桑根酮C吸入型粉雾剂的制备与体外性能初步评价  

Preparation and preliminary evaluation of sanggenon C inhalation powder aerosol

作　　者：吴祖芳 吴玉梅 韩薛魏 吴红阳 杨彩婷 袁建容 袁泽利 Wu Zufang;Wu Yumei;Han Xuewei;Wu Hongyang;Yang Caiting;Yuan Jianrong;Yuan Zeli(School of Pharmacy,Zunyi Medical University,Zunyi Guizhou 563006,China)

机构地区：[1]遵义医科大学药学院,贵州遵义563006

出　　处：《遵义医科大学学报》2024年第12期1164-1171,共8页Journal of Zunyi Medical University

基　　金：贵州省卫生健康委科学技术基金资助项目(NO:gzwjkj2020-1-212);贵州省教育厅2021年度普通本科高校青年科技人才成长项目[NO:黔教合KY字(2022)274]。

摘　　要：目的 设计制备桑根酮C吸入型粉雾剂,并对其粉体学性质、吸入性能及稳定性等方面进行初步评价。方法 选择聚乳酸-羟基乙酸共聚物为载体材料,以二氯甲烷和乙酸乙酯为溶剂,聚乙烯醇为乳化剂,采用乳化-溶剂挥发法来制备桑根酮C微球,并采用冷冻干燥制备粉雾剂;对粉雾剂的载药量、包封率、粉体学性质、吸入性能及稳定性等进行考察。结果 所制备的桑根酮C微球呈球形,粉雾剂中微球的粒径为(4.86±0.89)μm, zeta电位为(-4.37±1.10) mV,符合吸入制剂要求;水分含量为(3.01±0.59)%,吸湿增重百分率为(1.96±0.57)%,略有引湿性;堆密度为(0.136±0.005) g/mL,休止角为(24.31±2.54)°,粉体流动性良好;能迅速雾化,雾化性能良好,排空率均大于规定值90%;包封率高,约为100%,载药量为(0.764±0.011)%;pH值为中性,且在不同温度下稳定性良好。结论 所制备的桑根酮C吸入型粉雾剂达到了预期目标,为该制剂的后期生物应用提供了一定的实验基础。Objective To design and prepare sanggenon C inhalation powder aerosol,and evaluate its powder properties,inhalation performance and stability.Methods Poly(lactic-co-glycolic acid)was used as carrier material,dichloromethane and ethyl acetate were used as solvent,and polyvinyl alcohol was used as emulsifier.The sanggenon C loaded microspheres were prepared by emulsification-solvent evaporation method,and the powder was prepared by freeze drying method.The drug loading,encapsulation efficiency,powder properties,inhalation properties and stability of the powder were investigated.Results The prepared sanggenon C microspheres were spherical,the particle size of microspheres in the powder was(4.86±0.89)μm,and the zeta potential was(-4.37±1.10)mV,which met the requirements of inhalation preparation.The moisture content was(3.01±0.59)%,and the weighting percentage of moisture absorption was(1.96±0.57)%.The bulk density was(0.136±0.005)g/ml,and the angle of repose was(24.31±2.54),thus the powder had good fluidity.It could be atomized quickly with good atomization performance,and the emptying rate was more than 90%of the specified value.The encapsulation rate was about 100%,and the drug loading was(0.764±0.011)%.The pH value was neutral,and it was stable at different temperatures.Conclusion The preparation of sanggenon C inhaled powder has reached the expected goal,which provides a certain experimental basis for the later biological application of this preparation.

关 键 词：桑根酮C 聚乳酸-羟基乙酸共聚物 微球 粉雾剂 

分 类 号：R944.9[医药卫生—药剂学]