聚合物来源变化的影响,在甲装载眼科插件中对水凝结构和产品性能的影响
Michael A VandenBerg1, Rokon Uz Zaman2, Christine L Plavchak1
1Office of Pharmaceutical Quality Research, Office of Pharmaceutical Quality, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD 20993, USA.
International journal of pharmaceutics
|July 11, 2025
概括
开发通用眼科插件需要对聚乙烯糖醇 (PEG) 助剂进行详细分析. PEG质量的变化显著影响水凝的特性和甲释放动力学,这对仿制药开发至关重要.
科学领域:
- 眼科药物输送是眼科药物输送.
- 聚合物科学 聚合物科学
- 制药发展 制药发展
背景情况:
- 持续释放的眼科插件在局部药物输送方面比眼滴具有优势.
- 聚乙烯甘醇 (PEG) 水凝插件用于持续释放的药物,如德克萨米他.
- 开发基于PEG的通用插件是困难的,因为在表征非活性成分方面存在挑战.
研究的目的:
- 调查聚乙烯糖醇 (PEG) 助剂变异对德克萨米他眼科插入物质的影响.
- 建立聚合物质量,水凝微结构和药物释放动力学之间的相关性.
- 突出综合分析方法对于仿制药产品开发的重要性.
主要方法:
- 使用NMR,FTIR,MALDI和SEC进行PEG前体材料和制造插件的表征.
- 通过X射线显微镜,热,机械和密度测量,分析插入网络属性,包括孔径,孔径大小,机械强度和结晶性.
- 在体外药物释放测试和与胀率和德克萨米他颗粒大小的相关性.
主要成果:
- 确定了PEG终端组功能化,杂质含量和分子重量的变化.
- 辅助剂的差异导致了水凝网络特性和插入微观结构的显著变化.
- 药物释放特征在不同配方中有所不同,与水凝膨胀率和德克萨米他颗粒大小相关.
结论:
- 综合性表征对于了解辅助剂质量如何影响眼科插入器性能至关重要.
- 在PEG质量,水凝微结构和药物释放动力学之间建立了相关性.
- 为了成功开发通用持续释放眼科插件,进行全面的分析评估至关重要.
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