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纸质出版日期:2010-7-20,
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张怀敬, 何华, 吕燕妮, 顾艳, CHUONG Pham-Huy. PAMAM树状大分子对酮基布洛芬溶解度的影响[J]. 高分子学报, 2010,(7):876-883.
ZHANG Huaijing, HE Hua, LÜ, Yanni, GU Yan. EFFECTS OF PAMAM DENDRIMERS ON THE SOLUBILITY OF KETOPROFEN[J]. Acta Polymerica Sinica, 2010,(7):876-883.
张怀敬, 何华, 吕燕妮, 顾艳, CHUONG Pham-Huy. PAMAM树状大分子对酮基布洛芬溶解度的影响[J]. 高分子学报, 2010,(7):876-883. DOI: 10.3724/SP.J.1105.2010.09253.
ZHANG Huaijing, HE Hua, LÜ, Yanni, GU Yan. EFFECTS OF PAMAM DENDRIMERS ON THE SOLUBILITY OF KETOPROFEN[J]. Acta Polymerica Sinica, 2010,(7):876-883. DOI: 10.3724/SP.J.1105.2010.09253.
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、G3.5 PAMAM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pH 4.0~6.0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.
The aim of this study was to study the effect of polyamidoamine(PAMAM) dendrimers on the aqueous solubility of ketoprofen and investigate the mechanism of solubilization.PAMAM dendrimers of G1.0
G1.5
G2.0
G2.5
G3.0 and G3.5 were used as drug carriers of ketoprofen. The effects of pH and concentration of the dendrimers on the solubility of ketoprofen were studied by UV spectroscopy.In addition
the computational simulation was used to investigate the mechanism of interaction between PAMAM dendrimers and ketoprofen.Results showed that the pH
generation size
and concentration influenced the solubilization of ketoprofen.The solubility of ketoprofen increased with the increase of pH
generation size
and concentration of PAMAM dendrimers at pH 4.0~6.0.Both amino and ester terminated dendrimers caused the increase in ketoprofen solubility.However
at each pH
the solubility of ketoprofen was greater in the presence of amino-terminated dendrimers compared to the ester-terminated dendrimers possessing the same number of surface functional groups.The results of computational simulation show that interaction between ketoprofen and PAMAM dendrimers is mainly electrostatic force.Its mechanism of solubilization maybe an electrostatic interaction between the carboxyl group of ketoprofen and the primary amines or tertiary amines of PAMAM dendrimers.
PAMAM 树状大分子酮洛芬增溶作用
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