Abdel-Tawab Mona, Waßmuth Markus, Gegenfurtner Florian, Hawe Andrea, Schefe Jan H, Strunz Anke M, Wübert Joachim
Central Laboratory of German Pharmacists, Eschborn, Germany
Central Laboratory of German Pharmacists, Eschborn, Germany.
Eur J Hosp Pharm. 2022 Jul 19;31(2):135-42. doi: 10.1136/ejhpharm-2021-003198.
Aggregation is one of the key critical points limiting the stability of monoclonal antibodies in solution. The present study aimed to investigate the in-use stability of a residual monoclonal antibody solution after withdrawal of most of the filling volume of PF-06439535 (bevacizumab biosimilar), addressing the physical and chemical stability with respect to aggregation and fragmentation.
The stability of residual PF-06439535 solution (25 mg/mL) after withdrawal of 80% (12.8 mL) filling volume with a 20G needle was monitored over a light-protected storage period of 8 days at 2-8°C and 25°C with measurement time points at D0 (start of storage), D2, D4, and D8 (2, 4, and 8 days of storage after start, respectively). Unopened vials stored under the same conditions served as control. For this purpose, the analytical results from size exclusion chromatography, dynamic light scattering, and micro-flow imaging obtained after the individual measurement time points up to 8 days were compared with those obtained at D0 and with those obtained for unopened vials stored under the same conditions.
No aggregation or ongoing fragmentation due to partial withdrawal of filling volume could be observed in the residual PF-06439535 solution. Moreover, no changes in the particle size distribution at D8 compared with the D0 values were identified upon storage at either 2-8°C or 25°C (both opened and unopened vials). The total concentration of particles ≥10 µm of all samples was <100 particles/mL. In addition, no variations in the pH values or in the visual appearance were detected over the whole study period in all samples at all storage conditions.
Consequently, residual PF-06439535 solution (25 mg/mL) in opened vials may be regarded as stable when stored light-protected over a period of 8 days in the refrigerator (2-8°C) or at 25°C.
聚集是限制单克隆抗体溶液稳定性的关键临界点之一。本研究旨在探讨在抽出大部分填充体积的PF-06439535(贝伐单抗生物类似药)后残留单克隆抗体溶液的使用稳定性,研究其在聚集和碎片化方面的物理和化学稳定性。
用20G针头抽出80%(12.8 mL)填充体积后,残留的PF-06439535溶液(25 mg/mL)在2 - 8°C和25°C的避光储存期8天内进行监测,测量时间点为D0(储存开始)、D2、D4和D8(分别为储存开始后的2、4和8天)。在相同条件下储存的未开封小瓶用作对照。为此,将直至8天的各个测量时间点后通过尺寸排阻色谱法、动态光散射法和微流成像法获得的分析结果与在D0获得的结果以及在相同条件下储存的未开封小瓶获得的结果进行比较。
在残留的PF-06439535溶液中未观察到因部分抽出填充体积而导致的聚集或持续碎片化。此外,在2 - 8°C或25°C储存时(包括开封和未开封小瓶),与D0值相比,D8时的粒径分布没有变化。所有样品中≥10 µm颗粒的总浓度<100颗粒/mL。此外,在所有储存条件下的所有样品在整个研究期间均未检测到pH值或外观的变化。
因此,开封小瓶中的残留PF-06439535溶液(25 mg/mL)在冰箱(2 - 8°C)或25°C避光储存8天期间可视为稳定。