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

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。

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

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 Singlefactor 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.