高等学校化学学报

高等学校化学学报 ›› 1997, Vol. 18 ›› Issue (10): 1706.

• 论文 • 上一篇    下一篇

主链含膦酸酯的聚酸酐药物控制释放材料研究

傅杰, 卓仁禧, 范昌烈   

  1. 武汉大学化学系, 武汉 430072
  • 收稿日期:1995-08-29 出版日期:1997-10-24 发布日期:1997-10-24
  • 通讯作者: 卓仁禧
  • 作者简介:傅杰, 女, 33岁, 博士研究生, 武汉工业大学讲师.
  • 基金资助:

    国家自然科学基金

Studies on the Syntheses and Drug Release Properties of Polyanhydrides Containing Phosphonoformic(or Acetic)Acid Ethyl Ester in the Main Chain

FU Jie, ZHUO Ren-Xi, FAN Chang-Lie   

  1. Department of Chemistry, Laboratory Of Biomedical Polymer Materials of the StateEducation Commission of China, Wuhan University, Wuhan 430072
  • Received:1995-08-29 Online:1997-10-24 Published:1997-10-24

PDF (PC)

被引次数

10

摘要： 通过二氯膦甲(乙)酸乙酯与对羟乙氧基苯甲酸反应,制备了二羧苯氧乙氧基膦甲(乙)酸乙酯,将其转化成混合醋酐并通过熔融缩聚,合成了主链含膦甲(乙)酸乙酯的聚酸酐.以二羧苯氧乙氧基膦甲(乙)酸乙酯,分别与1,3-双(4－羧基苯氧基)丙烷(CPP)及癸二酸(SA)共聚,得到相应的共聚酸酐.对所合成的单体和聚合物的结构进行了表征.研究了它们的体外降解、酶促降解及其对抗肿瘤药物5-氟尿嘧陡和氨甲蝶呤的释放性能.

关键词: 聚酸酐, 药物控制释放材料, 5－FU, MTX

Abstract: Polyanhydrides were synthesized by melt polymerization of his (p--carboxyphenyloxy ethoxy), phosphonoformic (or acetic) acid ethyl ester 1(or 2). Copolyanhydrides weresimilarly prepared from 1 (or 2) and his(p--carboxyphenoxy)propane (CPP), or sebacic acid(SA). The chemical stru ctures of these new polyanhydrides and copolyanhydrides wereconfirmed by 1H NMR, FTIRand elemental analysis. The average molecular weight of thesepolymers was investigated. In vitro degradation of polyanhydrides and copolyandhydrides inphosphate buffer solution at 37 oC was monitored by HPLC. Experimental data revealed thatfission of phosphate bond took place after that of the anhydride bond. Enzymatic degradationshowed that Ribonuclease could catalyze and accelerate the degr adation of thesepolyanhydrides. Drug release profile of antitumor agents MTXand 5--Fu were also studied.

Key words: Polyanhydride, Drug controlled release material, 5-Fu, MTX

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