肺靶向米托蒽醌明胶微球的研究  

STUDIES ON LUNG TARGETING GELATIN MICROSPHERES OF MITOXANTRONE

作　　者：王剑红[1] 陆彬[1] 胥佩菱[1] 包定元[1] 张自然[1] 

机构地区：[1]成都华西医科大学药学院

出　　处：《药学学报》1995年第7期549-555,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金

摘　　要：采用二步法制备米托蒽醌明胶微球，球径范围为５．１～２５．０μｍ的占总数８７．３６％，体外释药与原药相比ｔ１／２延长４倍，ＤＴＡ曲线上的特征吸热峰为１３３℃，经３７℃，ＲＨ７５％考察３月，几乎无变化。经小鼠体内分布试验表明具有明显的肺靶向性，靶向效率增加３～３５倍，肺中药代动力学行为可用一室开放模型描述，平均滞留时间延长１０ｈ。Lung targeting gelatin microspheres of mitoxantrone(DHA)were prepared by atwo-step methed. The diameter of 87. 36%of the DHAQ gelatin microspheres (DHAQ-GMS)was inthe range of 5.1 to 25.0 μm. Release of the drug from the DHAQ-GMS in vitro became much slowerand its t1/2 was 4 times longer than that of pure DHAQ.The characteristic peak of heat absorption onthe differential thermal analysis curve was at 133℃ and almost no change was observed after theDHAQ-GMS were stored for 3 months at 37℃ (relative humidity 75%). The distribution test in vivoin mice indicated that the lung targeting effect of the DHAQ-GMS was obvious and that the targetingefficiency of the lung compared to other organs and blood increased 3 to 35 times, Kinetic behavior ofthe drug in mouse lung could be described by one open compartment model, and the average residual time increased by 10h.

关 键 词：米托蒽醌 明胶 微球 抗癌药 肺靶向给药 

分 类 号：R944.9[医药卫生—药剂学] R979.1[医药卫生—药学]