10-羟基喜树碱缓释微胶囊的组织分布学研究  

Tissue distribution of 10-hydroxycamptothecin microcapsules in mice

作　　者：杨玉焕[1] 邵长敏 骆沙曼[1] 郭宏红[1] 郑健[1] 王洋[1] 

机构地区：[1]东北林业大学盐碱地生物资源环境研究中心,东北油田盐碱植被恢复与重建教育部重点实验室,黑龙江哈尔滨150040

出　　处：《中成药》2013年第8期1644-1648,共5页Chinese Traditional Patent Medicine

基　　金：引进国际先进林业技术项目(2012-4-04);黑龙江省留学归国基金项目(LC201004)

摘　　要：目的考察了小鼠灌胃10-羟基喜树碱(HCPT)缓释微胶囊[HCPT(Fe3+/DS)n]后,药物在各个组织的分布特征。方法以氯化铁(Fe3+)和硫酸葡聚糖钠(DS)为囊壁材料,采用聚电解质静电吸引层层自组装的方法制备HCPT(Fe3+/DS)n。小鼠分别灌胃HCPT或HCPT(Fe3+/DS)n(80 mg/kg),给药前及给药后取小鼠心、肝、脾、肺、肾和脑组织。采用高效液相色谱-荧光检测法测定HCPT质量浓度,并计算药代动力学参数。结果 HCPT在各组织分布的质量浓度由高至低顺序为肝>肾>肺>脾>脑>心。同一组织中,HCPT(Fe3+/DS)n比HCPT更易于吸收。在肺、脾、脑三种组织中随着微胶囊外壳包裹层数的增多,HCPT质量浓度有升高趋势。结论 HCPT(Fe3+/DS)n与HCPT相比,能够改善药物在小鼠体内的组织分布,并且具有明显的肝组织靶向性。AIM To study the tissue distribution in mice after 10-hydroxycamptothecin（HCPT） gastric perfusion in the microcapsule [HCPT（Fe3＋/DS）n] form.METHODS Using ferric chloride and dextran sulfate sodium as wall,materials layer-by-layer adsorption was used to mark the electrostatic self assembly microcapsule.Mice were intragastrically administrated a single dose of HCPT or HCPT（Fe3＋/DS）n（80 mg/kg）.HCPT concentrations in heart,liver,spleen,lung,kidney and brain before and after gastric perfusion were measured by HPLC and the pharmacokinetic parameters were calculated.RESULTS HCPT concentrations in liver were the highest from high to low in turn in kidney,lung,spleen,brain and heart.In each tissue,the HCPT concentration released from HCPT（Fe3＋/DS）n was more than that of HCPT.With the increase of layer numbers of the microcapsules,the tissue distribution of HCPT significantly increased in lung,spleen and brain.CONCLUSION The experiment showed that HCPT（Fe3＋/DS）n could improve tissue distribution in mice and concentrate on liver in comparison with HCPT.

关 键 词：羟基喜树碱 缓释微胶囊 组织分布 

分 类 号：R966[医药卫生—药理学]