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以酮洛芬为模型药物,研究聚酰胺-胺(PAMAM)树状大分子对酮洛芬的增溶作用,并探讨其作用机理.采用紫外光谱法测定了G1.0、G1.5、G2.0、G2.5、G3.0、G3.5PAMAM在不同浓度和不同pH时对酮洛芬的增溶量.并运用计算机模拟方法对PAMAM与酮洛芬相互作用的机理进行了探讨.实验结果表明,酮洛芬的溶解度随溶液pH值变化而变化,在pH4.0~6.0范围内,PAMAM树状大分子对酮洛芬的增溶量随着PAMAM的代数、浓度和溶液pH的增加而增大.整代和半代都具有增溶作用.然而,在同一pH条件下,对于具有相同官能团数目的整代和半代,整代增溶效果要高于半代.计算机模拟结果表明PAMAM与酮洛芬主要靠静电作用力结合.增溶机理可能是酮洛芬的羧基与PAMAM的伯胺和叔胺发生静电作用.
Ketoprofen was used as a model drug to study the solubilization of ketamine by polyamide-amine (PAMAM) dendrimer and its mechanism of action.Ultraviolet spectroscopy was used to determine the effect of G1.0, G1.5, G2 .0, G2.5, G3.0, G3.5PAMAM solubilization of ketoprofen at different concentrations and pH, and the mechanism of the interaction between PAMAM and ketoprofen was also discussed by computer simulation.Experiment The results showed that the solubility of ketoprofen changed with the pH value of the solution, and the solubilization of ketoprofen with PAMAM dendrimer increased with the increase of PAMAM algebra, concentration and solution pH in the range of pH 4.0 ~ 6.0 But increased at the same time.At the same pH condition, for the whole generation and half generation with the same number of functional groups, the whole-generation solubilization effect was higher than that of the half generation.Computer simulation results showed that PAMAM and Ketoprofen mainly by electrostatic force binding.The solubilization mechanism may be ketoprofen carboxyl and PAMAM primary amine and tertiary amine electrostatic interaction.