Abstract：
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.
摘要：
在药品中添加抗氧化剂是抑制亚硝胺形成的潜在方法，特别是固体口服剂型如片剂和胶囊。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类药物的渗透性的影响。在不存在和存在抗氧化剂的情况下,跨MDCK-II单层在体外进行双向药物渗透性研究。无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。结果支持十种抗氧化剂中的任何一种，至少10毫克，可添加至固体口服剂型而不调节被动药物肠通透性。还讨论了其他考虑因素。
