Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD, 21201, USA.
Center for Drug Evaluation and Research, Food and Drug Administration, Silver Spring, MD, 20993, USA.
J Pharm Sci. 2024 Aug;113(8):2215-2222. doi: 10.1016/j.xphs.2024.03.005. Epub 2024 Mar 12.
The addition of antioxidants to pharmaceutical products is a potential approach to inhibit nitrosamine formation, particularly in solid oral dosage forms like tablets and capsules. The objective was to assess the effect of ten antioxidants on the permeability of four Biopharmaceutics Classification System (BCS) Class III drugs. Bi-directional drug permeability studies in the absence and presence of antioxidants were performed in vitro across MDCK-II monolayers. No antioxidant increased drug permeability, while the positive control sodium lauryl sulfate always increased drug permeability. Results support that any of the ten antioxidants, up to at least 10 mg, can be added to a solid oral dosage form without modulating passive drug intestinal permeability. Additional considerations are also discussed.
在药物产品中添加抗氧化剂是抑制亚硝胺形成的一种潜在方法，特别是在片剂和胶囊等固体制剂中。目的是评估十种抗氧化剂对四种生物药剂学分类系统（BCS）III 类药物渗透性的影响。在不存在和存在抗氧化剂的情况下，在 MDCK-II 单层中进行了双向药物渗透性研究。没有抗氧化剂增加药物渗透性，而阳性对照十二烷基硫酸钠总是增加药物渗透性。结果表明，十种抗氧化剂中的任何一种，至少添加 10mg，都可以添加到固体制剂中，而不会调节药物的肠道被动渗透性。还讨论了其他注意事项。
