摘要
目的研究黄芪甲苷脂质微球注射液的处方工艺并考察其物理稳定性。方法通过高速剪切法制备初乳,二级高压均质法制备脂质微球。以灭菌前后脂质微球的外观性状、粒径、Zeta电位变化为评价指标,分别考察了油相组成、乳化剂及稳定剂的用量、pH值、高压均质条件以及灭菌过程对制剂稳定性的影响。结果确定黄芪甲苷脂质微球注射液的相关处方组成及工艺为:质量分数(w)为10.0%的油相[注射用大豆油(LCT)与注射用中链脂肪酸甘油酯(MCT)等比例混合]、1.2%(w)的大豆卵磷脂、0.1%(w)的Tween80、0.2%(w)的F68、0.05%(w)的油酸钠、0.01%(w)的EDTA;均质前调节pH=8.0,80MPa的压强条件下均质8次,于121℃高压灭菌8min。制得该脂质微球注射液的包封率为88.01%,灭菌后制剂仍能保持良好的物理化学稳定性。结论该处方工艺可行,所得制剂的物理化学稳定性良好。
Objective To optimize the formulation and the preparation process of astragaloside IV lipid microspheres for injection and investigate the physical stability. Methods The coarse emulsion obtained by high-shear mixing was homogenized into a fine monodispersed emulsion with a two-stage pressure homogenizer. The physical stability of the lipid microspheres was evaluated by observing the appearance,measuring the particle size and the Zeta potential of the lipid microspheres before and after sterilization. Factors influencing the preparation process,including homogenization condition,composition of the oil phase,quantity of the emulsifiers and stabilizers,pH value and sterilization procedure,were investigated. Results The optimal formulation was LCT-MCT ( m :m = 1:1 ,total w = 10 %),1.2 % soybean lecithin,0.2% F68,0.1% Tween 80 and 0.05 % sodium oleate. pH was adjusted to 8.0 before homogenization and the sample was homogenized at a pressure of 80 MPa for 8 times at 20 ℃. Finally,astragaloside IV lipid microspheres for injection were sterilized for 8 min by autoclaving at 121℃ and exhibited good stability after sterilization,the entrapment efficiency was 88.01%. Conclusion The prepared astragaloside IV lipid microspheres for injection are stable and the preparation process is feasible.
出处
《中国药剂学杂志（网络版）》
2009年第4期290-298,共9页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
脂质微球注射液
物理稳定性
处方优化
黄芪甲苷
pharmaceutics
lipid microsphere
physical stability
formulation optimization
astragaloside IV
