吴茱萸碱脂质体在大鼠体内的药动学及小鼠体内的组织分布研究
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篇名: 吴茱萸碱脂质体在大鼠体内的药动学及小鼠体内的组织分布研究
TITLE:
摘要: 目的:研究吴茱萸碱脂质体在大鼠体内的药动学特征和在小鼠体内的组织分布及其靶向性。方法:取大鼠随机分为2组,每组8只,分别单剂量尾iv吴茱萸碱脂质体和吴茱萸碱溶液(以吴茱萸碱计10 mg/kg);给药后分别于0.083、0.25、0.5、0.75、1、1.5、2、3、4、5 h眼底静脉丛取血0.5 ml,采用高效液相色谱法测定血浆中吴茱萸碱的浓度,采用DAS 2.1.1软件计算药动学参数。取小鼠随机分为2组,每组30只,分别单剂量尾iv吴茱萸碱脂质体和吴茱萸碱溶液(以吴茱萸碱计8 mg/kg),给药后分别于0.083、0.25、0.5、1、2、4、6、8、10、12 h处死3只,立即取出心、肝、脾、肺、肾,采用高效液相色谱法测定其中的药物浓度,考察吴茱萸碱的组织分布。结果:吴茱萸碱脂质体及溶液在大鼠体内的药动学符合非房室模型,t1/2分别为(1.78±0.58)、(1.06±0.40) h,AUC0-t分别为(4.63±0.33)、(2.75±0.09) μg·h/ml(P<0.01);在小鼠体内的组织浓度分别为肝>脾>肺>心脏>肾,脾>肝>肾>心脏>肺。结论:与溶液比较,脂质体增加了吴茱萸碱吸收,且增加了其在肝脏中的分布,具有良好的肝靶向性。
ABSTRACT: OBJECTIVE: To study the pharmacokinetic characteristics of evodiamine liposome in rats and the tissue distribution and targeting in mice. METHODS: The rats were randomly divided into 2 group with 8 rats in each group; they were given evodiamine liposomes and solution (10 mg/kg by evodiamine) via tail vein respectively. 0.5 ml fundus venous plexus blood were sampled respectively at 0.083, 0.25, 0.5, 0.75, 1, 1.5 ,2, 3, 4 and 5 h after administration. The plasma concentration of evodiamine in rats were measured by HPLC. The pharmacokinetic parameters were calculated by DAS 2.1.1 software. The mice were randomly divided into 2 groups with 30 rats in each group; they were given evodiamine liposomes and solution (8 mg/kg by evodiamine) via tail vein respectively. The heart, liver, spleen, lung and kidney tissues were removed immediately after every 3 mice were sacrificed at 0.083,0.25,0.5,1,2,4,6,8,10,12 h after administration. The concentrations of evodiamine were measured by HPLC, and the distribution of evodiamine in each tissue was analyzed. RESULTS: The pharmacokinetics of evodiamine liposomes and solutions in rats were in line with non-compartment model; their pharmacokinetic parameters were as follows as t1/2 of (1.78±0.58) h and(1.06±0.40) h, AUC0-t of (4.63±0.33) μg·h/ml and (2.75±0.09) μg·h/ml (P<0.01). The concentrations of evodiamine in each tissue of mice were in descending trend as liver>spleen>lung>heart>kidney, and spleen>liver>kidney>heart>lung. CONCLUSIONS: Compared with solution, liposomes promote the absorption of evodiamine and the distribution of it in liver, showing good liver targeting.
期刊: 2016年第27卷第16期
作者: 邢玉桂
AUTHORS: XING Yugui
关键字: 吴茱萸碱;脂质体;药动学;组织分布;大鼠;小鼠
KEYWORDS: Evodiamine; Liposomes; Pharmacokinetics; Tissue distribution; Rats; Mice
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