利福平白蛋白微球肺组织靶向性动物实验研究

Studies on the lung tissue targeting of rifampin albumin microspheres in animals

目的 :研究静脉注射利福平白蛋白微球后微球的体内分布及降解、肺组织病理变化以及肺靶向后对动脉血中氧分压的影响。方法 :微球用12 5I标记 ,静脉注射后测定大鼠各组织的放射性记数 ;取肺组织做病理切片观察病理改变 ;肺靶向后取动脉血测定氧分压。结果 :静注12 5I标记的微球后 5min肺部分布达 95 %以上并缓缓降解 ;肺靶向后对肺组织病理和动脉血中氧分压无明显影响。结论 :将抗结核药利福平制备成微球制剂 ,肺部分可提高药物在肺部的分布 ,静注后无明显不良反应。

OBJECTIVE:To study the tissue distribution and degradation after i.v rifampin albumin microspheres (RA MS) and the change of lung tissue pathology and oxygen partial pressure after pulmonary tar geting.METHODS:Tissue distribution of RA MS in mice was studied by 125 I labeled microspheres.Lung tissue pathology change was analyzed by observing pathological section.The change of gas exchange function was studied by determining blood oxygen partial pressure in rats.RESULTS:Above 95 percent 125 I labelled microspheres were distributed to lung tissue in 5 minutes and RA MS were degraded gradually.Pulmonary targeting had no significant effects on lung tissue pathology and blood oxygen partial pressure.CONCLUSION:The lung tissue pulmonary distribution rate of rifampin may be promoted by making rifampin into microsphere dosage form and there were no significant side effects.