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目的:根据流体动力学平衡体系(HBS)原理研制以羟丙甲基纤维素(HPMC)为骨架材料的胃内漂浮型缓释片,并对其体外释放度和释放机制进行探讨。方法:以硬脂酸和聚乙二醇6000(PEG6000)为载体,采用熔融法制备间尼索地平固体分散体;采用正交设计优化处方,以HPMC为缓释骨架,十八醇为助漂剂,碳酸氢钠为发泡剂,乳糖为填充剂,湿法制粒压片法压片。结果:体外释药符合Higuchi方程,体外释药量与释药时间有良好的相关性。缓释片的药物释放机制是通过药物的扩散和骨架溶蚀协同作用。结论:该法制备的胃内漂浮型缓释片具有起漂快,漂浮时间长,缓释效果好,制备工艺简单等优点。
OBJECTIVE: To develop sustained release tablets in the stomach with hydroxypropyl methylcellulose (HPMC) as the framework material according to the principle of hydrodynamic equilibrium system (HBS), and to investigate its in vitro release and release mechanism. Methods: The solid dispersion of m-nisoldipine was prepared by melt method with stearic acid and polyethylene glycol 6000 (PEG6000) as carrier. The orthogonal design was used to optimize the formulation. HPMC was used as sustained-release matrix and stearyl alcohol Agent, sodium bicarbonate as a foaming agent, lactose as a filler, wet granulation tabletting method. RESULTS: In vitro drug release was in accordance with Higuchi’s equation. The in vitro drug release was in good correlation with drug release time. The drug release mechanism of sustained-release tablets is synergistic through drug diffusion and skeleton erosion. Conclusion: The intragastric floating sustained-release tablets prepared by this method have many advantages such as fast floating, long floating time, good sustained-release effect and simple preparation process.