在液体配方中导航2-基-β-环氧二烯的使用:对物理性质和表面活性剂兼容性的系统研究
Rakesh Dachineni1, Haichen Nie1
1Drug Product Development, Biologics CMC, Teva Branded Pharmaceutical Products R&D LLC, West Chester, PA 19380, USA.
International journal of pharmaceutics
|December 15, 2025
概括
2- propyl-β-cyclodextrin (HPβCD) 可以改善液体和冷凍配方. 然而,HPβCD可以与聚酸盐引起相分离,影响配方的稳定性和清晰度.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 材料科学 材料科学 材料科学
背景情况:
- 2-propyl-β-cyclodextrin (HPβCD) 是一种用于制药配方的多功能辅助剂.
- 了解HPβCD的物理特性和相互作用对于开发稳定的液体和冷解药物产品至关重要.
- 辅助剂的兼容性,特别是与聚酸盐等表面活性剂的兼容性,显著影响配方性能.
研究的目的:
- 评估HPβCD在液体配方中的物理性质和热行为.
- 评估HPβCD与常见辅助剂的兼容性,重点关注聚酸盐.
- 使用热图开发相位图,以预测和防止包含HPβCD的配方中的相位分离.
主要方法:
- 在各种条件下对HPβCD的度,粘度和玻璃过渡温度 (Tg') 的系统评估.
- 高通量紫外线灭测量和主要组件分析以生成相位图.
- 在HPβCD与多酸盐 (PS80,PS20) 和波洛克萨默188 (P188) 的二元混合物中评估相位分离.
主要成果:
- HPβCD显示了合适的度和粘度范围,并且可以增强Tg'以提高配方稳定性.
- 在HPβCD/PS80和HPβCD/PS20溶液中观察到相分离,暗示度增加.
- 与PS20相比,PS80的相分离更严重,表明度依赖的相互作用;P188没有诱导相分离.
结论:
- 惠普βCD是液体和冷化配方的有价值的辅助剂,但其与聚酸盐的兼容性需要仔细考虑.
- 阶段映射为选择辅助剂和优化度提供了定量方法,以确保配方清晰度和物理稳定性.
- 彻底的辅助剂兼容性研究,包括相位映射,对于开发可靠的无菌注射配方和减轻相位分离风险至关重要.
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