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 formula of andrographolide-loaded PLGA microsphere. Methods The microspheres were prepared by the solvent evaporation method using PLGA as drug carriers. The effects of the concentration of PLGA and PVA, and the oil-water phase ratio were investigated. According to the drug loading amount and encapsulation efficiency, the formula was optimized by Box-Behnken design and response surface method. Results The optimal formula was as follows: PLGA concentration of 0.20 g/mL, PVA concentration of 18 mg/mL, and oil-water phase ratio of 1∶90, respectively. The drug loading amount of the microsphere was (47.21 ± 2.36)% and the encapsulation efficiency was (90.15 ± 3.48)%, which were very close to the predicted values. Conclusion It is effective and feasible to apply Box-Behnken design and response surface method for the formula optimization of the andrographolide-loaded PLGA microsphere.

烟台大学青年学术骨干培养项目资助（2012）