紫苏醇亚微乳的处方工艺优化与稳定性研究

Optimization of the Preparation Technology and Stability Study of Perilla Alcohol Submicron Emulsion

目的：优化紫苏醇亚微乳注射液制备处方工艺,并对制剂的稳定性进行考察。方法：采用高压匀质法制备紫苏醇亚微乳,采用单因素法和正交试验优化处方工艺。以包封率为指标,大豆油用量、大豆磷脂S75-泊洛沙姆188（F68）的比例、匀质转速、匀质次数为因素,并考察最优处方工艺所制得的制剂在离心、高温、光照、加速试验中的稳定性。结果：最优处方工艺中,大豆油用量为12.5 g、大豆磷脂（S75）-泊洛沙姆188（F68）的比例为2∶1、匀质转速为1 400 r/min、匀质次数为8。所制微乳的粒径呈单峰分布,平均粒径为270~300 nm,Zeta电位为41.5~46.7 mV,包封率为48.7%~62.3%,离心后未见分层和油滴。与0时比较,高温、强光、加速条件下制剂各项指标均无明显变化。结论：所制紫苏醇亚微乳具有较好的物理化学稳定性。

OBJECTIVE： To optimize the preparation technology of Perilla alcohol submicron emulsions, and to investigate the stability of the preparation. METHODS ： Perilla alcohol submicron emulsion was prepared by pressure homogenization. The preparation technology was optimized by single factor and orthogonal experiment with entrapment efficiency as index using the amount of soybean oil, the proportion of granulesten （$75） to poloxamer 188 （F68）, rotation rate and times of homogenization as factors. The stability of Perilla alcohol submicron emulsion was investigated under conditions of centrifugation, high temperature, strong light and acceleration test. RESULTS： The optimal preparation technology was as follows： 12.5 g soybean oil, the ratio of S75 to F68 of 2：1, rotation rate of 1 400 r/min, homogenization times of 8 times. There was one apex on particle size distribution curves; mean particle size were 270-300 nm, Zeta-potential were 41.5-46.7 mV, and entrapment efficiency was 48.7 %-62.3%. No stratification and oil bloom was found after centrifugation. No significant change was found in each index under conditions of high temperature, strong light and acceleration test, compared with 0 h. CONCLUSIONS： Perilla alcohol submicron emulsion has the good physical and chemical stability.