综述专论

蛋白药物中聚山梨酯的降解及潜在风险研究进展*

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  • 1.国家药品监督管理局药用辅料质量研究与评价重点实验室,中国食品药品检定研究院,北京 100050;
    2.国家药品监督管理局药物制剂及辅料研究与评价重点实验室,中国药科大学,南京 210009;
    3.上海市医疗器械化妆品审评核查中心,上海 200001
第一作者 王 珏 Tel: 13371669032; E-mail:myxwj2007@163.com
江 颖 Tel: 15103283315; E-mail:jy17800274701@163.com
**Tel: (010)53852486; E-mail:sunhm@126.com

收稿日期: 2021-07-16

  网络出版日期: 2024-06-24

基金资助

*国家科技重大专项资助项目(2017ZX09101001006);中国食品药品检定研究院中青年发展研究基金资助项目(No. 2018C7)

Research progress on degradation and potential risks of polysorbates in protein pharmaceutical preparations*

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  • 1. NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients, National Institutes for Food and Drug Control, Beijing 100050, China;
    2. NMPA Key Laboratory for Research and Evaluation of Pharmaceutical Preparations and Excipients, China Pharmaceutical University, Nanjing 210009, China;
    3. Evaluation and Verification Center for Medical Equipment and Cosmetics of ShangHai, Shanghai 200020, China

Received date: 2021-07-16

  Online published: 2024-06-24

摘要

聚山梨酯20和聚山梨酯80是蛋白药物制剂中常用的稳定剂,但二者本身具有复杂的降解途径,降解产物会对蛋白药物的稳定性和安全性均产生影响。降解产物不仅可能带来直接的免疫原性,还会对蛋白质造成氧化损伤,引起蛋白质不稳定,参与蛋白质药物中颗粒的形成,进而导致免疫原性和使用风险。理解、预测和防止聚山梨酯20和聚山梨酯80的降解对减少其对蛋白药物的不良影响,使其更好的发挥稳定剂的作用至关重要。本文综述了蛋白药物制剂中聚山梨酯20和聚山梨酯80可能的降解途径及潜在风险,旨在为制定相关质量标准、建立动态分析过程保证蛋白药物制剂中聚山梨酯的完整性提供理论依据。

本文引用格式

王珏, 江颖, 孙春萌, 杨锐, 孙会敏 . 蛋白药物中聚山梨酯的降解及潜在风险研究进展*[J]. 药物分析杂志, 2022 , 42(9) : 1483 -1492 . DOI: 10.16155/j.0254-1793.2022.09.01

Abstract

Polysorbate 20 and polysorbate80 are commonly used in protein pharmaceutical preparationsas stabilizing agents. However, they both have multiple degradation pathways, and the degradation products may have side effects on the stability and safety of protein drugs.The degradation products may not only bring direct immunogenicity, but also cause oxidative damage to the protein, cause protein instability, and participate in the formation of particles in protein drugs, which further leads to immunogenicity and risk of use.Understanding, predicting and preventing the degradation of polysorbate 80 and polysorbate 20 is very important to reduce their adverse effects and makes them play a better role as stabilizers. In this paper, the possible degradation pathways and potential risks of polysorbate 80 and polysorbate 20 in protein pharmaceutical preparations were summarized, aiming to provide theoretical basis for formulating relevant standards, establishing dynamic analysis process and ensuring the integrity of polysorbates in protein pharmaceutical preparations.

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