Wang J H, Lu B, Xu P L, Bao D Y, Zhang Z R
School of Pharmacy, West China University of Medical Sciences, Chengdu.
Yao Xue Xue Bao. 1995;30(7):549-55.
Lung targeting gelatin microspheres of mitoxantrone (DHAQ) were prepared by a two-step method. The diameter of 87.36% of the DHAQ gelatin microspheres (DHAQ-GMS) was in the range of 5.1 to 25.0 microns. Release of the drug from the DHAQ-GMS in vitro became much slower and its t1/2 was 4 times longer than that of pure DHAQ. The characteristic peak of heat absorption on the differential thermal analysis curve was at 133 degrees C and almost no change was observed after the DHAQ-GMS were stored for 3 months at 37 degrees C (relative humidity 75%). The distribution test in vivo in mice indicated that the lung targeting effect of the DHAQ-GMS was obvious and that the targeting efficiency of the lung compared to other organs and blood increased 3 to 35 times. Kinetic behavior of the drug in mouse lung could be described by one open compartment model, and the average residual time increased by 10 h.
采用两步法制备了米托蒽醌（DHAQ）肺靶向明胶微球。87.36%的DHAQ明胶微球（DHAQ-GMS）直径在5.1至25.0微米范围内。DHAQ从DHAQ-GMS中的体外释放变得慢得多，其t1/2比纯DHAQ长4倍。差示热分析曲线上的吸热特征峰在133℃，DHAQ-GMS在37℃（相对湿度75%）下储存3个月后几乎没有变化。小鼠体内分布试验表明，DHAQ-GMS的肺靶向作用明显，与其他器官和血液相比，肺的靶向效率提高了3至35倍。药物在小鼠肺中的动力学行为可用一级开放房室模型描述，平均残留时间增加了10小时。
