Sucrose and Trehalose in Therapeutic Protein Formulations
Sucrose and Trehalose in Therapeutic Protein Formulations
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治疗性蛋白质制剂中的蔗糖和海藻糖
DOI：
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发表时间：
2018
期刊：
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通讯作者：
S. Singh
中科院分区：
文献类型：
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作者：
S. Singh
蔗糖和海藻糖是生物治疗剂的配制和稳定的关键成分。它们的效用和功能是由其独特的化学和物理性质驱动的，特别是在本章总结的水溶液中。有共性，以及从他们的构象，氢键特性，水结合能力，玻璃化转变温度，多晶型行为，溶解度，化学稳定性等产生的这些性质的差异。这两种糖都非常适合提供溶液状态的稳定，以及冷冻和冻干保护，治疗蛋白作为制剂中的赋形剂。这两种糖都有药典专论，安全性和耐受性已得到充分证明。尽管最终评估取决于个体生物量，但经验表明，除非受到低pH制剂的限制，否则在大多数情况下，蔗糖通常被认为是合适的。
Sucrose and trehalose are key ingredients in the formulation and stabilization of biotherapeutics. Their utility and function is driven by their unique chemical and physical properties, especially in aqueous solutions which are summarized in this chapter. There are commonalities as well as differences in these properties that arise from their conformation, H-bonding characteristics, water-binding ability, glass transition temperatures, polymorphic behavior, solubility, chemical stability etc. Both sugars are well suited to provide solution-state stabilization, as well as cryo- and lyo-protection, for therapeutic proteins as excipients in the formulations. Compendial monographs are available for both sugars, and the safety and tolerability have been well documented. Although the final assessment is dependent on the individual biotherapeutic, experience suggests that sucrose can generally be considered as suitable in most cases, unless constrained by a low-pH formulation.