复方葡萄籽原花青素亲水凝胶骨架片的制备工艺及其释放度的研究

Preparation and in vitro release mechanism study of hydrophilic matrix sustained release tablets of compound grape seed procyanidines

目的:研究复方葡萄籽花青素骨架片的处方工艺及其体外释药行为。方法:通过单因素试验,确定影响释药效果的主要因素,进行正交设计,以原花青素中单体成分儿茶素体外累积释放度为依据,优选出最佳工艺。结果:所制缓释片无突释现象,缓释周期12 h。采用零级、一级、Higuchi及Peppas方程判断儿茶素的释药机制,表明儿茶素释放行为符合Higuchi模型,释放机制为骨架溶蚀机制。结论:该法制备的复方葡萄籽花青素骨架片制备工艺简单易行,具有良好的释放机制。

Objective： In this study, hydrophilic matrix sustained release tablets of compound grape seed procyanidines and the in vitro release behavior were evaluated. Method： The main factors influencing drug release were investigated by single factor test. Then technology was optimized using in vitro cumulative dissolution degree of catechu （one monomer of procyanidines） through orthogonal design. Result： No burst drug release from the obtained matrix tablets was observed. Drug release sustained for 12 h. The release mechanism of grape seed procyanidines was accessed by zero-order, first-order, Higuchi and Peppas equation. The release behavior of grape seed procyanidines was better accorded with Hignchi model and the drug release from the tablets was controlled by degradation of the matrix. Conclusion： The preparation of hydrophilic matrix sustained release tablets of compound grape seed procyanidines is simple with good performance of drug release.