摘要
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 prepare intragastric floating sustained-release tablets with hydroxypropyl methyl cellulose （HPMC） as frame material according to hydrodynamically balanced system（HBS） principle, and study its in vitro release rate and release mechanism. METHODS Stearic acid and polyethylene glycol（PEG 6000） as carrier, m-nisoldipine solid dispersion was prepared by melting method with orthogonal design hydroxypropyl methyl cellulose as releasing skeleton, stearyl aleohol as assist floating agent, sodium bicarbonate （NaHCO3） as blowing agent, lactose as fillers, wet granulation was adopted. RESULTS The release in vitro was in line with Higuchi equation, in vitro release and the release time had a good eorrelation. Sustained-release tablet drug release mechanism was concurrence of the matrix＇ s dissolution and the drug＇s diffusion. CONCLUSION The intragastric floating sustained-release tablets have the advantage of fast floating with good sustained-release property.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2009年第4期287-292,共6页
Chinese Journal of Hospital Pharmacy
关键词
间尼索地平
胃内漂浮型缓释片
累积释放度
m-nisoldipine
intragastric floating tablets
cumulative release rate
