Novel application method of talcum powder to prevent sticking tendency and modify release of esomeprazole magnesium enteric-coated pellets

作者：Liu, Zan; Wang, Weiwei; Chen, Hao; Liu, Jianping^*; Zhang, Wenli

来源：Pharmaceutical Development and Technology, 2016, 21(4): 405-414.

DOI：10.3109/10837450.2015.1016616

• Barrier
• esomeprazole magnesium pellets
• Eudragit (R) L30D-55
• release behavior
• talcum powder

Actually, reflecting drug release from polymer-coated pellets remains a challenge. In this study, sticking of pellets caused by Eudragit (R) L30D-55 was observed during the release process, leading to change in drug release. Talcum powder (talc) was used in esomeprazole magnesium pellets to prevent sticking and modify release of pellets. Three methods including talc incorporated in enteric layer, physically mixed and coating resulted pellets were employed to prevent the sticking. The release of pellets was modified by addition talc into subcoat. The dispersion coefficient (F-d) and release profiles were determined in phosphate buffer solution (pH 6.8 and 6.0) and distilled water. It was found that the first manner made F-d increase to about 0.75, but the latter two methods could completely prevent sticking. Also, the second manner was more simple and readily scaled up. In addition, talc in subcoat significantly slowed the drug release in water, but the slowing release effect is less pronounced at pH 6.0 and 6.8. These different effects of talc were attributed to a different release mechanism in three media. The release profiles in water were fitted to Nuttanan model, and the K designated as diffusive resistance constant was linearly increased with talc levels in subcoat (R-2=0.9874).

• 出版日期2016-5-18
• 单位中国药科大学