Formulations Development, Regeneron Pharmaceuticals, Inc., 777 Old Saw Mill River Road Tarrytown, New York, 10591, USA.
AAPS PharmSciTech. 2021 Mar 11;22(3):100. doi: 10.1208/s12249-021-01949-4.
Intravitreal (IVT) administration of therapeutics is the standard of care for treatment of back-of-eye disorders. Although a common procedure performed by retinal specialists, IVT administration is associated with unique challenges related to drug product, device and the procedure, which may result in adverse events. Container closure configuration plays a crucial role in maintaining product stability, safety, and efficacy for the intended shelf-life. Careful design of primary container configuration is also important to accurately deliver small volumes (10-100 μL). Over- or under-dosing may lead to undesired adverse events or lack of efficacy resulting in unpredictable and variable clinical responses. IVT drug products have been traditionally presented in glass vials. However, pre-filled syringes offer a more convenient administration option by reducing the number of steps required for dose preparation there by potentially reducing the time demand on the healthcare providers. In addition to primary container selection, product development studies should focus on, among other things, primary container component characterization, material compatibility with the formulation, formulation stability, fill volume determination, extractables/leachables, and terminal sterilization. Ancillary components such as disposable syringes and needles must be carefully selected, and a detailed administration procedure that includes dosing instructions is required to ensure successful administration of the product. Despite significant efforts in improving the drug product and administration procedures, ocular safety concerns such as endophthalmitis, increased intraocular pressure, and presence of silicone floaters have been reported. A systematic review of available literature on container closure and devices for IVT administration can help guide successful product development.
玻璃体内(IVT)治疗药物的给药是治疗眼后疾病的标准护理。虽然这是视网膜专家经常进行的常见程序,但 IVT 给药与药物产品、设备和程序相关的独特挑战有关,这些挑战可能导致不良事件。容器封闭结构在维持产品稳定性、安全性和预期货架寿命内的功效方面起着至关重要的作用。对初级容器结构进行仔细设计对于准确输送小体积(10-100μL)也很重要。剂量过大或过小可能导致不良事件或缺乏疗效,从而导致不可预测和可变的临床反应。IVT 药物产品传统上以玻璃小瓶形式呈现。然而,预充注射器通过减少剂量准备所需的步骤提供了更方便的给药选择,从而可能减少医疗保健提供者的时间需求。除了初级容器选择外,产品开发研究还应侧重于初级容器组件特性、材料与制剂的相容性、制剂稳定性、填充体积确定、浸出物/可提取物以及终端灭菌等方面。一次性注射器和针头等辅助组件必须仔细选择,并且需要详细的给药程序,包括剂量说明,以确保产品的成功给药。尽管在改进药物产品和给药程序方面做出了重大努力,但仍有眼部安全问题,如眼内炎、眼内压升高和硅浮子的存在。对 IVT 给药的容器封闭和设备的现有文献进行系统审查可以帮助指导成功的产品开发。