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目的 制备符合肝动脉栓塞要求的莪术油明胶微球 (ZT GMS)。方法 用正交设计优化了微球的制备工艺 ,对微球的制备工艺、粉体学性质、体外释药、初步稳定性和初步药效进行了研究。结果 球径在 40～ 16 0 μm的微球占 97 16 % ,平均产率为 89 73 % ,平均含药量为 2 13 % ,平均包封率为 19 36 % (均以莪术醇计 )。体外释药 12h达 80 % ,符合一级动力学模型 ,释药机理为溶蚀加扩散。稳定性考察实验结果表明其稳定性较好。肝动脉栓塞荷瘤大鼠实验结果表明大鼠平均生存率显著延长 (P <0 0 1) ,肿瘤体积显著减小 (P <0 0 1)。结论 微球的制备工艺及粒径分布较好 ,体外释药有明显的缓释作用 ,有一定疗效
Objective To prepare zedoary oil gelatin microspheres (ZT GMS) that meet the requirements of hepatic artery embolization. Methods The preparation process of microspheres was optimized by orthogonal design. The preparation process, powder properties, in vitro release, initial stability and preliminary efficacy of microspheres were studied. Results The microspheres with a diameter of 40-160.0 μm accounted for 97 16 %. The average yield was 89 73 %. The average drug content was 213 %, and the average entrapment efficiency was 19 36 % (both with curcumol). The in vitro release rate reached 80% at 12h, which was in line with the first-order kinetic model. The drug release mechanism was dissolution and diffusion. Stability test results show that the stability is better. The experimental results of hepatic artery embolization in rats showed that the mean survival rate of rats was significantly prolonged (P < 0.01) and the tumor volume was significantly reduced (P <0 01). Conclusion The preparation process and particle size distribution of the microspheres are good. The drug release in vitro has obvious sustained-release effect and has a certain curative effect.