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¹²⁵I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¹²⁵I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 getting.METHODS:Tissue distribution of RA-MS in mice was studied by ¹²⁵I 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 ¹²⁵I 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.