摘要
目的研究苯酚类螯合剂８１０２在大鼠体内的药代动力学。方法采用液体闪烁计数技术测量３Ｈ－８１０２在血液、组织、尿和粪中的放射性强度。结果大鼠肌注８１０２（２０、５０、１００ｍｇ／ｋｇ）后，其体内血药浓度－时间曲线符合二室开放模型，而静注８１０２（５０ｍｇ／ｋｇ）其药－时曲线符合三室模型。肌注和静注８１０２其分布相Ｔ１／２α分别为０．５和０．５５ｈ，消除相Ｔ１／２β分别为７４．２３和３６．３１ｈ。大鼠肌注８１０２（５０ｍｇ／ｋｇ）后，组织中的药物浓度，以肾浓度最高，肺、肝、脾次之。２４ｈ内尿、粪排泄量分别为注入量的７６．５％和０．８％。８１０２和血浆蛋白的结合率为３６．５％～４６．８％。结论８１０２进入体内后能快速分布和排泄，且具有组织分布选择性，均有利于加快体内核素的排除。
Purpose To study the pharmacokinetics of
phenolic chelating agent8102 in rats. Methods The amount of 3H8102 was measured by
liquid scintillation counting method. Results It was found that the characteristic of the plasm
drug concentration time curve fit a two compartment model after im injection of 3H 8102 to
rats and conforme to a three compartment model after iv injection.The half life time was 0.50
and 0.55h respectively for the distribution phase with im and iv injection. T 1/2β was
74.23 and 36.31h respectively for the elemination phase with im and iv injection.Drug
accumulation was the highest in the kidney,and the sencond in lung,live and spleen within 60
min after im injection.8102 excreted in urine and feces within 24h was 76.5% and 0.8%
respectively.The binding percentage of 8102 to plasm protein was 36.5%～46.8%. Conclusions
8102 quickly distributed to tissues and excreted in urine.It is accumulated selectively in the
tissues favourable to excretion of the radionuclide.
出处
《上海医科大学学报》
CSCD
1999年第2期103-105,112,共4页
Journal of Fudan University(Medical Science)
