抗氧化剂添加对药物溶解的影响:对NDSRI缓解生物豁免的影响
Rutu R Valapil1, James E Polli1
1Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, United States of America.
International journal of pharmaceutics
|June 3, 2025
概括
将抗氧化剂添加到迪克洛菲纳克片中通常不会影响药物溶解. 这项研究评估了六种抗氧化剂,发现它们与平板电脑配方最兼容,支持它们用于控制尼托胺杂质的使用.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 不洁净性分析 (Impurity Profiling) 是一种分析方法.
背景情况:
- 药品中的尼托胺杂质存在突变致病风险.
- 建议使用抗氧化剂,以减轻在药片和囊中酸胺的形成.
- 根据FDA的新指导,对抗氧化剂对药物溶解的影响的实践数据有限.
研究的目的:
- 为了研究添加抗氧化剂对迪克洛菲纳克片体外溶解的作用.
- 为了评估各种抗氧化剂与二甲配方的兼容性.
- 评估抗氧化剂添加在制药制造中的实际影响.
主要方法:
- 制造两种含有抗氧化剂和不含抗氧化剂的迪克洛芬雅克片 (50毫克) 制剂家族.
- 在美国药典模拟肠液 (USP SIF) 和二碳酸缓冲器中的体外溶解测试.
- 使用相似度因子f2比较溶解资料.
主要成果:
- 亚酸,氨酸和二碳酸没有显著影响USP SIF和缓冲器中的溶解,除了一个例外.
- 咖啡酸,酸和甲一般会减缓溶解,只有一个例外.
- 大多数经过测试的抗氧化剂在没有对药物溶解产生负面影响的情况下显示出可行性.
结论:
- 将某些抗氧化剂添加到二甲片中是可行的,而不会影响药物的溶解.
- 需要仔细选择抗氧化剂,以避免对药物释放谱的潜在影响.
- 研究结果支持在固体剂型中使用抗氧化剂来控制尼托胺.
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