摘要
作者选用α、β－聚（３－羟丙基）ＤＬ－天冬酰胺［α、β－ｐｏｌｙ（３－ｈｙｄｒｏｘｙｐｒｏｐｙｌ）ＤＬ－ａｓｐａｒｍｉｄｅ］（ＰＨＰＡ）这一可生物降解的高分子作为载体，将阿司匹林（ＡＳＡ）通过羧酸酯键与之结合成阿司匹林－聚天冬酰胺共价复合物（ＡＳＡ－ＰＨＰＡ）。将该复合物完全水解后，用紫外分光光度法测定水解产物水杨酸的含量。由此得出该复合物中阿司匹林的接入率为４０．７％（Ｗ／Ｗ）。我们还对该复合物在ｐＨ＝７．４，离子强度μ＝０．５的磷酸缓冲液中的释放作了研究。结果显示：该复合物释放８天后即以零级动力学平稳地释放，平均释放速率以水杨酸计算为２．２２±０．２５μｇ／１０ｍｇ高聚物·天。
Biodegradable α、β-(3-hydroxypropyl)D,L-asparamide was applied as a polymeric carrier to covalent aspirin. The rate of aspirin loading in the polymeric drug was 40.7% (W/ W)through the determination of content of the salicylic acid by UV-spectrophotometry,which was followed by complete hydrolysis of the polymeric drug. The in-vitro release of polymeric drug in phosphate buffer (pH=7.4,ionic strengthμ=0.5) was also studied. The results showed a constant release rate on the eighth day of the releasing experiment.The average release rate was 2.22±0.25μgSA/10 mg-polymer-day.
关键词
阿司匹林
聚天冬酰胺
化学合成
体外释放
Aspirin-polyasparamide/chem syn
Aspirin load rate
Release rate in vitro
