肺靶向利福平聚乳酸微球的研究  

STUDY ON THE RIFAMPICIN POLYLACTIC ACID MICROSPHERES FOR LUNG TARGETING

作　　者：张万国[1,2] 蒋雪涛[1,2] 朱才娟[1,2] 胡晋红 

机构地区：[1]第二军医大学药学院 [2]第二军医大学长海医院药剂科

出　　处：《药学学报》1998年第1期57-61,共5页Acta Pharmaceutica Sinica

摘　　要：在单因素考察的基础上进行正交试验设计，筛选出肺靶向利福平聚乳酸微球的最佳制备工艺条件；利用桨板法研究了微球的体外释药规律；考察了微球在不同温度下的稳定性；用新西兰兔为实验对象，研究了利福平聚乳酸微球的体内药动学及组织药物分布。结果制得的微球形态圆整，粒径在５～１５μｍ范围内的占总体积的８６５４％，微球平均粒径为９００±４０８μｍ；包封率为３１９％；载药量为１６０％；体外释药方程为Ｑ＝２０７７＋１０１２Ｔ１／２（γ＝０９８９２）；微球在冰箱４℃和室温（２０～２５℃）条件下性质稳定；体内实验表明微球具有长效和肺靶向双重作用。In this paper, the effects of different variables on the preparation of polylactic acid microspheres (PLAMS ) were studied. The optimized preparation conditions of rifampicin polylactic acid microspheres (RFPPLAMS) were aquired through orthogonal test. The paddle method was used to study the drug release properties of RFPPLAMS. Stability of RFPPLAMS at different temperatures was also studied. Pharmacokinetic and tissue distribution of RFPPLAMS after intravenous administration were carried out in rabbits. The experiments revealed that the RFPPLAMS was regular in its morphology with a mean diameter of 900±408 μm.The drug loading was 160% and encapsulation efficiency was 319%. The release properties could be expressed by the following equation: Q=2077+1012T1/2 (γ=09892). The RFPPLAMS was stable after stored at 4℃ and room temperature under desiccated condition for three months. RFPPLAMS showed a combination of lung targeting and sustained drug release in experiments on rabbits.

关 键 词：利福平 聚乳酸 微球 肺靶向 

分 类 号：R978.3[医药卫生—药品] R944.9[医药卫生—药学]