| 摘要: |
| 【目的】制备伊维菌素脂质体(IVML),并对其进行质量评价。【方法】 采用改良薄膜分散法制备IVML,选取卵磷脂与胆固醇质量比、伊维菌素(IVM)与卵磷脂质量比、缓冲液PBS的pH为配方影响因子,超声裂解时间、蒸发温度、冻融次数为制备工艺的影响因子,通过设计L9(34)正交试验对以上影响因子进行筛选。以筛选的最佳配方和工艺条件制备IVML,利用高速冷冻离心法测定其包封率,并对其理化性质和稳定性进行评价。【结果】 IVML的制备最佳配方和工艺为:卵磷脂与胆固醇质量比为9∶1,IVM与卵磷脂质量比为1∶10,缓冲液PBS的pH 为7.0;超声裂解5 min,蒸发温度40 ℃,冻融3次。所制备的IVML粒径为86~115 nm,平均粒径为(91.8±1.5) nm,包封率为(90.71±0.8)%(n=3),对热稳定,但对光不稳定。【结论】 得到了制备IVML的最佳配方和工艺,且制备工艺简单可行;IVML外观和质量浓度未发生明显变化,性质稳定。 |
| 关键词: 伊维菌素 脂质体 配方和制备工艺 质量评价 |
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| 基金项目:西藏农牧科学院科研基金资助项目(10-1) |
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| Preparation and quality evaluation of ivermectin liposome |
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| Abstract: |
| 【Objective】 The study was to prepare Ivermectin liposome(IVML) and evaluate its quality.【Method】 Modified thin film dispersion method was adopted to prepare the IVML,which was chosen for influencing factors of formula such as mass ratio of lecithin to cholesterol,mass ratio of Ivermectin(IVM) to lecithin,pH of PBS and of preparation technology such as freeze thawing times,ultrasonic time,evaporated temperature.These influencing factors were selected by orthogonal design L9(34),of which the optimum factors were adopted to prepare the IVML.High speed freezing centrifugation was used to determine its encapsulation efficiency and its characteristics and stability were evaluated. 【Result】 The optimal prescription for preparation of IVML were as follows:m(Lecithin)∶m(Cholesterol)=9∶1,m(IVM)∶m(Lecithin)=1∶10,pH of PBS 7.0,conducting ultrasonic toward 5 minutes,evaporating at 40 ℃,and freezing and thawing 3 times.Its diameter was distributed mainly in 86-115 nm and the average grain size was (91.8±1.5) nm. The encapsulation efficiency of prepared IVML reached (90.71±0.8)%(n=3),and it was stable for heat,but unstable for light.【Conclusion】 The optimal preparation technology of IVML,which was simple and feasible,was obtained.The outlook and content of IVML didn't change clearly and its quality was stable. |
| Key words: Ivermectin liposome prescription and preparation technology quality evaluation |