树状大分子聚酰胺-胺的合成及对药物分子增溶性能研究

Synthesis of dendrimer polyamidoamine and solubility enhancement of drug in its solution

采用发散法合成了以乙二胺为核的1.0～3.0树状大分子聚酰胺-胺(PAMAM).采用红外光谱和核磁共振对PAMAM的结构进行了表征,并考察了不同pH值、不同浓度的PAMAM对难溶药物布洛芬的增溶能力.结果表明:PAMAM较十二烷基苯磺酸钠(SDS)对布洛芬有较强的增溶能力,增溶量随PAMAM浓度增加而增大,其增溶机理是由于PAMAM的氨基与布洛芬的羧基之间存在静电作用.

A series of dendrimic polyamidoamine(PAMAM) has been synthesized by divergent with ethylenediamine as core. The dendrimers were characterized with IR, NMR and terminal analysis. The study investigated the effect of pH and concentration of the dendrimers on the solubility enhancement of ibuprofen. The solubility of the hydrophobic drug ibuprofen has been compared in an aqueous solution of PAMAM G3 dendrimer and sodium dodecyl sulphate(SDS). The PAMAM G3 dendrimer solution significantly enhanced the solubility of ibuprofen compared to 20 g/L SDS solution. Its solubilizing mechanism involves an electrostatic interaction between the carboxyl group of the ibuprofen molecule and the amine groups of the dendrimer molecule.