Cheng Yuan, Duong Huu Thuy Trang, Hu Qingyan, Shameem Mohammed, Tang Xiaolin Charlie
Formulation Development Group, Regeneron Pharmaceuticals Inc, 777 Old Saw Mill River Rd, Tarrytown, NY 10591, USA.
Antib Ther. 2024 Nov 21;8(1):13-25. doi: 10.1093/abt/tbae030. eCollection 2025 Jan.
The development of lyophilized protein drug products is a critical and complex task in the pharmaceutical industry, requiring a comprehensive understanding of the myriad of factors affecting product quality, stability, and the efficiency and robustness of the lyophilization process. This review offers practical advice on the critical aspects of lyophilized protein drug product development. Practical considerations across both the early and late stages of development are discussed, underscoring the necessity of a strategic approach from initial development through to commercialization. The review then delves into formulation optimization strategies that are essential for enhancing protein stability and the efficiency of the lyophilization process. This section outlines stable formulation design and highlights the unique considerations required for high protein concentration lyophilized drug products. It further explores the formulation strategies to enhance the lyophilization process' efficiency. Moreover, the paper examines the critical elements in selecting primary containers and closures for lyophilized drug products, focusing on vials and dual chamber systems. The analysis encompasses the effects of the container/closure's material, size, geometry, and fill volume on product quality and process efficiency. Lastly, the review provides practical considerations in lyophilization cycle development, including the design and optimization of the freezing, primary drying, and secondary drying stages to achieve a robust, scalable, and efficient lyophilization process. By offering comprehensive insights into these key areas to enhance their understanding and implementation of best practices in the field, this paper serves as a useful resource for researchers, formulators, and process engineers involved in the development of lyophilized protein drug products.
冻干蛋白药物产品的开发是制药行业一项关键且复杂的任务,需要全面了解影响产品质量、稳定性以及冻干过程效率和稳健性的众多因素。本综述就冻干蛋白药物产品开发的关键方面提供了实用建议。讨论了开发早期和后期的实际考虑因素,强调了从初始开发到商业化采取战略方法的必要性。该综述接着深入探讨了对于提高蛋白质稳定性和冻干过程效率至关重要的配方优化策略。本节概述了稳定配方设计,并突出了高蛋白浓度冻干药物产品所需的独特考虑因素。它进一步探讨了提高冻干过程效率的配方策略。此外,本文研究了为冻干药物产品选择主要容器和密封件的关键要素,重点是小瓶和双腔系统。分析涵盖了容器/密封件的材料、尺寸、几何形状和填充体积对产品质量和过程效率的影响。最后,该综述提供了冻干周期开发中的实际考虑因素,包括冷冻、一次干燥和二次干燥阶段的设计和优化,以实现稳健、可扩展且高效的冻干过程。通过对这些关键领域提供全面见解,以增进对该领域最佳实践的理解和实施,本文为参与冻干蛋白药物产品开发的研究人员、配方师和工艺工程师提供了有用的资源。