醋酸布舍瑞林纳米粒的制备及体外释放特性研究

目的:制备醋酸布舍瑞林纳米粒并考察其体外释药特性。方法:以复乳法制备纳米粒。采用高效液相色谱法测定其含量并计算制剂包封率及载药量,透析袋法考察制剂体外释药特性。结果:所制制剂外观圆整,醋酸布舍瑞林检测浓度的线性范围为0.1～8.0μg·mL-(1r=0.999 9),平均回收率为105.38%,日内RSD<1.78%,日间RSD<0.93%。制剂包封率为(63.37±0.29)%,载药量为(1.03±0.09)%,在pH 7.4的磷酸盐缓冲液中72 h的累积释药百分率为62.35%。结论:该制剂制备工艺简单可行,具有明显的缓释效果。

Study on the Preparation of Buserelin Acetate Nanoparticles and Its Release Property in Vitro

OBJECTIVE： To prepare Buserelin acetate nanoparticles（BA-NP） and to investigate its release property in vitro.METHODS： The BA-NP was prepared using double emulsion method.The content determination of BA-NP was performed using HPLC,and encapsulation efficiency and drug-loading rate of BA-NP were calculated.In vitro drug release property of nanoparticles was investigated by bag filter method.RESULTS： Prepared nanoparticles were even and regular in appearance.The linear range of buserelin acetate was 0.1～8.0 μg·mL-1（r=0.999 9） with an average recovery of 105.38%.The RSD of intra-day and inter-day were lower than 1.78% and 0.93% respectively.The encapsulation efficiency of nanoparticles was（63.37±0.29）% and drug-loading rate of（1.03±0.09）%.The accumulative release rate of nanoparticles in phosphate buffer（pH=7.4） at 72 h was 62.35%.CONCLUSION： The preparation process of BA-NP is simple and particle with ideal release effect.