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自旋冷冻参数和辅料组成对聚乙二醇化肽制剂产品稳定性的影响。

Impact of spin-freezing parameters and excipient composition on product stability of a PEGylated peptide formulation.

作者信息

Schaal Zarah, Bockstal Pieter-Jan Van, Lammens Joris, Lenger Julian H, Funke Adrian P, Schneid Stefan C, Beer Thomas De

机构信息

RheaVita, Poortakkerstraat 9C, 9051 Ghent, Belgium; Laboratory of Pharmaceutical Process Analytical Technology, Department of Pharmaceutical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, 9000 Ghent, Belgium.

RheaVita, Poortakkerstraat 9C, 9051 Ghent, Belgium.

出版信息

Int J Pharm. 2025 Oct 15;683:126007. doi: 10.1016/j.ijpharm.2025.126007. Epub 2025 Aug 6.

Abstract

This study examines the impact of spin‑freezing parameters, as applied in continuous spin-freeze-drying processes, and formulation composition on the stability of a PEGylated peptide following freeze‑drying and storage. A trehalose‑based reference formulation was compared with two reformulated systems in which trehalose was replaced by either mannitol or a 75:25 sucrose-mannitol blend. Samples were processed under four distinct spin‑freezing conditions, varying in cooling and crystallization rates, followed by batch‑drying and storage at either 2-8 °C or 50 °C for up to 13 weeks. Product quality was evaluated by assessing peptide concentration, monomer content, and cake morphology. Across all formulations and storage conditions, variations in spin‑freezing parameters exhibited no consistent or statistically significant effect on peptide or monomer levels. In contrast, formulation composition emerged as the dominant stability determinant. Trehalose‑based samples maintained robust stability under both refrigerated storage and stress conditions, whereas mannitol‑based samples exhibited moderate degradation at elevated temperatures. The sucrose-mannitol formulation demonstrated pronounced instability at 50 °C, characterized by cake collapse, browning, and interference in peptide quantification, likely as a result of sucrose hydrolysis and the formation of aromatic degradation products. These findings highlight that, for the formulations investigated, the choice of excipient is critical for product stability and that systems susceptible to sugar degradation may require adapted analytical approaches, as well as optimized drying protocols and storage conditions.

摘要

本研究考察了连续旋转冷冻干燥过程中应用的旋转冷冻参数以及配方组成对聚乙二醇化肽冻干和储存后稳定性的影响。将基于海藻糖的参比制剂与两种重新配制的体系进行比较,在这两种体系中,海藻糖分别被甘露醇或75:25的蔗糖-甘露醇混合物替代。样品在四种不同的旋转冷冻条件下进行处理,冷却和结晶速率各不相同,随后进行分批干燥,并在2-8℃或50℃下储存长达13周。通过评估肽浓度、单体含量和饼状形态来评价产品质量。在所有配方和储存条件下,旋转冷冻参数的变化对肽或单体水平均未表现出一致的或统计学上显著的影响。相比之下,配方组成成为主要的稳定性决定因素。基于海藻糖的样品在冷藏储存和应激条件下均保持较强的稳定性,而基于甘露醇的样品在高温下表现出中度降解。蔗糖-甘露醇配方在50℃下表现出明显的不稳定性,其特征为饼状塌陷、褐变以及对肽定量的干扰,这可能是由于蔗糖水解和芳香族降解产物的形成所致。这些发现突出表明,对于所研究的配方,辅料的选择对产品稳定性至关重要,并且易发生糖降解的体系可能需要采用适应性的分析方法以及优化的干燥方案和储存条件。

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