应用溶剂注入法制备抗耐药结核菌药物利奈唑胺脂质体的实验研究  

Experimental study on preparation of linezolid liposomes against drug-resistant tuberculosis by solvent-injection method

作　　者：刘金丽 佟雷[2] 于春艳 刘军宏 王丽颖 LIU Jinli;TONG Lei;YU Chunyan;LIU Junhong;WANG Liying(Department of infection,Hongqi Hospital Affiliated to Mudanjiang Medical University,Mudanjiang157011,China;School of Pharmacy,Hongqi Hospital Affiliated to Mudanjiang Medical University,Mudanjiang157011,China)

机构地区：[1]牡丹江医学院附属红旗医院感染科,黑龙江牡丹江157011 [2]牡丹江医学院药学院,黑龙江牡丹江157011

出　　处：《中国现代医生》2020年第4期33-36,F0003,共5页China Modern Doctor

基　　金：黑龙江省省属高等学校基本科研业务费科研项目(2018-KYYWFMY-0064)。

摘　　要：目的利用乙醇注入法制备利奈唑胺脂质体,并通过响应面法优化处方及工艺。方法单因素考察优选出主要影响因素并联合Box-Behnken响应面法分析筛选出最佳处方及工艺,并以此工艺制备载药脂质体。使用倒置荧光显微镜对最佳工艺条件下制备的利奈唑胺脂质体进行形貌观察。结果最佳工艺为:胆固醇与卵磷脂的质量比1:3、类脂注入缓冲液速度1.2 mL/min、超声时间3 min。包封率82.36%,RSD=1.32%,显微镜观察利奈唑胺脂质体粒径较均一,形态圆整。结论乙醇注入法制备利奈唑胺脂质体具有较高的包封率,Box-Behnken响应面法可快速全面选取最佳制备工艺,方便准确。Objective To prepare linezolid liposome using ethanol injection method and optimize its prescription and preparation using the response surface method.Methods Single-factor experiment was used to select main influencing factors,and Box-Behnken response surface analysis was combined to find the optimal prescription and preparation.The linezolid liposome prepared using the optimal preparation process was observed for morphology by inverted fluorescent microscope.Results Under the optimal preparation process,the mass ratio of cholesterol to lecithin was 1:3,the velocity of lipoid buffer injection was 1.2 mL/min,and the ultrasonic time was 3 min;the entrapment rate was 82.36%,RSD=1.32%.Under microscopic observation,the particle diameter of linezolid liposome was uniform,and the morphology was round.Conclusion The entrapment rate of linezolid liposome prepared by the ethanol injection method is relatively high,and the Box-Behnken response surface method can quickly and comprehensively select the optimal preparation process,which is convenient and accurate.

关 键 词：耐药结核菌 利奈唑胺脂质体 乙醇注入法 响应面法 包封率 

分 类 号：R944[医药卫生—药剂学]