阐明驱动可表化翻转现象的关键因素
Zijian Wang1, Chenguang Wang1, Changquan Calvin Sun1
1Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, USA.
International journal of pharmaceutics
|February 12, 2025
概括
药物配方中的可片性翻转现象 (TFP) 受助剂可塑性和颗粒大小的影响. 当添加辅助物质时,药物的可分片性降低时,TFP会发生,特别是具有相似的可塑性和特定颗粒特性的药物.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 片状性对于片状形成至关重要,它取决于粒子间粘合面积 (BA) 和粘合强度 (BS).
- таблетка性翻转现象 (TFP) 描述了与辅助剂配制时与纯形式相比,药物的 таблетка性下降.
- 影响BA和BS的因素,如机械性能和粒子特性,可以影响TFP,但缺乏系统的评估.
研究的目的:
- 系统地评估API加载,辅助剂类型,颗粒大小和片剂速度对TFP的影响.
- 确定影响TFP的发生和程度的关键配方和加工参数.
主要方法:
- 根据不同的API负载,辅助剂类型,颗粒大小 (API和辅助剂) 和片剂速度,研究了TFP.
- 分析了这些参数与观察到的平板拉伸强度和平板性之间的关系.
主要成果:
- 当辅助剂的可塑性与较软的API相匹配时,TFP的可能性更高,特别是在中间药物负载和高压缩压力下.
- 辅助剂颗粒大小对TFP的发生和程度都有重大影响.
- API颗粒大小和片制速度仅对TFP产生边际影响.
结论:
- 辅助剂的可塑性和颗粒大小是管理TFP的关键因素.
- 配方策略应考虑API和辅助剂的机械性能和颗粒特征之间的相互作用,以减轻TFP.
- 优化片剂条件,特别是辅助剂选择和颗粒大小,对于可预测的片剂性至关重要.
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