盐酸文拉法辛凝胶骨架片制备及体外释药特性研究

目的 制备盐酸文拉法辛(VH)亲水凝胶骨架片，考察处方、工艺对其体外释药行为的影响，并对其释药机理进行初步分析。方法 以羟丙基甲基纤维素(HPMC)为基本骨架材料，羧甲基纤维素钠(CMC-Na)为阻滞剂，采用湿法制粒制备凝胶骨架片，通过单因素试验筛选辅料种类，利用正交设计试验优化处方，建立释放度测定方法，并通过不同方程拟合释放曲线。结果 盐酸文拉法辛缓释片体外释药符合一级释药特征，药物释放主要是通过Fick扩散完成。HPMC用量和黏度、阻滞剂用量对释放速率有显著影响，填充剂、制粒方法和压片压力对释放速率的影响不显著。结论 以HPMC K100M和CMC-Na为骨架材料，制备的盐酸文拉法辛缓释片具有良好的缓释效果。

Preparation of Venlafaxine Hydrochloride Matrix Tablets and Study of in Vitro Release

Objective: To prepare venlafaxine hydrochloride gel matrix sustained-release tablets, and to evaluate the effect of formula composition, preparation method on the drug release behavior, further to elucidate the mechanism of drug release. Methods: The matrix tablets were prepared by wet granulating, used hydroxypropyl methylcellulose (HPMC) as matrix material and sodium carboxymethyl cellulose (CMC-Na) as retardants. The formulation was chosen by Sigel-factor test, then optimized by the orthogonal design test. A method for determination of in vitro release has been established and fitted by different curve equation. Results: The release behavior of VH matrix tablets is consistent with first kinetic equation. The release mechanism was due to diffusion of the drug from matrix tablets. The release behavior is mainly affected by the amount and viscosity of HPMC and the amount of CMC-Na. The additives, granulation methods and compression pressure show no effect on release. Conclusion: The release of VH could be controlled by using HPMC K100M and CMC-Na.