目的:制备包封率高、可持续释药35d的丙氨瑞林微球。方法:以生物可降解聚合物聚乳酸-聚羟基乙酸(PLGA)为载体,采用W/O/W复乳溶剂挥发法制备缓释丙氨瑞林微球,以包封率为观察指标,用正交设计L9(34)对微球制备工艺进行优化。在pH=7.0的磷酸盐缓冲溶液中考察微球的体外释放。结果:经优化工艺制备的丙氨瑞林微球包封率为(93.2±1.6)%,90%的微球粒径分布范围为55~65μm。在选择的释放条件下,至35d时,药物累积释放92.3%,突释为9.7%。结论:该制备工艺简单、稳定。优化条件下制备的丙氨瑞林微球包封率高、粒径适宜、突释少。
Objective: To prepare alarelin microspheres with high encapsulation rate and sustained release for 35 days. Methods:Poly(laetic-co-glycolic acid)(PLGA) which could be biodegraded was used as a carrier. Alarelin microspheres were prepared with the W/O/W double emulsion solvent evaporation method, encapsulation rate was used as evaluating indicators. Then, the preparation was optimized with orthogonal test EL9 (34 )]. In vitro release of alarelin microspheres was investigated in the phosphate buffer solution(pH 7.0). Results: The encapsulation rate of alarelin microspheres was (93.2 ± 1.6)%. Almost 90% of the particle diameter of alare|in microspheres was distributed in 55-65 um. Under the selected release conditions, the cumulative drug release was 92.3~ and the burst release was 9.7~ within 35 days. Conclusion: This preparation process is simple and stable. The alarelin microspheres prepared with this optimized method have high encapsulation rate, appropriate particle diameter and low burst release rate.