格列吡嗪pH非依赖型缓释片的处方前研究  

Preformulation study of pH independent sustained release tablet of glipizide

作　　者：谢燕贤 黄劲恒 林华庆[2] 余楚钦[2] 符方方[1] 

机构地区：[1]深圳市宝安区石岩人民医院,广东深圳518108 [2]广东省药物新剂型重点实验室/广东药科大学药物研究所,广东广州510006

出　　处：《广东药科大学学报》2017年第4期433-438,共6页Journal of Guangdong Pharmaceutical University

基　　金：2016年深圳市科技计划项目(JCYJ20160428091243299)

摘　　要：目的开发一种基于微环境pH调控技术的格列吡嗪pH非依赖型缓释片,对格列吡嗪、辅料、pH调节剂进行处方前研究。方法采用差示扫描量热法和傅里叶变换红外光谱法评价格列吡嗪与辅料是否相容;采用高效液相色谱法测定格列吡嗪和有关物质的质量分数。结果差热分析结果表明,乳糖、硬脂酸镁和候选的pH调节剂对格列吡嗪的特征峰位有影响,影响范围在1~13℃之间;傅立叶红外光谱分析结果表明,格列吡嗪在特征区和指纹区内的特征峰没有发生明显的变化;液相分析结果显示,样品中的格列吡嗪质量分数在99.4%以上,有关物质质量分数在0.5%以下。结论所选辅料、pH调节剂全部与格列吡嗪相容,对格列吡嗪的稳定性没有明显的影响,可用于处方研究当中。Objective To develop a kind of pH-independent sustained release tablet of glipizide based on microenvironment modulation, and investigate the preformulation of glipizide, excipients and pH modifiers. Methods The compatibility between glipizide and excipients was evaluated by differential scanning calorimetry and fourier transform infrared spectroscopy. The contents of glipizide and related substances were assayed by high performance liquid chromatography. Results The results of differential thermal analysis showed that the inherent peak of glipizide was affected by lactose, magnesium stearate and pH modifiers, ranging from 1 to 13 ℃. While the results of fourier transform infrared spectroscopy elucidated that the characteristic and finger print region of glipizide had no change. The results of HPLC analysis showed that the contents of glipizide in the samples were over 99. 4%, and that of the related substances were below 0.5%. Conclusions All the candidates were compatible with glipizide, and had little influence on the stability of glipizide, which could be employed in the formulation study.

关 键 词：微环境 处方前研究 相容性 差示扫描量热法 傅立叶变换红外光谱法 

分 类 号：R943[医药卫生—药剂学]