摘要
目的:优选脱氧氟尿苷脂质体的制备工艺及建立其质量评价方法。方法:采用逆相蒸发法制备脂质体,并以包封率为参考指标,以处方中卵磷脂与胆固醇摩尔比(A)、有机相与水相体积比(B)、脱氧氟尿苷浓度(C)、磷酸盐缓冲液pH值(D)为因素通过正交试验优选该脂质体的处方,并对脂质体粒径、包封率、稳定性、体外释药情况等进行考察。结果:最佳处方为A2:1、B5:1、C2mg.mL-1、D7.0。以此处方制备的脂质体平均粒径231nm,包封率(52.22±1.30)%,贮藏49d稳定性较好,与脱氧氟尿苷溶液比较具有明显的缓释性。结论:建立的脱氧氟尿苷脂质体制备方法简便、可行,以优选处方制备的脂质体质量符合要求。
OBJECTIVE： To optimize the preparation technology of doxifluridine （DFUR） liposomes and establish its quality evaluation method. METHODS： The DFUR liposomes were prepared by reverse phase evaporation technique using entrapment efficiency as index, the optimal formulation of liposomes was determined with mole ratio of lecithin to cholesterin （A）, volume ratio of organic phase to water phase （B）, DFUR concentration （C） and the pH of buffer phosphate （D） as factors, and the particle size, entrapment efficiency, stability and in vitro drug release were investigated as well. RESULTS： The optimal formulation was as follows： A was 2 ： 1, B was 5 ： 1, C was 2 mg · mL ^-1 and D was 7.0. Under this formulation, the mean diameter of the liposomes was 231 nm and the entrapment efficiency was （52.22 ± 1.30） %, and the liposomes were stable within 49 days and marked by sustained - release as compared with DFUR solution. CONCLUSION ： The operation of prepa- ration is simple and feasible, and the optimized liposomes were up to the standard.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第31期2439-2441,共3页
China Pharmacy
基金
吉林大学“大学生创新性实验计划”资助项目(2008C73202)
关键词
脱氧氟尿苷
脂质体
制备
质量评价
包封率
Doxifluridine
Liposomes
Preparation
Quality evaluation
Entrapment efficiency
