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目的:制备胸腺五肽(TP-5)微球注射剂,考察不同制备方法对微球性质的影响。方法:以乳酸-羟基乙酸共聚物[poly(lactide-co-glycolide),PLGA]为包裹材料,分别采用复乳法(W/O/W)、固体/油/油法(S/O/O)和固体/油/水法(S/O/W)制备TP-5微球。以微球形态、粒径、微球载药量以及包封率、体外释药曲线等作为微球的质量评价指标,选择合适的制备方法。结果:W/O/W法制备出的TP-5微球流动性良好,形态圆整,平均粒径为(22.14±0.28)μm,微球的包封率为(54.2±3.1)%,突释为(24.3±0.49)%,28d的累积释放量在90%以上。结论:采用复乳法,可以制备含TP-5的PLGA微球。
Objective: To prepare thymopentin (TP-5) microspheres injections and investigate the influence of different preparation methods on the properties of microspheres. METHODS: Poly (lactide-co-glycolide) (PLGA) was used as the encapsulating material in this study. The effects of multiple emulsifying agents (W / O / W), solid / oil / ) And solid / oil / water (S / O / W) TP-5 microspheres. Microsphere morphology, particle size, microspheres drug loading and entrapment efficiency, in vitro release curve as the microsphere quality evaluation index, select the appropriate preparation method. Results: The TP-5 microspheres prepared by the W / O / W method showed good fluidity and roundness with an average particle diameter of (22.14 ± 0.28) μm and encapsulation efficiency of (54.2 ± 3.1)% The release was (24.3 ± 0.49)%, and the cumulative release of 28 days was over 90%. Conclusion: PLGA microspheres containing TP-5 can be prepared by double emulsion method.