联苯双酯固体脂质纳米粒在小鼠体内的组织分布研究  

Tissue Distribution of Bifendate Solid Lipid Nanoparticles in Mice

作　　者：张洪[1] 成蓓[2] 詹新安[2] 谭晔[2] 

机构地区：[1]武汉大学人民医院药学部,武汉市430060 [2]武汉大学药学院,武汉市430072

出　　处：《中国药房》2009年第22期1718-1720,共3页China Pharmacy

摘　　要：目的:研究联苯双酯(DDB)固体脂质纳米粒(DDB-SLN)在小鼠体内的组织分布情况及肝靶向性。方法:60只小鼠尾静脉分别注射含DDB剂量为20mg.kg-1的DDB-SLN及DDB溶液(DDBS),在给药后0.083、0.25、1、3、5h时分别取样,以高效液相色谱法测定并计算不同时间血浆、心、肝、脾、肺、肾、脑中DDB的浓度,以及DDB-SLN对DDBS的药物靶向指数(DTI)和药物选择性指数(DSI)。结果:各组织中DDB浓度2组中均以肝中为最高;给药后0.25、1、3、5h时肝中浓度DDB-SLN分别是DDBS的1.15、3.04、2.72、3.62倍,DTI分别为1.151、3.038、2.720、3.622,DSI分别为3.269、7.891、5.948、7.759。结论:DDB-SLN具有肝靶向性,且强于DDBS。OBJECTIVE： To study the tissue distribution and liver- targeting activity of bifendate solid lipid nanoparticles （DDB- SLN） in mice. METHODS： A total of 60 mice were injected with DDB-SLN or DDB solution （DDBS） with DDB dosage at 20 mg.kg^-1. Sampling was scheduled at 0.083, 0.25, 1, 3 and 5 hours, and HPLC was employed to determine and compute the concentrations of DDB in plasma, heart, liver, spleen, lung, kidney and brain as well as the Drug Targeting Index （DTI） and the Drug Selecting Index （DSI） of DDB-SLN on DDBS. RESUTLS： The DDB concentrations in liver were the highest for both groups. At 0.25, 1, 3 and 5 h, the DDB concentrations in liver in DDB-SLN group were 1.15, 3.04, 2.72 and 3.62 times those in DDBS group. The DTI of DDB- SLN were 1.151, 3.038, 2. 720 and 3. 622, respectively and the DSI were 3.269, 7.891, 5.948 and 7.759, respectively. CONCLUSION： As compared with DDBS, DDB-SLN is a more potent liver - targeting drug.

关 键 词：联苯双酯 固体脂质纳米粒 小鼠 组织分布 肝靶向性 

分 类 号：R965[医药卫生—药理学] R975.5[医药卫生—药学]