目的 筛选溶剂蒸发法制备九节龙皂苷I聚乳酸微球（ADS-I-PLA-MS）最佳工艺。方法 采用HPLC-ELSD测定方法，以包封率和载药量为评价指标，W/O/W溶剂蒸发法制备微球；通过单因素和正交试验设计，考察内水相九节龙皂苷I（ADS-I）甲醇溶液的质量浓度、ADS-I甲醇溶液与聚乳酸（PLA）二氯甲烷溶液体积比、PLA二氯甲烷溶液质量浓度和聚乙烯醇（PVA）体积等因素对ADS-I-PLA-MS包封率及载药量的影响。结果 溶剂蒸发法制备ADS-I-PLA-MS的最佳工艺条件为ADS-I甲醇溶液质量浓度为8 mg/mL、ADS-I甲醇溶液与PLA二氯甲烷溶液体积比为1∶13、PLA二氯甲烷溶液质量浓度为90 mg/mL、PVA体积为500 mL。结论 优选出的ADS-I-PLA-MS制备工艺合理可行。

Objective To select the optimum conditions for the preparation of ardipusilloside-I polylactic acid microspheres (ADS-I- PLA-MS) by solvent evaporation method. Methods HPLC-ELSD was used for the evaluation with encapsulation efficiency (EE) and drug loading as indexes. Microspheres were prepared using W/O/W evaporation method. Through single factor and orthogonal tests, the effects of the concentration of inner-water ADS-I methanol solution, volume ratio of ADS-I methanol solution-PLA methylene chloride solution, concentration of PLA methylene chloride solution, and the volume of polyvinyl alcohol (PVA) on EE and drug loading were investigated. Results The optimum conditions for the preparation of ADS-I-PLA-MS were as follows: the concentration of ADS-I methanol solution 8 mg/mL, the volume ratio of ADS-I methanol solution-PLA methylene chloride solution 1∶13, the concentration of PLA methylene chloride solution 90 mg/mL, and the volume of PVA 500 mL. Conclusion This optimized ADS-I-PLA-MS preparation technology is reasonable and feasible.

国家自然科学基金面上项目（30973952）；陕西省资源主导型产业关键技术（链）项目（2011KTCL03-01）