肺靶向米托蒽醌明胶微球的研究

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。

STUDIES ON LUNG TARGETING GELATIN MICROSPHERES OF MITOXANTRONE

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.