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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 means of sample pretreatment of oxidation combustion furnace. METHODS: The mice were fed with [3H]-acetylshikonin for a single time. Tissues, blood, urine, and fecal samples were collected. Oxidation furnace method was used for sample pretreatment. The liquid scintillation counter was used to determine the level of radioactivity. RESULTS: After a single oral administration of [3H]-acetylshikonin (120 mg/kg, 2.96 × 107 Bq/kg) to the mice, the radioactivity was mainly distributed in the stomach and intestines, followed by the gallbladder, liver, kidney, and lungs. And less distributed in the spinal cord. After 271 h, (68.5±3.3)% of the administered dose was collected from the feces, (17.6±3.1)% was collected in the urine and (86.1±5.5)% was the total of the feces. Another exploratory study was conducted on the presence of acetylshikonin in the blood, the distribution ratio of blood cells and plasma, and the form and binding rate of plasma tyrosine. Conclusion: Acetylshikonin is poorly absorbed; tissue distribution is widespread; excretion is complete; no prototype is detected in 1 hour; plasma and blood cell drug content distribution ratio is approximately 4:1; human plasma protein binding rate is high; plasma protein The combination of covalent and hydrophobic effects coexists.