正交实验法优选舒芬太尼固体脂质纳米粒制备工艺

Preparation of Sufentanil solid lipid nanoparticles optimized by orthogonal experiment

目的:优化舒芬太尼固体脂质纳米粒配方及制备工艺条件。方法:选择影响工艺条件的舒芬太尼的用量(A)、表面活性剂的浓度(B)、固体脂质的含量(C)、硬脂酸和卵磷脂的比例(D)为四个因素,每个因素选取三个水平,以粒径为主要评价指标,按L9(34)正交试验设计表进行工艺筛选实验。结果:通过对各配方的综合评价研究得出理想配方为舒芬太尼用量为100μg,F68浓度为1.5%,药脂比为1∶100,硬脂酸与卵磷脂的比值为5∶1。结论:根据正交实验结果制备的舒芬太尼固体脂质纳米粒在粒径方面符合要求,且在稳定性、外观方面均较理想。

Objective： To optimize the formulation and preparation condition of the Sufentanil solid lipid nanopartcles（ SUF-SLN）. Methods： Four influence factors on the preparation condition of the SUF-SLN,including the dosage of Sufentanil（ A）,the concentration of surfactant（ B）,the content of solid lipid（ C） and the ratio of stearic acid and lecithin（ D）,were evaluated in the study. Three levels of each factor were selected,and the particle size was the major evaluation index. The screening experiment on the SUF-SLN preparation was performed based on the L9（ 34） orthogonal experimental table. Results： The optimal formulation of SUF-SLN processed by comprehensive evaluation and statistical analysis was 100 μg Sufentanil dosage,1. 5% F68 concentration,1∶ 100 ratio of the drug and the lipid,and 5： 1 ratio of stearic acid and lecithin. Conclusion： The SUF-SLN prepared by orthogonal experiment fulfills the criteria of the particle size,with optimal stability and appearance.