注射用BAPTA-AM脂质体在大鼠体内的组织分布和胆汁排泄  

Tissue distribution and biliary excretion of BAPTA-AM liposome for injection in rats

作　　者：郑枫[1] 刘文英[1] 魏伟[2] 

机构地区：[1]中国药科大学药物分析教研室,江苏南京210009 [2]合肥恒星医药研究所,安徽合肥230088

出　　处：《中国新药与临床杂志》2010年第11期858-862,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的研究1,2-二(2-氨基苯氧基)乙烷-N,N,N',N'-四乙酸四乙酰氧甲基酯(BAPTA-AM)脂质体注射液在大鼠体内的组织分布和胆汁排泄。方法 Sprague-Dawley大鼠24只,每组6只,每只大鼠尾静脉注射BAPTA-AM脂质体注射液3.0 mg.kg-1。给药后10 min、1.5 h、9 h各处死一组动物,采集各组织制作匀浆,测定各组织中的BAPTA-AM浓度。另一组大鼠收集给药后12 h内各时间段内胆汁,测定胆汁中的BAPTA浓度。结果大鼠静脉注射BAPTA-AM脂质体3.0 mg.kg-1后,药物在组织中浓度显著高于血浆中浓度,主要分布在肺、肝、脾和肾。大鼠静脉注射BAPTA-AM脂质体后BAPTA胆汁排泄较为缓慢,12 h后仍未达平台期。结论大鼠注射BAPTA-AM脂质体后大量分布在组织中,以水解产物BAPTA的形式排出体外。AIM To investigate the tissue distribution and biliary excretion of 1,2-bis（2-aminophenoxy）ethane-N,N,N＇,N＇-tetraacetic acid tetra（actoxymethyl ester）（BAPTA-AM）liposome in rats.METHODS Twenty-four Sprague-Dawley rats were randomly divided into four groups with six rats for each group.BAPTA-AM liposome dissolved in physiological saline was administered to different groups of rats by tail vein at a dose of 3.0 mg·kg-1.Tissue homogenates of experimental animal were made at 10 min,1.5 h and 9 h after administration.Bile samples were collected from bile cannulated rats at each interval after administration.The concentration of BAPTA-AM in rat tissue homogenates and the concentration of BAPTA in rat bile were quantified,respectively.RESULTS After i.v.injection of BAPTA-AM liposome 3.0 mg·kg-1 to rat,the parent drug concentrations in tissues were higher than those in plasma at the same time.Parent drug was mainly distributed in lung,liver,spleen and kidney.The BAPTA-AM concentrations were reduced significantly at 9 h after dosing in most tissue.After i.v.injection of BAPTA-AM liposome injection,the biliary excretion rate of BAPTA was slowly,and cumulative biliary excretion did not plateau during the 12 h collection period.CONCLUSION After intravenous injection,BAPTA-AM liposome is rapidly distributed into tissue in rat and is eliminated via biliary excretion of BAPTA.

关 键 词：-二(-氨基苯氧基)乙烷-N N N' N'-四乙酸四乙酰氧甲基酯 脂质体 大鼠 组织分布 胆汁排泄 

分 类 号：R965[医药卫生—药理学]