Brandstetter Dominik, Arsiccio Andrea, Hawe Andrea, Svilenov Hristo L, Menzen Tim
Coriolis Pharma Research GmbH, Fraunhoferstr. 18 b, 82152 Martinsried, Germany; Technische Universität München, TUM School of Life Sciences, Biopharmaceutical Technology, Emil-Erlenmeyer-Forum 5, 85354 Freising, Germany.
Coriolis Pharma Research GmbH, Fraunhoferstr. 18 b, 82152 Martinsried, Germany.
J Pharm Sci. 2025 Jul;114(7):103805. doi: 10.1016/j.xphs.2025.103805. Epub 2025 Apr 24.
Lyophilization is frequently employed to stabilize sensitive biopharmaceuticals. The potential importance of the edge vial effect, defined as the discrepancy in temperature and drying behavior between vials located in different positions of the batch, attracts considerable attention from the lyophilization community. Here, we lyophilized two model fusion-protein formulations by applying a design space representation to select conservative as well as aggressive lyophilization protocols on the verge of structural collapse of the cake. The effect of vial position and number of neighbor vials on cake appearance, cake volume, and residual moisture content was quantified. Moreover, the stability of the fusion-protein was assayed in relation to monomer content, size distribution of submicron and subvisible particles, as well as the presence of visible particles. Additionally, the images of micron-sized particles were analyzed by using a machine-learning based "fingerprinting" method to identify potential morphological differences induced by the edge vial effect. We concluded that the investigated quality attributes, including cake appearance, residual moisture, particle burden, and particle morphology, were not significantly affected by the edge vial effect. In contrast, the aggressive lyophilization cycle on the verge of collapse showed a minor, formulation-dependent impact on cake volume and particle count.
冻干法经常用于稳定敏感的生物制药。边缘瓶效应的潜在重要性,即批次中不同位置的瓶子在温度和干燥行为上的差异,引起了冻干领域的广泛关注。在此,我们通过应用设计空间表示法对两种模型融合蛋白制剂进行冻干,以选择在冻干饼结构即将崩溃时保守以及激进的冻干方案。量化了瓶位和相邻瓶数量对冻干饼外观、冻干饼体积和残余水分含量的影响。此外,还针对单体含量、亚微米和亚可见颗粒的尺寸分布以及可见颗粒的存在情况测定了融合蛋白的稳定性。另外,通过使用基于机器学习的“指纹识别”方法分析微米级颗粒的图像,以识别由边缘瓶效应引起的潜在形态差异。我们得出结论,所研究的质量属性,包括冻干饼外观、残余水分、颗粒负荷和颗粒形态,均未受到边缘瓶效应的显著影响。相比之下,在即将崩溃时采用的激进冻干循环对冻干饼体积和颗粒计数有轻微的、依赖于制剂的影响。