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[摘要]
目的 建立并优化人参皂苷Re(Re)脂质体制备工艺,提高Re脂质体贮藏稳定性。方法 薄膜分散-机械震荡法制备Re脂质体,透析法分离脂质体与未包封的游离药物,HPLC法测定包封率,冷冻干燥技术制备冻干脂质体制剂;以包封率为主要筛选指标,采用正交试验设计优选脂质体处方及冻干工艺。结果 薄膜分散-机械震荡法制备的Re脂质体包封率最高,最佳处方工艺为药物与磷脂质量比1:30,磷脂与胆固醇质量比16:1,冰水浴超声30 min,双蒸水为水化液;最佳冻干工艺为以蔗糖为冻干保护剂,二糖-水质量比为1:10,−;20℃为预冻温度,0.9%的生理盐水为再水化液。结论 Re脂质体制备工艺稳定可行,以蔗糖为冻干保护剂制得的Re脂质体各指标良好,显著延长贮存时间。
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[Abstract]
Objective To establish and optimize preparation technology of ginsenoside Re liposomes, therefore to improve storage stability. Methods Ginsenoside Re liposomes were prepared by the method of film dispersion-mechanical vibration, which were collected by separating liposome from disclosed free drug by dialysis method. Measure entrapment efficiency by HPLC. Prepare freeze-dried liposome preparations by freezing-drying technology. Taking entrapment efficiency as the main screening index, optimize liposome formulation and freezing-drying technology by orthogonal test design. Results The entrapment efficiency of ginsenoside Re lipidosomes prepared by the method of film dispersion-mechanical vibration is the highest. The best formulation technology is:Mass ratio of drug and phospholipid is 1:30, mass ratio of phospholipid and cholesterol is 16:1, ice-water bath ultrasound is 30 min, and double distilled water is hydration solution; The best freezing-drying technology is:Taking sucrose as the freeze-drying protective agent, mass ratio of disaccharide-water is 1:10, pre-freezing temperature is −20℃, and normal saline of 0.9% is reconstitution solution. Conclusion The preparation technology of liposome is stable and practicable. The ginsenoside Re liposome prepared by taking the sucrose as the freeze-drying protective agent has good indexes, which can extend the storage period.
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