海星甾醇琥珀酸酯(A1998)脂肪乳静脉给药后在大鼠体内的组织分布  

Tissue distribution of 3-hydroxyandrost 5-en-17-one succinate (A1998) intralipid after the intravenous injection in rats

作　　者：张天宇[1] 章国良[1] 步秀云[1] 王昕[1] 楼雅卿[1] 

机构地区：[1]北京大学基础医学院药理系,北京100083

出　　处：《中国新药杂志》2005年第12期1414-1417,共4页Chinese Journal of New Drugs

摘　　要：目的:研究海星甾醇琥珀酸酯(3β-羟基雄甾-5烯-17酮琥珀酸酯,A1998)脂肪乳经静脉给药后在大鼠体内的组织分布经时变化规律。方法:大鼠单次静脉注射20 mg.kg-1A1998脂肪乳后,分别于不同时间点剖取各组织脏器,采用HPLC柱前衍生法测定大鼠各组织脏器药物含量。结果:A1998在大鼠体内主要分布于肺、肝、脾等器官,给药后15 min,测得肺脏药物含量最高(32.73±3.87)μg.g-1,脾脏(23.47±8.04)μg.g-1及肝脏(14.87±1.63)μg.g-1次之,均远高于同时间点大鼠血药浓度。A1998在上述3脏器中药物浓度维持时间亦久,至给药36 h后仍能检测出较高浓度,分别为(4.37±2.74),(4.69±2.37)及(8.30±5.96)μg.g-1。静注A1998后心脏及肾脏中药物浓度的经时变化与同时间点血药浓度相似。在胃、小肠、子宫、卵巢、体脂中未检测到药物分布。结论:大鼠单次静脉注射20 mg.kg-1A1998脂肪乳后,药物在血浆中消除迅速,并快速分布于各组织。A1998在大鼠体内的组织分布具有较强的选择性,各组织中药物浓度经时变化结果提示对肺、肝、脾等脏器具有高度的亲和力。Objective： To assess the tissue distribution of 3/^-hydroxyandrost-5-ene-17-one succinate （A1998） intralipid after iv administration to rats. Methods：After single iv administration of A1998 intralipid 20 mg·kg^-1, rats were euthanized at certain prescheduled timepoints to collect reated rat tissues for the determination of the A1998 concentration-time curve by a pre-column derivation HPLC. Results： The A1998 was mainly distributed in rats＇ lung, spleen and liver. Compared with the concentration-time curve in the plasma, heart and kidney tissues, the lung, spleen and liver tissues of rats showed significantly higher A1998 concentrations after 15 minutes of iv administration, i.e., （32.73 ± 3.87）, （23.47 ± 8.04） and （14.87 ±1.63） μg·g^-1, respectively, and longer sustenance of the A1998 concentration after 36 hours of the iv administration [（4.37 ± 2.74）, （4.69 ± 2.37） and （8.30 ± 5.96）μg·g^-1 , respectively]. No A1998 concentrations were detected in rats＇stomach, small intestinal, ovarian, uterine and body fat tissues. Conclusion： The A1998 was rapidly distributed into tissues from the plasma in terms of highly selective affinity to lung, live and spleen tissues.

关 键 词：海星甾醇琥珀酸酯(3β-羟基雄甾-5烯-17酮琥珀酸酯 A1998) 大鼠 组织分布 HPLC柱前衍生法 

分 类 号：R969.1[医药卫生—药理学] R972.2[医药卫生—药学]