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聚缩醛药物载体的合成表征及其降解动力学的NMR研究

舒婕1, 彭敏1, 余家会2, 罗淑芳2, 俞磊2, 陈群1   

    1. 华东师范大学光谱学与波谱学教育部重点实验室,
    2. 新药创制先进技术研究院, 上海200062
  • 收稿日期:2006-11-04 修回日期:1900-01-01 出版日期:2007-07-10 发布日期:2007-07-10
  • 通讯作者: 余家会

Synthesis and Characterization of Polyacetals and NMR Study on Its Degradation Kinetics

SHU Jie1, PENG Min1, YU Jia-Hui2*, LUO Shu-Fang2, YU Lei2, CHEN Qun1   

    1. Key Laboratory of Optical and Magnetic Resonance Spectroscopy,
    2. College of New Drug Innovation Research & Development, East China Normal University, Shanghai 200062, China
  • Received:2006-11-04 Revised:1900-01-01 Online:2007-07-10 Published:2007-07-10
  • Contact: YU Jia-Hui

摘要:

在对甲苯磺酸催化下, 将聚乙二醇2000(PEG2000)和氨基保护的丝胺醇与三甘醇二乙烯基醚三元共聚, 再脱去丝胺醇的氨基保护基团, 合成了4种氨基含量不同的聚缩醛PA1, PA2, PA3和PA4, 用1H NMR表征了其结构. 同时, 利用1H NMR监测了聚缩醛PA3在pH值为7.4, 6.5和5.7的磷酸缓冲液及pH值为4.7, 4.1和3.8的醋酸缓冲液中的降解行为. 结果表明, PA3在酸性缓冲液介质中的降解反应符合一级反应动力学方程, 且随着介质pH值的减小降解速率常数增大, 降解半衰期减小.

关键词: 聚缩醛合成, 降解动力学, 一级动力学, 1H NMR

Abstract:

With p-TSA as catalyst, four different types of polyacetals(PA1, PA2, PA3, PA4) were synthesized with amino-protected serinol, tri(ethylene glycol) divinyl ether and PEG2000 in different molar ratios. The structure of the resultant polyacetal was characterized with 1H NMR.The degradation process of the copolymers was monitored via 1H NMR in pH=7.4, 6.5, 5.7 PBS and pH=4.7, 4.1, 3.8 acetic buffer, respectively. It was found that the degradation reaction in acidic buffer of PA3 obeyed the first order kinetics equation. With decreasing pH values of the buffer solution, the degradation rate constant increases and the half-life decreases.

Key words: Synthesis of polyacetals, Degradation kinetics, First order kinetics, 1H NMR

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