大蒜素聚合物胶束的制备及质量评价  

Preparation and Quality Evaluation of Diallyl Trisulfide Polymeric Micelles

作　　者：邓薇 张洪[1] 高洁芳[1] 范月莹 Deng Wei;Zhang Hong;Gao Jiefang;Fan Yueying(Department of Pharmacy, Renmin Hospital of Wuhan University, Wuhan430060, China;Hubei Provincial Hospital of Traditional Chinese Medicine)

机构地区：[1]武汉大学人民医院药学部,武汉430060 [2]湖北省中医院

出　　处：《中国药师》2019年第4期759-763,共5页China Pharmacist

摘　　要：目的:制备大蒜素聚合物胶束,并对其进行质量评价及初步稳定性考察。方法:以泊洛沙姆P123和泊洛沙姆F127为载体材料,采用薄膜分散法制备大蒜素聚合物胶束,以包封率为指标,通过正交试验筛选最佳处方工艺;采用透射电镜、激光粒度测定仪对大蒜素聚合物胶束进行质量评价;考察聚合物胶束的稳定性并筛选冻干工艺处方。结果:大蒜素聚合物胶束的最佳工艺处方为大蒜素10 mg,泊洛沙姆P123 15 mg,泊洛沙姆F127 15 mg,水相体积20 ml,水化温度20℃;制备的大蒜素聚合物胶束在透射电镜下呈球形,平均粒径(160.1±10.5)nm(n=3),包封率(84.38±1.61)%(n=3)。结论:薄膜分散法制备的大蒜素聚合物胶束粒径适中,冻干产品再分散后粒径变化不大,4℃避光条件下保存1个月,冻干品含量基本稳定。Objective: To prepare diallyl trisulfide( DATS) polymeric micelles,and investigate the characteristics and preliminary stability. Methods: DATS polymeric micelles were prepared by a film-thin hydration method with poloxamer P123 and poloxamer F127 as the carriers,and the best formulation was selected by orthogonal test with the entrapment efficiency as the index. The stability of the micelles and the formulation of freeze drying technology were selected. Results: The best preparation technology of DATS polymeric micelles was as follows: DATS was 10 mg,P123 was 15 mg,F127 was 15 mg,the volume of aqueous phase was 15 ml,and the bath temperature was 20 ℃. Under the transmission electron microscope,the micelles were spherical with the average particle size of( 160. 1 ± 10. 5) nm( n = 3),and the encapsulation rate was( 84. 38 ± 1. 61)%( n = 3). Conclusion: DATS polymeric micelles prepared by the film-thin hydration method have a moderate size. The particle size of lyophilized products does not change after re-dispersion,and keeps basically stable at 4 ℃ for a month in dark place.

关 键 词：大蒜素 聚合物胶束 处方工艺 质量评价 

分 类 号：R944.9[医药卫生—药剂学]