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目的采用Box-Behnken实验设计方法,对穿心莲内酯微球处方进行优化。方法以聚乳酸羟基乙酸(PLGA)为药物载体,采用溶剂挥发法制备穿心莲内酯微球。分别以PLGA质量浓度、聚乙烯醇(PVA)质量浓度、油水相体积比为考察对象,以载药量和包封率为评价指标,采用Box-Behnken效应曲面法筛选穿心莲内酯微球的最佳处方。结果穿心莲内酯微球的最优处方为PLGA为0.20 g/mL,PVA为18 mg/mL,油水相体积比为1∶90(0.011),所得微球的载药量为(47.21±2.36)%,包封率为(90.15±3.48)%,与模型预测值接近。结论 Box-Behnken实验设计可用于穿心莲内酯微球的处方优化筛选。
Objective To optimize the formulation of andrographolide microspheres by Box-Behnken experimental design. Methods Poly (D, L - lactic acid) glycolic acid (PLGA) was used as drug carrier to prepare andrographolide microspheres by solvent evaporation. The mass concentration of PLGA, the concentration of polyvinyl alcohol (PVA) and the volume ratio of oil-water phase were investigated respectively. The drug loading and entrapment efficiency were used as indexes to evaluate the effects of Box-Behnken effect surface method on the screening of andrographolide microspheres Good prescription. Results The optimal formulation of andrographolide microspheres was 0.20 g / mL for PLGA, 18 mg / mL for PVA and 1:90 (0.011) for volume ratio of water to oil. The drug loading of the obtained microspheres was (47.21 ± 2.36) %, Encapsulation efficiency (90.15 ± 3.48)%, close to the model predictive value. Conclusion The Box-Behnken experimental design can be used to optimize the formulation of andrographolide microspheres.