盐酸伊立替康脂质体的制备及包封率的测定  

Preparation of irinotecan hydrochloride liposomes and quantification of its entrapment efficiency

作　　者：李哲[1] 王绍宁[2] 黄微葳[1] 邓意辉[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2011年第9期687-690,720,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备盐酸伊立替康脂质体，建立包封率测定方法。方法采用乙二胺四乙酸铵梯度法制备盐酸伊立替康脂质体；以阳离子交换树脂离心法分离脂质体和游离药物；采用紫外可见分光光度法测定脂质体包封率。结果阳离子交换树脂柱对质量浓度为1．0—2．4g·L^-1伊立替康能够完全吸附，且对空白脂质体无吸附，空白脂质体回收率达99．73％；采用紫外可见分光光度法测定盐酸伊立替康含量，在372nm波长下，空白辅料对药物测定无干扰，盐酸伊立替康质量浓度在2．5～45．0mg·L^-1内线性关系良好（r=0．9999），精密度和回收率均符合要求；盐酸伊立替康脂质体包封率为95．4％。结论乙二胺四乙酸铵梯度法适用于制备盐酸伊立替康脂质体，所建立的分析方法简单快速，准确可靠，可用于盐酸伊立替康脂质体包封率的测定。Objective To prepare irinotecan hydrochloride（ CPT-11 ） liposomes and develop a method for the determination of its entrapment efficiency. Methods CPT-11 was encapsulated in the liposomes by ammonium ethylenediaminetetraacetate（ NH4EDTA） gradient method. Free CPT-11 and liposomes was separated by cation exchange resin. UV-visible spectrophotometry was applied to determine the entrapment efficiency. Results 1.0-2. 4 g.L^-1 CPT-11 was completely absorbed by cation exchange resin,while blank liposomes was not absorbed. The recovery rate of liposomes was 99. 73 %. In the conditions of the UV-visible spectrophotometry method, blank adjuvant could not interfere with determination of CPT-11 at 372 nm wavelength. The standard curve was linear over the range of 2. 5- 45.0 mg. L - 1 with the coefficient of 0. 999 9. The precision and recovery of the method accorded with the requirement. The entrapment efficiency of CPT- 11 liposomes by NH4EDTA gradient method was 95.4%. Conclusions The NH4EDTA gradient method is suitable for preparing CPT-11 liposomes. The method established in this study is simple, rapid and accurate for the determination of the entrapment efficiency of CPT-11 liposomes.

关 键 词：乙二胺四乙酸铵梯度法 盐酸伊立替康 脂质体 阳离子交换树脂柱离心法 包封率 

分 类 号：R94[医药卫生—药剂学]