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肺靶向利福平聚乳酸微球的研究
引用本文:张万国,蒋雪涛,朱才娟,胡晋红.肺靶向利福平聚乳酸微球的研究[J].药学学报,1998,33(1):57-61.
作者姓名:张万国  蒋雪涛  朱才娟  胡晋红
作者单位:1. 第二军医大学长海医院药剂科,上海,200433
2. 第二军医大学药学院
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。

关 键 词:利福平  聚乳酸  微球  肺靶向
收稿时间:1997-03-04

STUDY ON THE RIFAMPICIN POLYLACTIC ACID MICROSPHERES FOR LUNG TARGETING
Zhang Wanguo,Jiang Xuetao,Zhu Caijuan,Hu Jinhong.STUDY ON THE RIFAMPICIN POLYLACTIC ACID MICROSPHERES FOR LUNG TARGETING[J].Acta Pharmaceutica Sinica,1998,33(1):57-61.
Authors:Zhang Wanguo  Jiang Xuetao  Zhu Caijuan  Hu Jinhong
Affiliation:School of Pharmacy, Second Military Medical University, Shanghai 200433.
Abstract: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 microns. 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 (gamma = 0.9892). The RFP-PLA-MS was stable after stored at 4 degrees C 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.
Keywords:Rifampicin  Polylactic acid  Microspheres  Lung targeting
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