氧化苦参碱脂质体的制备及其质量评价

目的:制备氧化苦参碱脂质体并建立其质量评价方法。方法:采用逆相蒸发法,以包封率为检测指标,利用正交试验法优选处方和制备工艺;考察优选处方所制脂质体形态与粒径,并采用透析法结合反相高效液相色谱法测定其包封率。结果:最佳处方为磷酸盐缓冲液pH7.2,大豆卵磷脂与胆固醇的质量比为2∶1,大豆卵磷脂与氧化苦参碱质量比为10∶1,水相与有机相体积比为1∶3;制备的脂质体为球状小囊泡,外观圆整,粒径范围60～150nm,包封率为60.72%;氧化苦参碱检测浓度线性范围为10～150μg.mL-1(r=0.9998),平均回收率为98.62%(RSD=1.47%,n=5)。结论:优选处方和制备工艺稳定可行,可为开发其新剂型提供参考。

Preparation of Oxymatrine Liposomes and Evaluation of the Quality

OBJECTIVE:To prepare oxymatrine liposomes and establish a quality evaluation method thereof.METHODS:The liposomes were prepared by reverse-phase evaporation technique.Served as quota with encapsulation efficiency of liposomes,the optimal formation and preparation were selected by an orthogonal design test.The encapsulation efficiency of liposomes was determined by RP-HPLC after liposomeswere being dialyzed.Transmission electron microscopy was performed for examining the appearances of liposomes and the diameter of the particles.RESULTS:The encapsulation efficiency and the diameter range of oxymatrine liposomes were 60.72% and 60nm～150nm,respectively.The average recovery was(98.62±1.45)%(RSD=1.47%).CONCLUSION:The selected formulation and preparation of oxymatrine liposomes is practicable.