奥曲肽长效生物可降解微球的制备工艺研究

摘要

运用复乳法制备奥曲肽PLGA长效生物可降解微球,并用正交法优化微球制备工艺.利用HPLC、显微镜、激光粒度仪等对微球进行综合质量研究.结果表明,复乳法制备奥曲肽微球的最佳工艺参数为:内水相药物与中油相PLGA的质量比为1∶5,中油相PLGA的浓度为10％,外水相乳化剂为1％的22 000分子量聚乙烯(PVA)水溶液,中油相与外水相的体积比不小于1∶50,复乳化采用机械搅拌法,搅拌速度为1 200 r/min.在该工艺条件下制得的微球,包封率为35.1％,载药量为2.98％,平均粒径为26.3 μm,微球外观圆整,形态良好.%To prepare the octreotide microsphere which is sustained release with biodegradable poly ( DL-lactide-co-glycolide) (PLGA). The method utilizes the W/O/W craft to prepare the microspheres of octreotide peptide in PLGA,and orthogonal testing method to optimize microspheres preparation craft. Take comprehensive quality research with HPLC,microscope,and ultraviolet spectrophotometer. Results showed that the best prescription of octreotide and PLGA is 1:5, the concentration of PLGA is 10% , the concentration of PVA is 1% of the 22 000 molecular weight,oil phase and external water phase volume ratio of not less than 1:50, and the stirring rate is 1 200 r/min, in this craft conditions, the entrapment rate is 35.1% ,the drug loading is 2. 98% , the microspheres particle size is 26.3 μm,the microspheres are rounded appearance and good formed.