Ressing M E, Jiskoot W, Talsma H, van Ingen C W, Beuvery E C, Crommelin D J
Laboratory for Inactivated Viral Vaccines, National Institute of Public Health and Environmental Protection, Bilthoven, The Netherlands.
Pharm Res. 1992 Feb;9(2):266-70. doi: 10.1023/a:1018905927544.
The influence of lyophilization on the stability of a monoclonal antibody (MN12) was investigated. MN12 was freeze-dried in different formulations [without lyoprotectant or in the presence of sucrose, dextran, or hydroxypropyl-beta-cyclodextrin (HP beta CD)] and under varying conditions (with or without secondary drying). Subsequently, the monoclonal antibody was stored for 18 or 32 days at various temperatures (4, 37, or 56 degrees C). For comparison, solutions of MN12 were stored under the same conditions. Regardless of the lyoprotectant used, precipitation and a concomitant reduction of the antigen-binding capacity by about 10% were observed upon reconstitution of lyophilized MN12. HP beta CD proved to be the most effective stabilizer to prevent degradation of lyophilized MN12 during storage. Compared with MN12 solutions, HP beta CD-containing lyophilized MN12 cakes were more resistant to heat-induced charge alterations and loss of antigen-binding capacity.
研究了冻干对单克隆抗体（MN12）稳定性的影响。MN12在不同配方（无冻干保护剂或存在蔗糖、右旋糖酐或羟丙基-β-环糊精（HPβCD））以及不同条件（有或无二次干燥）下进行冻干。随后，单克隆抗体在不同温度（4、37或56℃）下储存18或32天。作为对照，MN12溶液在相同条件下储存。无论使用何种冻干保护剂，冻干的MN12复溶后均出现沉淀，且抗原结合能力随之降低约10%。事实证明，HPβCD是防止冻干的MN12在储存期间降解的最有效稳定剂。与MN12溶液相比，含HPβCD的冻干MN12饼对热诱导的电荷变化和抗原结合能力丧失更具抗性。
