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颗粒化方法和改善洛克索含酸盐片硬度的机制
Aya Kuwata1,2, Agata Ishikawa1, Tetsuo Ono1
1Research & Development Headquarters Self-Medication, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-Cho, Kita-ku, Saitama 331-9530, Japan.
Pharmaceutics
|April 26, 2025
概括
洛克索酸盐 (LXP) 片的硬度受颗粒化溶剂和干燥温度的影响. 乙醇和较低的干燥温度通过影响表面自由能量和粒子凝聚力来改善平板电脑的硬度.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 洛克索 (LXP) 通常存在于二水合物形式.
- 药片硬度是制药配方的关键质量属性.
- 湿颗粒是一种常见的制备片剂的方法.
研究的目的:
- 为了研究洛克索 (LXP) 的压缩机制.
- 为了确定影响LXP片在湿颗粒过程中的硬度的参数.
- 了解溶剂和干燥条件对LXP片的特性所起的作用.
主要方法:
- 用水或乙醇作为溶剂制备LXP颗粒.
- 颗粒在各种条件下干燥,并根据颗粒大小进行选.
- 在添加1%的基酸盐 (Mg-st) 后,药片被压缩.
- 使用主要成分分析 (PCA) 和晶体结构分析.
主要成果:
- 颗粒化溶剂和干燥温度显著影响了药片的硬度.
- 乙醇作为溶剂导致平板电脑硬度比水更高.
- 平板硬度与表面自由能量 (SFE) 和极性成分 (γ(p)) 有正相关,与分散成分 (γ(d)) 有负相关.
- 无水LXP形式,受到特定的干燥温度的青,由于增加了g (p) 的硬度,表现出更高的硬度.
结论:
- 优化溶剂选择和干燥温度对于提高LXP平板硬度至关重要.
- 表面自由能量评估有助于选择适当的辅助剂,以改善平板电脑的性能.
- 了解LXP水合状态及其对物理性质的影响,是配方开发的关键.
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