PDF(Pubmed)
Abstract：
Aim: Amide-linked amylose-based prodrugs were developed for colon-targeted release of mefenamic acid. Materials & methods: Activation of prodrug was studied spectrophotometrically, enzyme-linked immunosorbent assay appraised cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibition at different concentrations of the prodrug, the behavior of prodrug under physiological conditions was monitored by scanning electron microscopy. Results: Prodrug was poorly activated in the enzyme-free simulated gastric media and simulated intestinal media (SIM) but preincubation in pancreatin followed by treatment in aminopeptidase containing SIM led to a significant activation of prodrug. Conclusion: Amide-linked amylose-mefenamic acid conjugates showed a slow release in simulated gastric media and a controlled release in SIM with pancreatin playing an important role in drug release.
摘要：
目的：开发了基于酰胺连接的直链淀粉的前药，用于甲芬那酸的结肠靶向释放。材料与方法：用分光光度法研究了前药的活化，酶联免疫吸附试验评价了不同浓度的前药对环氧合酶-1（COX-1）和环氧合酶-2（COX-2）的抑制作用，通过扫描电子显微镜监测前药在生理条件下的行为。结果：前药在无酶的模拟胃介质和模拟肠介质（SIM）中的活化能力较差，但在胰酶中预孵育，然后在含氨肽酶的SIM中处理导致前药的显着活化。结论：酰胺连接的直链淀粉-甲芬那酸缀合物在模拟胃介质中显示出缓慢释放，在SIM中显示出受控释放，而胰酶在药物释放中起重要作用。
