左金胃漂浮缓释片中小檗碱、巴马汀、吴茱萸碱和吴茱萸次碱的体外释放规律和机制研究

Releasing properties and mechanism in vitro of berberine,palmatine,evodiamine,and rutaecarpine from gastric floating sustained-release tablet containning Zuojin Pellet extraction

目的探讨左金胃漂浮缓释片体外多成分释放的规律和机制。方法采用转篮法以人工胃液为介质,以HPLC法测定左金胃漂浮缓释片中小檗碱、巴马汀、吴茱萸碱和吴茱萸次碱在8 h内的体外累积释放率,通过相似因子比较法、Higuchi方程,零级、一级释放方程等释放模型拟合法以及Peppas方程研究左金胃漂浮缓释片多成分释放的规律。结果左金胃漂浮缓释片中4种生物碱的平均释放曲线相互之间的相似因子均大于80%,均以Higuchi释放模型为最佳拟合模型,释放机制均为扩散协同骨架溶蚀作用。结论左金胃漂浮缓释片中生物碱类成分的释放具有均衡缓释性。

Objective To study the releasing properties and mechanism in vitro of the active ingredients of the gastric floating sustained-release tablet containning Zuojin Pellet extraction（ZJ-GFST）. Methods The release rates of berberine, palmatine, evodiamine, and rutaecarpine from ZJ-GFST in vitro within 8 h were measured by using rotating basket method in Chinese Pharmacopeia. The cumulative curve of drug release data was fitted to zero order, first-order and Higuchi equation to ascertain the kinetic modeling of drug release. Release mechanism was ascertained using Peppas equation. Results The similar factors of the cumulative release curve of all the four ingredients mutually compared were more than 80~, indicating that the release of the four ingredients were similar. The cumulative release rate of all the four ingredients fitted Higuchi equation. The value of slopes of Peppas models of all the four ingredients were more than 0.45, indicating that drug released by concurrent action of diffusion and matrix erode （nonfickian diffusion）. Conclusion The releasing properties in vitro of the active ingredients of ZJ-GFST is consistent.