4种不同的包衣材料对非洛地平释药性能的影响

Effect of four different coating material on drug release property of the Felodipine

关键词:  非洛地平缓释片  薄膜包衣  释放度  相似因子

Key words:  felodipine sustaind-release tablets  film coating  drug release  similarity factor

摘要:

[目的] 考察4种不同的包衣材料对非洛地平释药性能的影响。[方法] 对不同包衣材料缓释片的硬度、脆碎度、吸湿性进行测定,结合电镜扫描图谱,采用非洛地平缓释片质量标准的释放度测定法,以相似因子f₂值为指标,筛选包衣材料的种类和增重量。[结果] f₂值为56.01,确定欧巴代Ⅱ型为非洛地平缓释片的包衣材料,包衣增重量为2%,硬度为109.11 N,脆碎度为0.46%和吸湿增重百分率为0.16%,均符合要求。并且结果可以满足中国药典对缓控释制剂的体外溶出要求,释放动力学特征以Ritger-Peppas模型拟合较好,根据Peppas方程,其释放机制是药物扩散和骨架溶蚀的共同作用。[结论] 欧巴代Ⅱ型包衣片与原研药的释药特性最为相似,可用于非洛地平的包衣材料。

Abstract:

[Objective] To study the effect of four different coating materials on the drug-release properties of the felodipine. [Methods] The hardness, friability and hygroscopicity of the different sustained-release tablets of coating materials were determined. The type and weight gain of the coating materials, the pattern combined with scanning electron microscope were screened through quality standards of felodipine sustained-release tablets release method according to the indicator of the similarity factor f₂ value. [Results] The f₂ value was 56.01. It was determined that the Opadry Ⅱtype was the coating material of the felodipine sustained-release tablet. All of the following results met the requirements: the weight gain of coating is 2%, hardness is 109.11 N, friability is 0.46% and hygroscopic percent weight gain is 0.16%. The result could satisfied the requirement of the Chinese Pharmacopoeia on the in vitro dissolution of the sustained-released preparations Ritger-Peppas model was a better fitting for release kinetics characteristics, the release mechanism of which was the combined action of the drug diffusion and skeleton dissolution according to Peppas equation. [Conclusion] The coating tablet of Opadry Ⅱ has the most similarities with the drug-release properties of the original research drug and it can be applied to the coating materials of the felodipine.