β-细辛醚微乳的制备及其性质考察

Preparation and quality investigation of β-asarone microemulsion

目的制备β-细辛醚微乳,并对其性质进行考察。方法根据β-细辛醚在各溶媒中的溶解度初步确定处方组成,通过绘制伪三元相图对处方进行优化;采用HPLC法测定微乳中β-细辛醚的质量分数;以外观、粒径及其分布、多分散指数(PI)、pH值、黏度和β-细辛醚的质量分数为指标考察所制备微乳的初步稳定性。结果优化的处方组合为β-细辛醚-肉豆蔻酸异丙酯-聚氧乙烯蓖麻油-丙三醇的质量比为1∶2∶8∶2。制备的微乳澄清透明,有蓝色乳光,平均粒径为(18.2±0.2)nm,PI为0.222±0.005,pH值为6.50±0.01,10 000 r/min离心10 min后和高温灭菌后均无分层现象,平均载药量为(21.5±0.48)mg/mL。结论所制备的微乳理化性质较稳定,符合鼻腔给药制剂的标准。

Objective To prepare β-asarone microemulsion （β-AME） and to investigate its physicochemical properties. Methods The formulation was investigated by solubility experiment and optimized by pseudotemary phase diagram; The content of β-asarone was determined by HPLC method. Physical appearance, particle size and its distribution, polydispersity index （PI）, pH value, viscosity, and content of β-asarone were used as indexes to evaluate the stability of β-AME. Results The optimized formulation was as follows： The proportion of β-asarone-isopropyl myristate-Cremophor EL-glycerol was 1 ： 2 ： 8 ： 2. The emulsion was transparent liquid with blue opalescence; The average particle size of β-AME was （18.2 ± 0.2） nm with a PI of 0.222 ± 0.005; The pH value was 6.50 ± 0.01, and after high temperature sterilizing and centrifuging at 10 000 r/min for 10 min there was no stratification; The drug loading amount was （21.5 ± 0.48） mg/mL. Conclusion The physicochemical properties of D-AME are relatively stable, which meets the standards of intranasal administration preparations.