[^3H]-乙酰紫草素在小鼠体内的组织分布、排泄及血中分布研究  

Tissue distribution,excretion and blood distribution of [~3H]-acetylshikonin in mice by Sample Oxidizer

作　　者：孙东晓[1] 田慧芳[1] 孟志云[1] 周佳雨[1] 丁建刚[1] 吴广瑞[1] 窦桂芳[1] 

机构地区：[1]军事医学科学院野战输血研究所,北京100850

出　　处：《军事医学科学院院刊》2008年第4期348-352,共5页Bulletin of the Academy of Military Medical Sciences

摘　　要：目的:用氧化燃烧炉样品预处理技术研究[3H]-乙酰紫草素在小鼠体内的组织分布、排泄和血中分布。方法:小鼠单次灌服[3H]-乙酰紫草素后,收集组织、血、尿和粪样,氧化燃烧炉法进行样品预处理,液闪计数仪测定放射性水平。结果:小鼠单次灌胃给[3H]-乙酰紫草素(120 mg/kg,2.96×107Bq/kg)后,放射性主要分布在胃、肠,其次是胆囊、肝、肾、肺,脑和脊髓分布较少。271 h后从粪中收集到给药剂量的(68.5±3.3)%,尿中收集到(17.6±3.1)%,粪尿合计(86.1±5.5)%。另对乙酰紫草素在血中存在形式、血细胞和血浆中的分配比例以及与血浆蛋白结合的形式、结合率进行了探索性研究。结论:乙酰紫草素吸收较差;组织分布广泛;排泄较完全;1 h血样中没有检测到原形;血浆、血细胞药物含量分配比约为4∶1;人血浆蛋白结合率高;血浆蛋白的结合为共价和疏水作用两种形式并存。Objective ：To study the tissue distribution, excretion and blood distribution of [ ^3H ]-acetylshikonin in mice by Sample Oxidizer pretreatment technology. Methods： After 0.5% carboxymethyl cellulose suspension containing [ ^3 H]- acetylshikonin was administered by gastric gavage at the dose of 120 mg/kg（2.96 × 10^7 Bq/kg）, the tissue, feces, urine and blood samples of the mice were collected. The samples were pretreated by Sample Oxidizer. The radioactivity was determined by Liquid Scintillation Analyzer Tri-Card 29007R. Results： After oral administration of [^3H ]-acetylshikonin 120 mg/kg with 2.96 × 10^7 Bq/kg to mice, [ ^3H]-acetylshikonin was mainly distributed in the stomach and intestine, secondarily in the gallbladder, liver, kidneys, lungs, and least in the brain and spinal cord. The cumulative radioactivity rate of the feces and urine was （ 68.5 ± 3.3 ） % and （ 17.6 ± 3.1 ） % within 271 h, respectively. The total excretion rate was （ 86.1 ± 5.5 ） %. Besides, the exploratory study was carried out on acetylshikonin the existing form of in blood, allocation in plasma and blood cells, binding mode and binding rates of plasma proteins. Conclusions ： Acetylshikonin has a relatively low absorption rate and wide distribution in mice, and is excreted completely more by fecal route than by urine. Acetylshikonin exits as a binding form in mouse blood. Allocation of acetylshikonin in mouse plasma and blood cells is nearly 4： 1. Plasma protein binding rates of three levels（ high, medium and low） are （94.7±0.44）% , （94.7 ±0. 29）% and （95.4± 0.13 ）% , respectively. The binding between acetylshikonin and human plasma protein is the coexistence of covalent bonding and hydrophobic interaction.

关 键 词：[^3H]-乙酰紫草素 氧化燃烧炉 组织分布 排泄 蛋白结合 血中分布 

分 类 号：R285[医药卫生—中药学]