阿糖腺苷脂质体的制备及其稳定性

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。

THE PREPARATION AND STABILITY OF LIPOSOMEENCAPSULATED ARA-A

This paper uses several preparation methods, such as thin-film, reverse-phase evaporation and freeze-thawing methods, and also compares encapsulation percentage of Ara-A in liposome (EN%) of these methods. The best operational conditions of preparing 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, the physical and chemical stabilities of the liposome-encapsulated Ara-A were observed. The result shows that there are no distinct changes in shape, size distribution of liposome, and EN% as well as Ara-A contained in liposome by means of sterilization at 100 degrees C for 30 minutes. Accelerating test at a constant temperature indicates that liposome-entrapped Ara-A has certain chemical stability.