【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。更多还原

【Abstract】 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.更多还原