用时域NMR测量T2放松计量无形固体分散中的活性药物成分的定量评价
Tsunenobu Katsumata1, Hiromu Taguchi2, Yusuke Minamino2
1Formulation Development Department, Development & Planning Division, Nichi-Iko Pharmaceutical Co., Ltd., 205-1 Shimoumezawa, Namerikawa, Toyama, 936-0857, Japan.
这项研究引入了时间域NMR T2放松计,作为一种新的方法来量化固体分散剂 (SD) 中的活性药物成分 (API) 水晶性. 该技术准确地测量了API晶度,为传统方法提供了有价值的替代方案.
科学领域:
- 制药科学
- 分析化学
- 材料科学
背景情况:
- 固体分散 (SD) 对于提高药物的溶解性和生物可用性至关重要.
- 在药物开发和质量控制中,精确量化药物活性成分 (API) 结晶度至关重要.
- 像粉末X射线衍射 (PXRD) 这样的传统方法可能耗时并且需要样本准备.
研究的目的:
- 提出并验证一种使用时间域核磁共振 (TD-NMR) T2放松计量方法来量化SD中的API晶度.
- 确定TD-NMR T2放松特征与API晶体与无形比的相关性.
- 为了证明TD-NMR T2放松计的准确性和适用性,作为PXRD的替代方法,用于评估SD中的API结晶性.
主要方法:
- 使用印美 (IMC) 和聚烯 (PVP) 制备模型固体分散剂 (SD).
- 使用时域核磁共振 (TD-NMR) T2放松计来进行放松测量.
- 在物理混合物 (PMs) 中分析了T2放松行为与不同晶体-非晶体IMC比率的关系.
- 将TD-NMR T2放松度结果与常规粉末X射线衍射 (PXRD) 进行比较以验证.
主要成果:
- 在T2放松率和晶体与非晶体的IMC比率之间发现了明显的线性关系.
- 在加速储存条件下,TD-NMR T2放松度测量与PXRD测量SD中的IMC结晶度非常一致.
- 在SD和物理混合物之间,T1放松行为有显著差异,而T2行为则相似.
结论:
- 时间域NMR (TD-NMR) T2放松计是一种可靠且准确的方法,用于量化固体分散中的API结晶性.
- 这种技术为PXRD等传统方法提供了有价值的,非破坏性的替代方案.
- TD-NMR T2放松计为监测药物配方的物理稳定性和结晶性变化提供了一个敏感的工具.
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