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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 synthetic conditions of PEG-PUE derivatization. Methods The PEG-PUE mass fraction, drug loading and yield were used as the evaluation indexes. The ratio of PEG to PUE, the amount of DMAP and the reaction time were optimized by HPLC. Results The optimum synthetic conditions of PEG-PUE derivatization were that the ratio of PEG-EDC-PUE-DMAP substance was 1: 1.2: 1.2: 0.3 and the reaction time was 12 h. Conclusion The optimum synthesis conditions of PEG-PUE derivatization are reasonable and feasible.