目的 合成β-环糊精聚乙二醇羟基喜树碱高聚物（β-CD-PEG-HCPT）并研究其载药量。方法 以β-环糊精和4-4'联苯二磺酰氯为起始原料，通过酰化反应、碘代反应、取代反应、酰化反应得到聚乙二醇-β-环糊精（β-CD-PEG）。采用羟基喜树碱（HCPT）为起始原料，利用乙酰基对10位羟基进行保护，再利用二氯甲烷/甲醇/乙酰氯这种温和的系统脱去乙酰基，得到乙酰羟基喜树碱甘氨酸酯（Ac-HCPT-Gly）。β-CD-PEG和Ac-HCPT-Gly反应得到目标产物β-CD-PEG-HCPT。结果 合成了目标产物β-CD-PEG-HCPT，其结构通过¹H-NMR确证。HCPT的载药量是4.3%。结论 改进了β-CD-PEG-HCPT的合成工艺，操作简单、成本低、收率较高。

Objective To synthesize β-CD-PEG-HCPT and study its drug loading capacity. Methods β-Cyclodextrin (β-CD) and biphenyl-4,4'-disulfonyl chloride were used as the starting materials to synthesize β-CD-PEG by acylation reaction, iodination reaction, substitution reaction, and acylation reaction. HCPT was used as the starting materials, and 10-OH of HCPT was protected by the acetyl group and deprotected by the system of CH₂Cl₂/CH₃OH/acetyl chloride to synthesize Ac-HCPT-Gly. β-CD-PEG and Ac-HCPT-Gly were reacted to synthesize the target compound β-CD-PEG-HCPT. Results The target compound β-CD-PEG-HCPT was synthesized, and the structure has been confirmed by ¹H-NMR. The drug loading of HCPT was 4.3%. Conclusion This study improves the synthesis process ofβ-CD-PEG-HCPT with simple operation, low cost, and high yield.

国家自然科学基金资助项目（81360485、81560577）；江西省卫计委中医药课题（2017Z014、2017A322）；江西省教育厅科研课题（20181110）