α-细辛脑长循环脂质体冻干工艺的研究

Study on freeze-drying process of the long-circulated lyophilized liposome of α-asarone

采用乙醇注入法制备α-细辛脑长循环脂质体,以冻干后的外观和再分散性作为筛选冻干保护剂的评价指标,确定以蔗糖和甘露醇联用作为冻干保护剂,两者的配比为糖∶醇=3∶7,总含量为20%.以冻干率为评价指标,通过正交试验对冻干工艺参数进行优化,确定冻干曲线中预冻温度为-50℃,预冻时间为9 h;升温时间为9 h;主升华干燥温度为-30℃,维持12 h,压力为15 Pa;之后以5℃/h的速度升温;解析干燥温度为35℃,维持5 h,压力为10 Pa.制备的α-细辛脑长循环脂质体冻干工艺重复性、稳定性好,生产可行性高.

α-asarone liposomes were prepared by ethanol injection. The appearance and redispersibility of freezedried α-asarone liposomes were selected as evaluation indexes for lyophilization protectant, the combination of saccharose and mannitol was used as a freeze-drying protective agent. The cryoprotective was 20% saccharose- mannitol （3 ： 7） and the optimum process of freeze-drying was ： pre-freeze for 9 h at -50℃, the heating-up time was 9 h; primary-drying for 12 h at -30℃, vacuum was 15 Pa; the temperature of desorption was 35℃ and maintaining 5 h, vacuum was 10 Pa. Stable α-asarone long-circulated lyophilized liposome could be obtained by screening cryoprotectives and optimizing freeze-drying process parameters and the physicochemical characters were good. The confirmatory test has proofed the feasibility and stability of the process.