Excipients represent diverse classes of molecules, small molecules or macromolecules, with versatile structures within a given class and are from natural, semi-synthetic and synthetic sources. They are essential ingredients in drug products independently of the route of administration where both traditional and non-traditional uses are present. Beyond their traditional use as formulation and manufacturing aids, certain excipients exhibit biological effects and thus can be used either as atypical active pharmaceutical ingredients alone or synergistically with conventional active pharmaceutical ingredients to affect the overall pharmacokinetics/ pharmacodynamics and therapeutic effect(s) of the co-administered drug(s). In reference to oral drugs, biological effects of the excipients that contribute to improved drug absorption and pharmacokinetics include their ability to modulate drug dissolution, intestinal membrane permeability, gut wall metabolism and efflux pumps. These non-traditional uses of excipients are illustrated in representative case studies from published literature. From a drug development and regulatory perspective, it is apparent that an appropriate excipient classification system is considered which is applied to new uses of existing excipients as well as to the development of novel excipients and segregates biologically active excipients from the larger pool of excipients. This classification system should be a useful tool to pharmaceutical scientists and its successful implementation and broader acceptance requires input and ownership from all major stakeholders, that is, the excipient manufacturers, the end users, excipient forums and discussion groups such as the International Pharmaceutical Excipients Council (IPEC) and regulatory agencies.

中文翻译：

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关于口服药物产品中赋形剂的传统和非传统使用的考虑和建议

赋形剂代表分子，小分子或大分子的不同类别，具有给定类别内的通用结构，并且来自天然，半合成和合成来源。它们是药物产品中的必需成分，与存在传统和非传统用途的给药途径无关。除了传统上用作制剂和制造助剂的用途以外，某些赋形剂还具有生物学作用，因此可以单独用作非典型活性药物成分，也可以与常规活性药物成分协同使用，以影响药物的总体药代动力学/药效学和治疗效果-给药的药物。关于口服药物，赋形剂对改善药物吸收和药代动力学的生物学作用包括调节药物溶解，肠膜通透性，肠壁代谢和外排泵的能力。赋形剂的这些非传统用途在公开文献的代表性案例研究中得到了说明。从药物开发和监管的角度来看，很明显，已经考虑了适当的赋形剂分类系统，该系统适用于现有赋形剂的新用途以及新型赋形剂的开发，并从较大的赋形剂库中分离出生物活性赋形剂。此分类系统应是制药科学家的有用工具，其成功实施和广泛接受需要所有主要利益相关者的投入和所有权，