| 引用本文: | 郭莎,李涵涵,祁志云,许东泽,吴昊.生物制剂中聚山梨醇酯的降解及其对制剂稳定性的影响 [J].中国现代应用药学,2024,41(18):87-96. |
| guo sha,li han han,qi zhi yun,xu dong ze,wu hao.The Degradation of Polysorbates in Biologics and Its Impact on Formulation Stability[J].Chin J Mod Appl Pharm(中国现代应用药学),2024,41(18):87-96. |
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| 摘要: |
| 在生物制剂中,聚山梨醇酯(PS 20和PS 80)作为表面活性剂,能够有效防止蛋白质聚集,维持蛋白质的稳定性。然而,这些表面活性剂在储存和使用过程中可能会降解,生成游离脂肪酸和过氧化物,这些降解产物可能与蛋白质发生化学反应,导致蛋白质聚集甚至引发免疫原性。本研究综述了聚山梨醇酯的降解机制、影响降解的因素、降解对蛋白质稳定性的影响以及降解产物的检测方法,并探讨了未来的研究方向和挑战。 |
| 关键词: 聚山梨醇酯 降解机制 蛋白质稳定性 自氧化 水解 生物制剂 |
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| The Degradation of Polysorbates in Biologics and Its Impact on Formulation Stability |
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guo sha1, li han han2, qi zhi yun2, xu dong ze2, wu hao2
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1.National Institutes for Food and Drug Control;2.Shenyang Pharmaceutical University
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| Abstract: |
| In biologics, polysorbates (PS 20 and PS 80) are used as surfactants to effectively prevent protein aggregation and maintain protein stability. However, these surfactants can degrade during storage and use, producing free fatty acids and peroxides. These degradation products can chemically react with proteins, leading to protein aggregation and potentially inducing immunogenicity. This review summarizes the degradation mechanisms of polysorbates, factors influencing degradation, the impact of degradation on protein stability, and methods for detecting degradation products. Future research directions and challenges are also discussed. |
| Key words: polysorbate degradation mechanism protein stability auto-oxidation hydrolysis biologics |
