１８４０是一个血浆半衰期短，并有组织分布选择性的药物。AIM: To investigate the pharmacokinetic of ungeremine acetate (AT1840) in rats. METHODS: AT1840 was detected by fluorescence method. RESULTS: It was found that the characteristics of the plasm drug concentration time curve fit the two compatrtment model after iv injection of this drug to rats. The half life time was 0 57 min for distribution phase and 5 51 min for elemination phase. Drug accumulation was highest in lung, kidney, second in liver, ovary, heart, spleen, stomach, and lowest in muscle, fat and brain. AT1840 excreted in urine, bile and faces within 24 h was 23 28%, 36 46% and 1 79% of the tolal dose administered, respectively. The binding percentage of AT1840 to plasm protein was 68 5%￣73 9%. CONCLUSION: AT1840 had short half life time and distributed in tissues selectively.

关 键 词：恩其明醋酸盐 药代动力学 抗癌药 

分 类 号：R979.1[医药卫生—药品] R969.1[医药卫生—药学]