阳离子交换树脂——HPLC法测定伊立替康脂质体包封率

Determination of the Entrapment Efficiency of Irinotecan liposomes by cation Exchange resin-HPLC

目的建立一种简单有效的伊立替康脂质体包封率测定方法。方法以阳离子交换树脂法分离游离的伊立替康和脂质体，HPLC法测定脂质体中伊立替康的含量，岛津c18（4．6×250mm，5μm，pH为40的甲醇-乙腈-磷酸盐缓冲液（55：5：45，加入三乙胺10mL，磷酸调节pH）为流动相，流速为1．0mL／min．检测波长为254nm，测定包封率。结果阳离子交换树脂对溶液中伊立替康的吸附率达到100％，对空白脂质体和伊立替康物理混合物的中的伊立替康吸附率达到100％。在01—20μg／mL范围内含量测定方法的线性关系良好，精密度RSD小于1．3％，平均回收率为99．87％。结论采用阳离子交换树脂-HPLC方法用于分离、测定脂质体包封率准确可靠、简便可行、重现性好，符合制剂的分析要求。

Abstact： Objective To establish cation exchange resin-HPLC method for the determination of the entrapment efficiency of Irinotecan liposomes. Methods The free Irinotecan from the liposomes separated by Cation exchange resin. The entrapment efficiency of Irinotecan liposomes was determined by HPLC. HPLC conditions were as follows： C18 column （4.6×250mm, 5μm）, the mobile phase consisted of methanol-acetonitrilephosphate （55：5：45） added triethylamine 10 mL（pH 4.0）, the flow rate 1.0mL/min, the detection wavelength 254 nm. Resμt By flowing through the cation exchange resin,Irinotecan in solution was absorbed completely, in the mixture of blank liposomes and Irinotecan, Irinotecan was absorbed completely too. The calibration curve was liner （r=0.999 8） with the range of 0.1-20μg/mL for Irinotecan. The precision RSD was less than 1.3%. The average recovery of Irinotecan with blank liposomes was 99.87%. Conclusion The method used to separate and determine the entrapment efficiency of Irinotecan was feasible, quick, accurate and efficiency. Key words： liposomes; entrapment efficiency; cation exchange resin; Irinotecan