微柱离心-HPLC法测定枸橼酸他莫昔芬脂质体包封率的方法研究  

Determination of Encapsulation Efficiency of Tamoxifen Citrate Liposomes by Microcolumn Centrifugation-HPLC Method

作　　者：景莎莎 梁宇 门靖 何艳妮 JING Sha-sha;LIANG Yu;MEN Jing;HE Yan-ni(The Second Affiliated Hospital of Shaanxi University of Chinese Medicine,Xianyang 712000,China;Shenzhen Broadwell Environmental Technology Co.,Ltd.,Xi'an Branch,Xi'an 710000,China;Xi'an Wanlong Pharmaceutical Co.,Ltd.,Xi'an 710119,China;Xi'an International Medical Center Hospital,Xi'an 710100,China)

机构地区：[1]陕西中医药大学第二附属医院,陕西咸阳712000 [2]深圳市博德维环境技术股份有限公司西安分公司,陕西西安710000 [3]西安万隆制药股份有限公司,陕西西安710119 [4]西安国际医学中心医院,陕西西安710100

出　　处：《精细化工中间体》2024年第5期84-88,共5页Fine Chemical Intermediates

摘　　要：建立了枸橼酸他莫昔芬脂质体(TAM-LIPs)包封率的测定方法。采用薄膜分散法制备TAM-LIPs,用葡聚糖凝胶G-50填充微柱,以水为洗脱液,离心分离TAM-LIPs与游离药物后,通过高效液相色谱法(HPLC)测定枸橼酸他莫昔芬浓度并计算包封率,利用Box-Behnken效应面法优化微柱离心法测定条件。优化条件下,HPLC法能准确测定药物含量,洗脱曲线表明洗脱4次可以使载药脂质体完全被洗脱,可实现脂质体与游离药物良好分离,验证制备的3批TAM-LIPs包封率的RSD值满足方法学要求。建立的葡聚糖凝胶微柱离心-HPLC法测定结果准确,操作简单快捷,可用于TAM-LIPs包封率的准确测定。A method to determine the encapsulation efficiency of Tamoxifen citrate liposomes(TAM-LIPs)was established.TAM-LIPs were prepared by thin film dispersion method.The microcolumn was filled with Sephadex G-50 gel and water was used as the elution.After separation of TAM-LIPs and free drugs by centrifugation,the concentration of tamoxifen was determined by high performance liquid chromatography(HPLC)and the encapsulation efficiency(EE)was calculated.Then the experimental condition of microcolumn centrifugation method was optimized by Box-Behnken design.The drug content could be accurately determined by HPLC.The elution curve showed that the drug-loaded liposomes could be completely eluted for 4 times.Under the optimal conditions,the liposomes and free drugs could be separated to the ultmost extent.The RSD of three batches of TAM-LIPs were verified to meet the methodological requirements.The established microcolumn centrifugation-HPLC method was accurate and simple,which could be used to determine the EE of TAM-LIPs.

关 键 词：枸橼酸他莫昔芬脂质体 包封率 高效液相色谱法 BOX-BEHNKEN效应面法 微柱离心法 

分 类 号：TQ016.1[化学工程]