用二步法制得流动性好、吸湿性小、稳定性深兰色粉未状的米托蒽醌明胶微球。球内含量为8.17%。带正电荷,其粒径5.1-2.50um占总数87.6%,体外释药符合一级动力学规律,与原药比释药t1/2延长4倍,小鼠体内分布到肺的药量经原药增加6.4倍,分布到心脏减少80%,肺的相对摄取率最大,肺的靶向效率增在3-35倍,在肺内符合一室模型,与原药比其消除半衰其从7.8h延长到27h,平均滞留时间37h延长到47h,清除率降低68%。在血中符合三室模型,与原药比其消除半衰期从74.8h延到132.5h,消除率降低23%,。对小鼠肺部S-180肿瘤的抑瘤率(60%)与原药的剂量减半时相当。成功地制成小鼠静注后药可浓集于肺,对S-180肿瘤抑瘤率高,降低心脏副作用的肺靶向给药系统。
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数据更新时间:2023-05-31
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