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含有肠道聚合物和弱基药物的无形固体分散的片剂的肠道涂层:增强体外释放的策略
Hanh Thuy Nguyen1, Tu Van Duong1, Lynne S Taylor1
1Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, IN 47907, United States.
含有德拉曼胺 (DLM) 的无形固体分散物 (ASD) 可以在胃酸中结晶. 药片上的肠道涂层防止了这种结晶,并减少了药物释放的可变性,提供了一个有前途的解决方案.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 含有德拉曼胺 (DLM) 和高素甲酸盐 (HPMCP) 的无形固体分散 (ASD) 容易在模拟的胃液中结晶.
- 这种结晶可能会对药物释放和生物可用性产生负面影响.
研究的目的:
- 开发一种策略,以防止胃环境中的自闭症引起的德拉曼结晶.
- 提高药物释放性能并通过对含有DLMASD的片剂涂上肠道涂层来降低变异性.
主要方法:
- 含有DLM ASDs与HPMCP的药片是用甲基酸共聚合物配制和涂层的.
- 实验室药物释放被评估使用一个两阶段溶解试验与可变的胃pH (1.6-5.0),其次是模拟的肠液.
- 肠膜的胃阻力时间在pH范围内进行了评估.
主要成果:
- 肠道涂层有效地保护了德拉曼胺ASDs在酸性条件下结晶,其中HPMCP是不溶性的.
- 与参考产品相比,药物释放的可变性在经历不同胃pH条件时显著降低.
- 该涂层在防止结晶和确保药物持续释放方面表现出有效性.
结论:
- 肠道涂层是一种可行的策略,可以防止胃环境中的ASDs的德拉曼胺结晶.
- 这种方法减轻了与不同prandial状态期间生理pH值变化相关的药物释放变化.
- 对ASD结晶抑制剂和保护性涂层策略的进一步研究是有必要的.
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