重组降血压肽缓释微球的制备与体外释放

目的采用复乳溶剂蒸发法制备重组降血压肽(rAHP)缓释微球。方法以聚乳酸(PLA)为缓释材料,利用正交设计优化微球制备的最佳工艺条件,并考察了微球的体外释药特性。结果微球制备的最优工艺为:油相中PLA的浓度为7.5%、初乳搅拌速度为900 r/min、内水相与油相体积比为1∶10,外水相聚乙烯醇124浓度为5%;按此工艺制备的微球粒径跨度小、分布均匀,包封率为81.35%,载药量在10.92%,微球得率在80.26%,微球的平均粒径分布范围在75～80μm之间;载药微球在磷酸盐缓冲液中0.5 h内的累积释药量为17.5%,第15天累积释药率达到98.6%。结论该微球制备工艺成熟,包封率高,符合我国药典对缓释制剂的指导原则要求。

Preparation and in vitro release of recombinant antipeptide sustained release microspheres

Purpose To prepare the recombinant peptide(rAHP)poly(L-lactide)(PLA)sustained release microspheres by double emulsion solvent evaporation method.Methods The rAHP-PLA microspheres preparation technique was optimized by orthogonal experiments and in vitro drug release profiles microspheres were also investigated.Results The optimal preparation technique of rAHP-PLA microspheres was:the PLA concentration was 7.5%,the stirring rate of the first emulsion was 900 r/min,the volume ratio of inner water phase to oil phase was 1∶ 10,and the PVA concentration was 5%.The rAHP-PLA microspheres prepared by the optimum technique were smooth,regular in morphology with small span,the encapsulation efficiency was 81.35%,the drug loading was 10.92%,the microsphere yield was 80.26%,and the average particle diameter was in the range of 75-80 μm.The cumulative in vitro release percentage in PBS was 17.5% within 0.5 h,and up to 98.6% in 15 d.Conclusion The rAHP-PLA microspheres can be prepared easily by good morphology with high entrapment efficiency.The in vitro release profiles were in accordance with the guideline of the Pharmacopoeia of China for sustained release preparation.