| 摘要: |
| ［摘要］ 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7～30 μm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。 |
| 关键词: 利福喷丁 聚乳酸微球 肺靶向性 缓释性 |
| DOI：10.3969/j.issn.1674-3806.2014.08.09 |
| 分类号:R 943 |
| 基金项目: |
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| Preparation of PLA-Rifapentinum microspheres and the effect of lung targeting in mice |
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FAN Ying, GUO Mei-hong, LIANG Kai, et al.
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School of Pharmaceutical Sciences,Guangxi Medical University,Nanning 530021,China
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| Abstract: |
| ［Abstract］ 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 distribution 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 distribution percentage of RifapM in lung after iv administration to mice was significantly higher than those in other tissues and blood，and was 3.3 times more than control group.Conclusion RifapM have evident sustained-release and lung targeting. |
| Key words: Rifapentinum PLA-microspheres Lung targeting Sustained-release |
