利用常见的离子添加来加速从Eudragit EPO挤出物中释放的佐洛皮德姆半酸盐
S Henry1, L Descamps2, V Vanhoorne1
1Laboratory of Pharmaceutical Technology, Ghent University, 9000 Ghent, Belgium.
这项研究通过解决缓慢溶解来优化佐洛皮血酸盐配方用于减压. 添加酸改善了药物释放动力学,在15分钟内使溶解率从10%增加到40%.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 配方科学科学 配方科学
背景情况:
- 优化非临床配方对佐尔皮的减记是非常重要的.
- 目前的配方中使用佐洛皮德姆血酸和尤德拉吉特EPO,其溶解性较差.
- 了解药物辅助剂相互作用是改善配方性能的关键.
研究的目的:
- 为了优化佐洛皮血酸和尤德拉吉特EPO配方,以改善溶解.
- 在配方过程中调查佐尔皮血酸盐的降解途径和相互作用.
- 为了增强佐尔皮血酸盐片的溶解动力学.
主要方法:
- 用二极管阵列检测 (HPLC-DAD) 进行热分析和高性能液态染色学,以评估药物的稳定性.
- 里埃变换红外光谱 (FTIR) 探讨药物辅助剂相互作用.
- 平板电脑压缩和溶解测试,以评估配方性能.
主要成果:
- 索尔皮德姆 (Zolpidem) 甲基酸盐容易发生热不成比例,在挤出后增加杂质含量.
- FTIR分析显示,Eudragit EPO的二甲基氨基乙基组由于佐尔皮不成比例而产生质子,解释了缓慢溶解.
- 在15分钟内,添加5%的葡萄酸显著增加了药物释放率,从10%增加到40%.
结论:
- 索尔皮德姆血酸盐不成比例和随后与Eudragit EPO的相互作用阻碍了溶解.
- 酸作为微环境pH调节剂,增强佐尔皮血酸盐溶解动力学.
- 需要进一步优化,以实现索尔皮配方的即时释放特征.
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