左金丸总生物碱缓释片的制备及体外释放度研究

Preparation of Sustained-release Tablets for Total Alkaloid from Zuojin Pills and Study on Their Release in Vitro

目的:制备左金丸总生物碱缓释片并考察其体外释放行为。方法:以左金丸总生物碱为主药,以羟丙基甲基纤维素为凝胶骨架材料制备缓释片,并对处方中辅料用量进行正交优化。通过药物释放动力学模型拟合左金丸总生物碱缓释片中盐酸小檗碱和吴茱萸碱的释放过程,并推测其释药机制。结果:每片缓释片中羟丙基甲基纤维素、微晶纤维素和乳糖的最佳用量分别为100、50和15 mg。盐酸小檗碱的释放接近Higuchi方程,吴茱萸碱的释放接近Peppas方程,2种成分的释放机制均为药物扩散和骨架溶蚀共同作用。结论:左金丸总生物碱缓释片缓释效果明显,符合设计要求,制备工艺简单可行。

Objective：To prepare sustained-release tablets for total alkaloid from Zuojin pills and to study their in vitro release behavior.Methods：The sustained-release tablets were prepared,with the total alkaloid from Zuojin pills as the principal component and hydroxypropyl methylcellulose（HPMC） as the gel-matrix.The optimal amount of exci-pients in the formulation was confirmed by orthogonal test.The release kinetics models were used to fit the release process of berberine and evodiamine from sustained-release tablets,and the mechanisms of drug release were deduced.Results：The optimal amount of exci-pients in the formulation was as follows：HPMC of 100 mg,microcrystal cellulose of 50 mg,and lactose of 15 mg.The release kinetic of berberine and evodiamine are basically in conformity with the Higuchi equation and Peppas equation,respectively.According to the Peppas equation,the release mechanisms of both berberine and evodiamine are affected by drug diffusion and matrix erosion.Conclusion：The sustained-release tablets for total alkaloid from Zuojin pills have the slow release characteristics and comply with the requirements of formulation design.Their preparation technique is simple and feasible.