盐酸罗沙替丁醋酸酯胃内滞留片的制备及体外释药特性

Preparation and in vitro release of intragastric retention tablets of roxatidine acetate hydrochloride

以盐酸罗沙替丁醋酸酯为模型药物制备胃内滞留片,并评价其体外释放特性。在单因素考察基础上,以漂浮性能和体外累积释放度作为主要考察因素,采用3因素3水平的正交设计进行处方优化,确定最佳处方。最佳处方为每片含盐酸罗沙替丁醋酸酯75 mg,HPMC K100M和壳聚糖(0.15 Pa.s)140 mg(2∶1),碳酸氢钠50 mg,乳糖35 mg,硬脂酸镁3mg。该处方片剂起漂快(<3 min),持续漂浮时间长(>8 h),体外释药时间长,其释药行为符合零级动力学和Higuchi方程。所得片剂漂浮性能良好,缓释作用明显,且制备工艺简单可行。

The aim of this study was to prepare raxatidine acetate hydrochloride （ROX） intragastric retention tablets and to study their in vitro releasing features. According to the cumulative release and floating capacity, formulations were optimized by single factor screening and orthogonal design with 3 factors and 3 levels. The optimal formula were ROX 75 rag, HPMC K100M-chitosan （0. 15 Pa. s） （2 ： 1） 140 mg, sodium bicarbonate 50 rag, lactose 35 rag, magnesium stearate 3 mg. The optimized tablets could float within 3 min and maintain for over 8 h, ideal sustained release characteristics in vitro coincided with zero-order kinetic and Higuchi equation. Prepared tablets showed good floating during the whole release process, and sustained release properties. The formulation and preparation technique were simple and feasible.