CAJ | 학술논문

目的：制备聚乳酸利福喷丁微球，评价其体外释药特性及其在小鼠体内的肺靶向性。方法采用溶剂挥发法制备聚乳酸利福喷丁微球，动态透析法考察其体外释药性能。实验动物静脉注射后，测定其各组织的药物浓度，研究其体内相对分布百分率及其肺靶向性。结果制得的聚乳酸利福喷丁微球在7～30μm粒轻范围的占聚乳酸利福喷丁微球总数的81.6％，平均粒径为（14.2±3.1）μm，包封率为78.39％，载药量为（39.6±3.6）％（n＝5），体外释药T50为68 min，较对照组延长了4.5倍。小鼠实验表明，制得聚乳酸利福喷丁微球后，药物在肺组织中的相对分布百分率明显高于其他组织与血液，并较对照组提高了3.3倍。结论该法制得的聚乳酸利福喷丁微球具有明显的缓释性及肺靶向性。
목적：제비취유산리복분정미구，평개기체외석약특성급기재소서체내적폐파향성。방법채용용제휘발법제비취유산리복분정미구，동태투석법고찰기체외석약성능。실험동물정맥주사후，측정기각조직적약물농도，연구기체내상대분포백분솔급기폐파향성。결과제득적취유산리복분정미구재7～30μm립경범위적점취유산리복분정미구총수적81.6％，평균립경위（14.2±3.1）μm，포봉솔위78.39％，재약량위（39.6±3.6）％（n＝5），체외석약T50위68 min，교대조조연장료4.5배。소서실험표명，제득취유산리복분정미구후，약물재폐조직중적상대분포백분솔명현고우기타조직여혈액，병교대조조제고료3.3배。결론해법제득적취유산리복분정미구구유명현적완석성급폐파향성。
Objective To prepare PLA-Rifapentinum microspheres(RifapM) for lung targeting and evaluate it′s rule of rifapentinum release and lung targeting in mice .Methods Solvent volatilization was used to prepare lung targeting RifapM,and dynamic dialysis method was adopted to observe the rule of rifapentinum release .In vivo distri-bution was studied .Results The diameters of 81.6% microspheres were between 7~30 μm,the average diameter was (14.2 ±3.1)μm.Entrapment efficiency was 78.39%.The drug supporter in microspheres was (39.6 ±3.6)%(n=5).The invitro release T50 was 68 min, and was 4.5 times more than that of the control group .The relative dis-tribution percentage of RifapM in lung after iv administration to mice was significantly higher than those in other tis -sues and blood ,and was 3.3 times more than control group .Conclusion RifapM have evident sustained-release and lung targeting .