AbbVie, 2525 Dupont Drive, Irvine, CA 92612, USA.
AbbVie, 2525 Dupont Drive, Irvine, CA 92612, USA.
J Pharm Sci. 2024 Oct;113(10):2997-3011. doi: 10.1016/j.xphs.2024.07.023. Epub 2024 Aug 6.
Topical ophthalmic drug product development is a niche research domain as the drug formulations need to be designed to perform in the unique ocular physiological conditions. The most common array of small molecule drug formulations intended for topical ophthalmic administration include solutions, suspensions, emulsions, gels, and ointments. The formulation components such as excipients and container closure are unique to serve the needs of topical ophthalmic delivery compared to other parenteral products. The selection of appropriate formulation platform, excipients, and container closure for delivery of drugs by topical ophthalmic route is influenced by a combination of factors like physicochemical properties of the drug molecule, intended dose, pharmacological indication as well as the market trends influenced by the patient population. In this review, data from literature and packaging inserts of 118 reference listed topical ophthalmic medications marketed in the US are collected and analyzed to identify trends that would serve as a guidance for topical ophthalmic formulation development for small molecule drugs. Specifically, the topics reviewed include current landscape of the available small molecule topical ophthalmic drug products in the US, physicochemical properties of the active pharmaceutical ingredients (APIs), formulation platforms, excipients, and container closure systems.
局部眼科药物产品的开发是一个利基研究领域，因为药物制剂的设计需要在独特的眼部生理条件下发挥作用。最常用于局部眼科给药的小分子药物制剂包括溶液、混悬剂、乳剂、凝胶和软膏。与其他注射产品相比，制剂成分（如赋形剂和容器密封件）是独特的，以满足局部眼科递送的需求。通过局部眼科途径递送药物的合适制剂平台、赋形剂和容器密封件的选择受到多种因素的影响，如药物分子的理化性质、预期剂量、药理学适应症以及受患者群体影响的市场趋势。在这篇综述中，收集和分析了美国市场上销售的 118 种参考列出的局部眼科药物的文献和包装插页中的数据，以确定可作为小分子药物局部眼科制剂开发指南的趋势。具体而言，审查的主题包括美国现有小分子局部眼科药物产品的现状、活性药物成分（API）的理化性质、制剂平台、赋形剂和容器密封系统。
