逆相蒸发法结合响应面优化抗耐药结核菌药物利奈唑胺脂质体处方工艺研究  

Prescription and preparation research of optimizing linezolid liposome,a drug against drug-resistant tuberculosis using reverse-phase evaporation method combined with response surface

作　　者：佟雷[1] 刘金丽 刘世娟 于春艳 TONG Lei;LIU Jinli;LIU Shijuan;YU Chunyan(Department of Pharmacy Teaching and Research Office,Mudanjiang Medical College,Mudanjiang157000,China;Department of Infectious Disease,Hongqi Hospital Affiliated to Mudanjiang Medical University,Mudanjiang157000,China;Department of Pharmacy,Hongqi Hospital Affiliated to Mudanjiang Medical University,Mudanjiang157000,China)

机构地区：[1]牡丹江医学院药剂学教研室,黑龙江牡丹江157000 [2]牡丹江医学院附属红旗医院感染科,黑龙江牡丹江157000 [3]牡丹江医学院附属红旗医院药学部,黑龙江牡丹江157000

出　　处：《中国现代医生》2020年第6期37-41,I0001,共6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(生物医药类支持计划项目,2018-KYYWFMY-0064)。

摘　　要：目的通过逆相蒸发法制备抗结核药物利奈唑胺脂质体,并利用响应面法优化其制备工艺和处方组成。方法以包封率为主要指标进行单因素试验,以Box-Behnken响应面分析法优化其制备工艺。并将最优工艺下制得的利奈唑胺脂质体于倒置荧光显微镜下观察其形态。结果通过逆相蒸发法制备利奈唑胺脂质体的包封率较高;最佳制备工艺:胆固醇-卵磷脂质量比为1:2.45,缓冲液pH值为6.65,超声时间为3.2 min,旋转蒸发仪转速为50 r。结论逆相蒸发法的制备工艺简单,重现性好,所得包封率高。Objective To prepare antituberculous drug linezolid liposome using the reverse-phase evaporation method,and optimize its preparation process and prescription composition using the response surface method.Methods Single-factor experiment was performed with the entrapment rate as key indicators,and Box-Behnken response surface analysis was used to optimize the preparation process.The linezolid liposome prepared using the optimal preparation process was observed for morphology by inverted fluorescent microscope.Results It was found that the entrapment rate of linezolid liposome prepared using the reverse-phase evaporation method was relatively high;under the optimal preparation process,the mass ratio of cholesterol to lecithin was 1:2.45,the pH value of the buffer solution was 6.65,the ultrasonic time was 3.2 min,and the rotation speed of the rotary evaporator was 50 r.Conclusion The reverse-phase evaporation method has the advantages of simple preparation process,good reproducibility and high entrapment rate.

关 键 词：利奈唑胺脂质体 逆相蒸发法 包封率 Box-Behnken响应面分析法 

分 类 号：R52[医药卫生—内科学]