右旋糖苷-阿司匹林高分子挂接药物的体外释放

为了评价不同载药率的右旋糖苷-阿司匹林高分子挂接药物在人工胃液和人工肠液中的体外释药性能,首先选择阿司匹林(ASA)在不同条件下的测定波长,绘制ASA的紫外吸收标准曲线和线性回归方程,并进行加样回收实验。通过固定温度及转速,做不同释放介质中的体外释药实验,评价其药学性能。结果表明,此药物在人工胃液和人工肠液中均呈零级释放,释药开始阶段无"爆释"现象,累积释药量随挂接药物载药量的增高而增高;挂接药物在人工肠液中的释放速率较其在人工胃液中快。此药物具有均匀缓慢释药的特性,而且能减轻ASA对胃粘膜的刺激作用。

Study of in vitro release of dextran-aspirin conjugate

The objective of this study is to evaluate in vitro release behavior of dextran-aspirin conjugates with different drug-loading ratios in artificial gastric juice and artificial intestinal juice. Wavelengths of aspirin in different media were detected first. Then the standard line of concentration to absorption was made to get the regression equation. The in vitro release study was carried out then in different release media under determinate temperature and rotating speed.The conjugates had a linear release of aspirin vs time with no abrupt release. And the release rate was nearly zero order. The release rate in artificial gastric juice was lower than that in artificial intestinal juice. The release rate enhanced with the increase of the drug-loading ratio. The dextran-aspirin conjugate is stable in the acid environment of the stomach, which may lead to less side-effect and stimulation of aspirin on the gastrointestinal (GI) tract. What's more, the dextran-aspirin conjugate has a sustained release of aspirin.