作　　者： (常金花）; (薛禾菲）; (刘沛）; (刘翠哲）;

机构地区： 承德医学院,河北省中药研究与开发实验室,河北承德067000

出　　处： 《中成药》 2017年第9期1819-1824,共6页

摘　　要： 目的制备薯蓣皂苷元纳米混悬液。方法介质研磨法制备纳米混悬液后,冷冻干燥法将其固化。以粒径及多分散系数(PDI)为评价指标,稳定剂种类、薯蓣皂苷元与稳定剂比例、初混悬液体积与研磨珠质量比例、研磨时间、冻干保护剂种类及其用量为影响因素,单因素试验筛选制备和固化工艺。观察纳米混悬液形态,测定纳米混悬液和冻干粉的粒径和PDI。结果最佳条件为薯蓣皂苷元与普朗尼克F127(稳定剂Ⅰ)比例6∶1,与十二烷基硫酸钠(SDS,稳定剂Ⅱ)比例50∶1,初混悬液体积与研磨珠质量比例1∶4,研磨时间120 min,以8%PEG-6000和2%甘露醇为冻干保护剂。纳米混悬液呈棒状或片状,平均粒径和多分散指数分别为(348.1±14.2)nm和0.244±0.059,均低于冻干粉。室温下,纳米混悬液、冻干粉粒径分别在35 d、3个月内保持稳定。结论薯蓣皂苷元冻干粉的物理稳定性优于其纳米混悬液,复溶后即可使用。 AIM To prepare diosgenin nanosuspensions. METHODS The nanosuspensions prepared by media milling method were solidificated by freeze drying method. With particle size and polydispersity index（ PDI）as evaluation indices,stabilizer kind,ratio of diosgenin to stabilizer,ratio of preliminary nanosuspension volume to grinding bead amount,milling time,lyoprotectant kind and its amount as influencing factors,single factor test was applied to screening preparation and solidification processes. The morphology of nanosuspensions was observed,then the particle sizes and polydispersity indices of nanosuspensions and freeze-dried powder were determined.RESULTS The optimal conditions were determined to be 6 ∶ 1 for ratio of diosgenin to Pluronic F127（ stabilizerⅠ）,50 ∶ 1 for ratio of diogenin to sodium dodecyl sulfate（ SDS,stabilizerⅡ）,1 ∶ 4 for ratio of preliminary nanosuspension volume to grinding bead amount,120 min for milling time,and 8% PEG-6000 and 2% mannitol as lyoprotectants. The average particle size and polydispersity index of rod-like or flaky nanosuspensions were（ 348. 1 ±14. 2） nm and 0. 244 ± 0. 059,respectively,which were lower than those of freeze-dried powder. At room temperature,the particle sizes of nanosuspensions and freeze-dried powder remained stable within 35 d and 3 months,respectively. CONCLUSION The physical stability of diosgenin freeze-dried powder is superior to that of its nanosuspensions,which can be used after being reconstituted.

关 键 词： 薯蓣皂苷元 纳米混悬液 介质研磨 冷冻干燥 单因素试验