阿斯匹林-壳聚糖偶联物的合成

文档编号:ZY050    文档字数:10737,页数:27

摘要： 为了改善阿司匹林药效，降低其毒副作用，研制出一种副作用低的缓释药物壳聚糖－阿司匹林偶联物。本文采用1-(3-二甲氨基丙基)-3-乙基碳二亚胺（EDC）和N-羟基琥珀酰亚胺（NHS）作为缩合剂，在室温常压下，合成阿司匹林－壳聚糖共价偶联物。该偶联物经过红外（IR）、紫外（UV）、差示扫描量热（DSC）分析，结构得到确证，经高效液相色谱测定偶联物的载药量为30.93%，阿司匹林转化率为21.70%。对制备的阿司匹林－壳聚糖共价偶联物进行初步吸湿性、pH稳定性的考察，偶联物在湿度在64.０%以上，吸湿明显；pH6.0~pH7.0之间相对稳定。
 关键词：阿司匹林，壳聚糖，偶联 
 
Abstract Objective: To improve the drug effect of aspirin, reduce its side effect, we sucessfully synthesize chitosan-aspirin conjugate with lower side effect．In this paper chitosan-aspirin was synthesized via EDC and NHS in normal pressure and room temperature. The product was characterized by FT-IR、UV and DSC. The drug-loading rate of product reached upto30.93% measured by HPLC and the conversion rate of aspirin reached upto 21.70%. Then we pilot studied the hygroscopicity and pH stability of the conjugate. The research results showed the humidity of the conjugate obvious increased in more than 64.0 percent moisture; the conjugate relatively was stable between.pH6.0 ~ pH7.0.
 Key Words:Chitosan;Aspirin ; Coupling inspect  
 目  录
中文摘要…………………………………………………………………………………………I
英文摘要 ………………………………………………………………………………………II
目录  …………………………………………………………………………………………III
1．绪论 …………………………………………………………………………………………1
    1.1 引言……………………………………………………………………………………1
 1.2阿司匹林概况   ……………………………………………………………………1
     1.3 甲壳素概况……………………………………………………………………… 2
     1.4立题依据……………………………………………………………………………6 
2.实验部分  …………………………………………………………………………………8
 2.1 实验仪器与试剂  …………………………………………………………………8
 2.2 壳聚糖-阿司匹林偶联物的合成………………………………………………… 9
 2.3偶联物的水解实验  ………………………………………………………………10
 2.4紫外光谱扫描  ……………………………………………………………………10
 2.5傅立叶转换红外线光谱表征………………………………………………………12
 2.6 差示扫描量法（DSC） ……………………………………………………………12
 2.7液相色谱分析……………………………………………………………………… 13                               
 2.8初步稳定性研究…………………………………………………………………… 13
3.  结果与讨论 …………………………………………………………………………… 15
 3.1 水解实验 …………………………………………………………………………… 17
 3.2偶联物结构表征……………………………………………………………………… 17
 3.3载药量分析…………………………………………………………………………  18
 3.4初步稳定性研究………………………………………………………………………19
4.  总结与展望 ………………………………………………………………………………20
致谢 ……………………………………………………………………………………………21
参考文献 ………………………………………………………………………………………2

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