骨炎一号微球的制备及其体外释药性能的研究

目的:制备骨炎一号微球,并考察其体外释药性能。方法:采用复乳-溶剂挥发法制备骨炎一号微球,用电子扫描显微镜观察微球表面形态,并测定微球的平均粒径、粒度分布、载药量、包封率,采用小杯法测定骨炎一号微球的体外释药情况,并计算其累积释药量。结果:制得的骨炎一号聚乳酸微球的形态圆整,微球的平均粒径为8.59μm,粒径在1-12μm的占总数的90%以上,载药量为48.39%,包封率为19.32%。骨炎一号微球在108h的累积释药量约为78.4%,t_1/2为40.8h,Higuchi方程为Y=0.1326 X-0.4782,r=0.9951。结论:得到了比较满意的骨炎一号微球制备工艺,且其体外释药性能符合长效制剂特征。

The preparation and the in vitro release of OANO-1 microspheres

OBJECTIVE: To prepare OANO-1 microspheres and test their release in vitro. METHOD: OANO-1 microspheres were made by W/O/W-liquid drying process. The surface morphology of the microspheres was observed by SEM. The mean diameter and the size distribution of microspheres, the drug loading and the incorporation efficiency were examined. The release of OANO-1 microspheres in vitro was examined by small cup method. The accumulated release percent of OANO-1 microspheres was examined. RESULT: The OANO-1 microspheres were regular in their morphology. The average particle size was 8.59 microm with over 90% of the microspheres being in the range of 1-12 microm. The drug loading and the incorporation efficiency were 48.39% and 19.32% respectively. The accumulated release percent of OANO-1 microspheres was 78.4% after 108 h. The release half-life t1/2 was 40.8 h and Higuchi equation was Y = 0.1326 X - 0.4782, r = 0.9951. CONCLUSION: The preparation of OANO-1 microspheres was well. The release in vitro of OANO-1 microspheres showed significant sustained release.