注射用人α-心房肽缓释微球的制备及体外释药研究  

Study on the Preparation and In Vitro Release of α-atrial Peptide Sustained-release Microspheres for Injection

作　　者：李新宇 支钦 姚志勇 

机构地区：[1]深圳市健元医药科技有限公司,深圳518057

出　　处：《海峡药学》2016年第11期7-10,共4页Strait Pharmaceutical Journal

摘　　要：目的制备注射用人α-心房肽缓释微球,以实现缓释作用和减少用药次数。方法采用复乳-液中干燥法和冷冻干燥,以聚乳酸-羟基乙酸(PLGA)为载体,羧甲基纤维素钠(CMC)水溶液为分散介质,乙酸乙酯为有机溶剂,甘露醇为保护剂,制备注射用人α-心房肽缓释微球;采用正交试验法,以微球粒径、收率、包封率为指标,优化微球的处方和制备工艺;采用透析法考察含药微球的体外释药特性,计算微球累积释药百分率,绘制体外释药曲线。结果通过正交设计筛选出了制备注射用人α-心房肽缓释微球的处方和制备工艺,载药量为35.4%,包封率为89.7%,Zeta电位为(-28.6±1.64)m V,含药缓释微球的体外释药过程符合Higuchi方程。结论制备的注射用人α-心房肽缓释微球具有长时间的缓释作用。OBJECTIVE To prepare a-atrial peptide sustained-release microspheres and realize the sustainedrelease effect and reduce the frequency of drug use. METHODS a-atrial peptide sustained-release microspheres ying. The prescription and preparation process were optimized by orthogonal test with particlesize, yield and encapsulation as the investigating index. The property of releasing drug in vitro was investigated by the method of dialysis. Calculate the cumulative drug-releasing percentage of sustained-release microspheres and draw the drug-releasing curve. RESULTS The prescription and preparation process were screened according to the orthogonal test with a drug loading capacity of 35.4%, an encapsulation efficiency of 89. 7% and a Zeta potential of （ -28.6 ± 1.64 ） mV. The in vitro releasing profile was in accordance with Higuchi equation. CONCLUSION The Nesiritide Acetatesustained-release microspheres for injection have a long time releasing effect.

关 键 词：人α-心房肽 缓释微球 体外释放 

分 类 号：R94[医药卫生—药剂学]