薛玉英, 翁帼英. 阿糖腺苷脂质体的制备及其稳定性J. 药学学报, 1992, 27(1): 74-80.
引用本文: 薛玉英, 翁帼英. 阿糖腺苷脂质体的制备及其稳定性J. 药学学报, 1992, 27(1): 74-80.
YY Xue, GY Weng. THE PREPARATION AND STABILITY OF LIPOSOMEENCAPSULATED ARA-AJ. Acta Pharmaceutica Sinica, 1992, 27(1): 74-80.
Citation: YY Xue, GY Weng. THE PREPARATION AND STABILITY OF LIPOSOMEENCAPSULATED ARA-AJ. Acta Pharmaceutica Sinica, 1992, 27(1): 74-80.

阿糖腺苷脂质体的制备及其稳定性

THE PREPARATION AND STABILITY OF LIPOSOMEENCAPSULATED ARA-A

  • 摘要: 本文比较了薄膜法、反相蒸发法、冰冻熔融法制备Ara-A脂质体的包裹率,采用正交设计法摸索Ara-A脂质体制备的最佳技术条件,利用自行设计的改良冰冻熔融法将难溶性药物Ara-A研制成脂质体,其包裹率可达约50%,为国外文献报道的采用反相蒸发法所制得的Ara-A脂质体的包裹率(5.2±0.9%)的10倍。本法操作简单、重现性好。本文还考察了Ara-A脂质体的物理和化学稳定性,实验表明:Ara-A脂质体采用100℃30min灭菌的方法,制品的形态、粒度分布、包裹率及含量均无明显改变,经恒温加速试验,表明Ara-A脂质体具有一定的化学稳定性。

     

    Abstract: This paper uses several preparation methods, such as thin - film, reverse-- phase evaporation and freeze - thawing methods, and also comparesencapsulation percen-tage of Ara - A in liposome (EN%) of these methods. The best operational conditions ofpreparing liposome-encapsulated Ara-A are explored. A higher EN%,about 50%,which is ten times that reported in foreign literature, is obtained by using improved freeze-thawing method, and this method is easy to operate and repeatable. At the same time, thephysical and chemical stabilities of the liposome - encapsulated Ara - A were observed. Theresult shows that there are no distinct changes in shape, size distribution of liposome, andEN% as well as Ara - A contained in liposome by means of sterilization at 100℃ for 30minutes. Accelerating test at a constant temperature indicates that liposome-entrapped Ara - A has certain chemical stability.

     

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