中国中药杂志

2016, v.41(18) 3457-3462

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西瑞香素半乳糖化脂质体在大鼠体内组织分布的研究
Tissue distribution of galactosyl daphnoretin liposomes in rats

颜红;欧阳婷;杨琼梁;向彪;夏新华;
YAN Hong;OUYANG Ting;YANG Qiong-liang;XIANG Biao;XIA Xin-hua;School of Pharmacy,Hunan University of Chinese Medicine;

摘要(Abstract):

研究西瑞香素半乳糖化脂质体在大鼠体内的组织分布。按剂量10 mg·kg-1给予健康SD大鼠单剂量尾静脉注射西瑞香素溶液、西瑞香素普通脂质体、西瑞香素半乳糖化脂质体,分别于给药5,15,30,45,60,120,240,360 min后采集大鼠全血和心、肝、脾、肺、肾、胃、小肠、脑、胸腺组织,采用HPLC测定血浆和各组织中西瑞香素的浓度。对比3组制剂,结果发现在不同时刻单位质量肝脏中西瑞香素的含量均以西瑞香素半乳糖化脂质体组为高;所有时间点西瑞香素半乳糖化脂质体对肝脏的靶向指数DTI值均大于西瑞香素普通脂质体,西瑞香素半乳糖化脂质体在肝组织的AUC0-6和Cm ax分别为西瑞香素溶液的2.23,5.22倍。表明西瑞香素半乳糖化脂质体能够在肝脏部位浓集,具有显著的肝脏靶向性。
To study the tissue distribution of galactosyl daphnoretin liposomes in rats. At the dose of 10 mg·kg- 1,daphnoretin solution,daphnoretin liposomes,and galactosyl daphnoretin liposomes were administered to healthy SD rats via tail vein injection. The blood and tissue of heart,liver,spleen,lung,kidney,stomach,small intestine,brain and thymus were collected at 5,15,30,45,60,120,240,360 min after administration. The concentrations of daphnoretin in plasma and tissue samples were determined by HPLC. The results showed that galactosyl daphnoretin liposomes group had the highest concentration of daphnoretin in liver of unit weight at different time points; and at all of the time points,the target index DTI values of galactosyl daphnoretin liposomes to liver were greater than that of daphnoretin liposomes. Compared with daphnoretin solution,the AUC0-6and Cm axof galactosyl daphnoretin liposomes in liver were 2. 23,5. 22 times,respectively. This indicated that galactosyl daphnoretin liposomes can be concentrated at liver,with a significant liver targeting effect.

关键词(KeyWords): 西瑞香素;半乳糖化脂质体;肝靶向;组织分布
daphnoretin;galactosylated liposome;liver targeting;tissue distribution

Abstract:

Keywords:

基金项目(Foundation): 湖南省“十二五”中药学重点学科建设项目(湘教通[2011]76号);; 湖南省科技厅科学研究项目(2012SK3133)

作者(Author): 颜红;欧阳婷;杨琼梁;向彪;夏新华;
YAN Hong;OUYANG Ting;YANG Qiong-liang;XIANG Biao;XIA Xin-hua;School of Pharmacy,Hunan University of Chinese Medicine;

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