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采用溶剂蒸发法制备了多杀菌素·甲氨基阿维菌素苯甲酸盐聚乳酸微球,考察了内相聚乳酸浓度(X1)、理论载药量(X2)和搅拌速率(X3)对微球载药量、包封率、粒径、跨距及5 d释放率的影响。用数学方法将试验设计中的多指标“归一”化,采用中心多点等距设计法,对各指标以及总评“归一值”进行二项式拟合,描绘三维效应面,用Design-expert V8.06软件对总评“归一值”较佳的试验条件进行预测。结果表明,当聚乳酸质量浓度和搅拌速率减小、以及理论载药量增大时,总评“归一值”增大。经预测,当聚乳酸质量浓度为77.79 mg/mL、理论载药量(质量分数)为51.06%、搅拌速率为560.91 r/min时,总评“归一值”理论值达到最大(0.681 1)。依据上述较佳条件制备的微球总评“归一值”实测值为0.630 8,与理论预测值的偏差为-5.03%,其中包封率为84.49%,粒径7.19μm,跨距为1.134,5 d释放率为52.95%。微球表面光滑,DSC测试结果表明,其有效成分与微球骨架结合完好。表明研究建立的数学模型可用来预测多杀菌素·甲氨基阿维菌素苯甲酸盐聚乳酸微球的较优配方。
The spinosad / emamectin benzoate polylactic acid microspheres were prepared by solvent evaporation method. The effects of internal phase polylactic acid concentration (X1), theoretical drug loading (X2) and stirring rate (X3) Ball drug loading, entrapment efficiency, particle size, span and 5 d release rate. Mathematical methods are used to test the multi-index in the experimental design, and the central multi-point equidistant design method is used to perform binomial fitting on each index and the generalized “normalized value” to describe the three-dimensional effect surface , Design-expert V8.06 software for the general rating “normalized value ” better test conditions are predicted. The results showed that when the mass concentration of polylactic acid and stirring rate decreased, and the theoretical drug loading increased, the overall rating “normalized value” increased. It is predicted that the theory of “normalized value” reaches the maximum when the concentration of polylactic acid is 77.79 mg / mL, the theoretical loading (mass fraction) is 51.06% and the stirring rate is 560.91 r / min ). The average value of “normalized value” of the microspheres prepared according to the above optimal conditions was 0.6308, which was -5.03% of the theoretical value. The entrapment efficiency was 84.49%, the particle size was 7.19μm and the spans were The release rate of 1.134,5d was 52.95%. The surface of the microspheres is smooth, and the DSC test results show that the active components are well bonded with the microsphere framework. The results show that the mathematical model established by this study can be used to predict the optimal formulation of spinosad-emamectin benzoate polylactic acid microspheres.