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溶解剂对基基甲基纤维素基无形固体分散片的结构和分解的影响
Natsuki Takahashi1, Miho Inoue2, Takayuki Terukina2
1Department of Pharmaceutical Engineering and Drug Delivery Science, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-Ku, Shizuoka-Shi, Shizuoka, 422-8526, Japan; Analytical Research Labs., Astellas Pharma Inc., 180 Ozumi, Yaizu-shi, Shizuoka, 425-0072, Japan.
溶解剂的选择对无形固体分散 (ASD) 片的性能产生了重大影响. 克罗斯波维 (CPV) 维持了平板电脑的分解,与克罗斯卡梅洛 (CCS) 不同,由于HPMC的结构变化导致延迟.
科学领域:
- 制药技术 制药技术 制药技术
- 材料科学 材料科学 材料科学
背景情况:
- 无形固体分散 (ASDs) 提高了水溶性较差的药物的溶性.
- 储存后ASD药片的分解延迟是一个主要的配方挑战.
研究的目的:
- 调查分解性质如何影响含有灰色富尔 (GRF) 的基于基基甲基纤维素 (HPMC) 的ASD药片的分解.
- 为了评估交叉糖 (CCS) 和交叉维 (CPV) 对ASD药片结构和加速储存下的性能的影响.
主要方法:
- 动态粘弹性测量 动态粘弹性测量
- 硬度测试 硬度测试 硬度测试
- 在加速储存条件下 (40°C/75%RH) 进行分解试验.
主要成果:
- 解体型显著影响了HPMC在储存后的结构重组.
- 由于HPMC链的重新排列,CCS导致了塑化和延迟的解体,这是由于保留水的便利.
- 通过其吸收能力,CPV保持了平板电脑的完整性和分解性能,防止结构变化.
结论:
- 溶解剂的选择对于优化ASD药片分解和药物吸收至关重要.
- 了解分解机制是开发具有改善生物可用性的稳定有效的ASD配方的关键.
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