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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 Xanthahnin galactosylated liposomes in rats. Dose of 10 mg · kg-1 was given to healthy SD rats single dose intravenous injection of cedilanid solution, cedilanidipin liposomes, cedilanidin galactosylated liposomes, respectively, in the administration of 5,15,30 The whole blood and heart, liver, spleen, lung, kidney, stomach, small intestine, brain and thymus tissues of rats were collected at 45, 60, 120, 240 and 360 min after injection. The concentrations of cedilanid in plasma and tissues were determined by HPLC. Comparing the three groups of preparations, the results showed that at different times, the content of middroperidin per unit mass of liver in the liver was higher than that in the cantavatin galactosylated liposome group; at any time point, the targeting index DTI values were greater than the common diterpene liposomes liposomal liposomal galactoside in the liver tissue AUC0-6 and Cm ax were 2.23,5.22 times the dorsal solution. Show that cedrupin galactosylated liposomes can be concentrated in the liver site, with significant liver targeting.