目的 优化新藤黄酸羟丙基－β－环糊精(HP－β－CD)包合物冻干粉针的制备工艺。方法 采用不饱和水溶液法，以L－精氨酸与新藤黄酸成盐助溶，制备新藤黄酸HP－β－CD包合物；采用冷冻干燥法制备新藤黄酸HP－β－CD包合物冻干粉针；HPLC法测定新藤黄酸的量；以包合率为指标，应用正交设计法优化制备工艺。结果 优化的制备工艺为HP－β－CD与新藤黄酸质量配料比为10∶1、20℃包合5 h；制备的包合物包合率高；包合物冻干粉色泽均匀、粉末蓬松、溶解性好。结论 工艺优化合理、重现性好。

Objective To optimize the preparation of gambogenic acid hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex of freeze-dried powder injection. Methods Gambogenic acid HP-β-CD inclusion complex of freeze-dried powder injection was prepared by freeze-drying method, gambogenic acid content was determined by HPLC, and the preparation was optimized by orthogonal design taking inclusion rate as index. Results The optimized preparation process for inclusion was that the reaction mass charge ratio (HP-β-CD-gambogenic acid) was 10∶1, for 5 h at 20 ℃. The inclusion rate of prepared inclusion complex was higher;The freeze-dried powder was with color uniformity, fluffy texture, and good solubility. Conclusion The process is reasonable and with good reproducibility.

国家重大新药创制专项(2009ZX09103-399)；安徽中医学院青年科学研究基金(2010qn005)