紫杉醇脂质体药物含量及包封率的测定  

Determination of content and entrapment efficiency of paclitaxel loaded liposome

作　　者：杨涛[1,2] 金大德[2] 崔福德[1] 

机构地区：[1]沈阳药科大学药剂教研室,沈阳110016 [2]首尔国立大学药学院,首尔韩国151-742

出　　处：《药物分析杂志》2008年第2期231-234,共4页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:建立紫杉醇脂质体含量及包封率的测定方法。方法:采用 RP-HPLC 法,LiChrospher 100反相 C_(18)(250 mm×4.6mm,5μm)色谱柱,乙睛-水(50:50)为流动相.流速为1.0 mL·min^(-1),紫外检测波长为227 nm,柱温为室温。利用混合有机溶剂对紫杉醇脂质体进行破坏,直接用 HPLC 法确定紫杉醇的含量。采用低速和超速离心法相结合的方法分离游离药物,确定脂质体中紫杉醇的包封率。结果:在脂质体平均粒径不到200 nm 的条件下,通过离心法可以将游离紫杉醇与脂质体完全分离。紫杉醇与辅料及溶剂峰分离良好,线性范围为0.04～1.0μg·mL^(-1);研究了负电荷对紫杉醇脂质体的作用,发现1%的磷脂酰丝氨酸(PS)能够提高紫杉醇的含量到(23.6±1.0)μg·mg^(-1),提高紫杉醇脂质体的包封率到(86.0±1.8)%。结论:所用方法简便、准确,可用于紫杉醇脂质体的含量及包封率测定。Objective：To develop a method for the determination of content and entrapment efficiency of paclitaxel loaded liposome. Methods：The separation of free paclitaxel from liposome was performed with a method combining low -speed centrifugation and uhracentrifugation method to determine the entrapment efficiency of paclitaxel -loaded liposome. After the liposome was destroyed by mixed organic solvent, the paclitaxel content in liposome was de- tected by RP - HPLC method at 227 nm and the flow rate of mobile phase was 1.0 mL · min^- 1 LiChrospher 100 RP- 18 column（250 mm ×4. 6 mm,5 μm）was used as analytical column and the mobile phase was composed of acetonitrile and water （50： 50） ,at room temperature. Results： The paclitaxel can be well separated from the liposome when the mean particle size of liposome was less than 200 nm. The effect of negative charge on the paclitaxel -loaded liposome was studied, which showed that 1% phosphatidylserine （PS） can increase the paclitaxel content in freeze - dried liposome powder to （23.6 ± 1.0） μg · mg^- 1 and the entrapment efficiency of paclitaxel to （86.0 ＋ 1.8） %, respectively. Conclusion： The method is accurate and can be used to determine the content and entrapment efficiency of paclitaxel loaded liposome.

关 键 词：紫杉醇 脂质体 包封率 

分 类 号：R917[医药卫生—药物分析学]