目的 合成以三分枝六聚乙二醇為親水部分、以十二胺為疏水部分的新型兩親性分子三分枝六聚乙二醇接枝十二胺共聚物（PGDA），并對(duì)其理化性質(zhì)進(jìn)行考察。方法 通過(guò)苯磺?；?、取代反應(yīng)、還原反應(yīng)、酯化后形成酰胺5步反應(yīng)合成了PGDA。使用核磁和質(zhì)譜確定其結(jié)構(gòu)和相對(duì)分子質(zhì)量；芘熒光探針法測(cè)量其臨界膠束濃度；并考察PGDA在水溶液中的形態(tài)、37℃穩(wěn)定性。結(jié)果 兩親性分子PGDA被成功合成。質(zhì)譜實(shí)測(cè)相對(duì)分子質(zhì)量與理論相對(duì)分子質(zhì)量1 171.69吻合；該兩親性分子在水中很容易自組裝成膠束，臨界膠束濃度為75 mg/L；PGDA膠束37℃孵育24 h粒徑無(wú)明顯變化、穩(wěn)定性良好。結(jié)論 成功合成了三分枝六聚乙二醇為親水部分和以十二胺為疏水部分的兩親性分子PGDA，其在水溶液中具有優(yōu)良的膠束化行為，有望能作為一種藥用輔料在難溶性藥物的膠束等制劑中得到應(yīng)用。

Objective To synthesize a novel amphiphilic molecule branched polyethylene glycol-co-dodecylamine (PGDA) with branched hexa polyethylene glycol being as the hydrophilic segment while dodecylamine as the hydrophobic segment, and study its physicochmical property. Methods PGDA was successfully synthesized through acylation, substitution reaction, reduction reaction and esterification. The chemical structure was verified by NMR and MS analysis. The critical micelle concentrations (CMC) of PGDA were determined by pyrene fluorescence probe spectrometry. The morphology of PGDA in water was examined by transmission electron microscopy and the size of PGDA micelles at 37℃ was monitored to assess the stability. Results The amphiphilic molecule was successful synthesized. MS proved the molecular weight of the obtained PGDA was in accordance with the theoretical molecular weight of 1 171.69. PGDA could easily self-assembly into micelles in aqueous solution with critical micelle concentrations of 75 mg/L. The resultant micelles were quite stable after incubation at 37℃ with constant particle size. Conclusion The novel amphiphilic molecule PGDA is successfully synthesized, and its ability to easily self-assembly in aquesous solution which suggested that the resultant amphiphilic PGDA may be used as a pharmaceutical adjuvant, especially in micelles preparation for insoluble drugs.

國(guó)家自然科學(xué)基金-廣東聯(lián)合基金資助項(xiàng)目（U1401223）