目的 优选葛根素聚乙二醇（PEG-PUE）衍生化的合成工艺条件。方法 以PEG-PUE的质量分数、载药量、收率为评价指标，采用HPLC法对PEG-PUE衍生化过程中PEG与PUE物质的量的比例、催化剂DMAP的用量、反应时间进行优选。结果 PEG-PUE衍生化的最佳合成工艺条件是PEG-EDC-PUE-DMAP物质的量的比例为1∶1.2∶1.2∶0.3，反应时间为12 h。结论 优选的PEG-PUE衍生化合成工艺条件合理，操作可行。

Objective To optimize the synthesis of PEGylated puerarin (PEG-PUE) by orthogonal test with multi-index evaluation. Methods The research has focused on the optimized interacting factors of the synthetic process of PEG-PUE by HPLC, such as ratio of PEG and PUE, catalyst DMAP dosage, and reaction time, using the purity, drug loading, and yield of PEG-PUE as evaluation indexes. Results The optimum synthesis conditions of PEG-PUE were as follows, PEG-EDC-PUE-DMAP (1 : 1.2 : 1.2 : 0.3) and reaction time 12 h. Conclusion The optimum synthesis condition of PEG-PUE is reasonable, as well as feasible.

科技部重大新药创制专项（2009ZX09502-007）