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-IPLA-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)