稳定HP-β-CD对液体配方和通过电制成的固体配方中的infliximab的稳定作用
Fanni Angéla Geyer1, Júlia Domján1, Tibor Viktor Szalai2
1Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Műegyetem rkp. 3, H-1111, Budapest, Hungary.
概括
2- propyl-β-cyclodextrin (HP-β-CD) 在液体和固体配方中稳定了infliximab. 这种辅助剂在加工和储存过程中增强稳定性,减少聚合和单体损失,这对于生物制药开发至关重要.
科学领域:
- 制药科学 制药科学
- 生物化学 生物化学
- 材料科学 材料科学 材料科学
背景情况:
- 生物制药配方,特别是像Infliximab这样的单克隆抗体,面临着重大的稳定性挑战.
- 开发稳定的液体和固体剂型对于有效的药物输送和保质期至关重要.
研究的目的:
- 为了研究2-propyl-β-cyclodextrin (HP-β-CD) 对液体和固体配方的infliximab的稳定作用.
- 评估HP-β-CD在各种条件下在加工和储存期间对因弗力西马布稳定性的影响.
- 阐明HP-β-CD稳定因弗利西马布的基础分子机制.
主要方法:
- 使用高速电制备固体因弗利西马布配方.
- 配制具有不同HP-β-CD度的液体infliximab溶液.
- 压力测试和长期稳定性研究 (长达6个月) 评估单体回收,碎片和聚合物.
- 使用生物层干涉计和异热定位热量计的分子相互作用研究.
主要成果:
- 电固体配方表现出优异的溶解性能和在低温和湿度下有望稳定.
- 使用HP-β-CD的Infliximab配方显示,即使在室温下2个月后,单体损失也低于10%.
- 液体配方中HP-β-CD度的增加显著提高了因弗利西马布的稳定性和对机械应力的保护.
- HP-β-CD被证明可以降低infliximab的自我相互作用,与减少聚合相关.
结论:
- 惠普-β-CD是液体和固体Infliximab配方的高效稳定辅助剂.
- 惠普-β-CD显示了提高因弗利西马布生物治疗药物的耐热性和保质期的潜力.
- 稳定机制涉及减少因弗利克西马布的自我相互作用和聚合.
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