In-situ Solid-state NMR Characterization of Pharmaceutical Materials: An Example of Drug-Polymer Thermal Mixing,Magnetic Resonance in Chemistry

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In-situ Solid-state NMR Characterization of Pharmaceutical Materials: An Example of Drug-Polymer Thermal Mixing
Magnetic Resonance in Chemistry ( IF 1.9 ) Pub Date : 2020-01-02 , DOI: 10.1002/mrc.4982
Jinglin Yin ₁ , Chengbin Huang ₂ , Hanxi Guan ₁ , Zhenfeng Pang ₁ , Yongchao Su _{2,

3} , Xueqian Kong ₁

Affiliation

Pharmaceutical amorphous solid dispersions (ASDs), a multi-component system prepared by dispersing drug substances into polymeric matrix via thermal and mechanical processes, represent a major platform to deliver the poorly water-soluble drug. Microscopic properties of drug-polymer contacts play mechanistic roles in manipulating long-term physical stability as well as dissolution profiles. While solid-state NMR (ssNMR) has been utilized as an indispensable tool to probe structural details, previous studies are limited to ex-situ characterizations. Our work provides likely the first documented example to investigate co-melting of ketoconazole (KTZ) and polyacrylic acid (PAA), as a model system, in an in-situ manner. Their physical mixture is melted and mixed in the ssNMR rotor under magic angle spinning at up to approximately 400 K. Critical structural events of molecular miscibility and interaction have been successfully identified. These results design and evaluate the instrumental and experimental protocols for real-time characterizations of the co-melting of pharmaceutical materials.

中文翻译：

药物材料的原位固态 NMR 表征：药物-聚合物热混合示例

药物无定形固体分散体 (ASD) 是一种多组分系统，通过热和机械过程将药物物质分散到聚合物基质中，代表了提供水溶性差的药物的主要平台。药物-聚合物接触的微观特性在操纵长期物理稳定性和溶出曲线方面发挥着机械作用。虽然固态核磁共振 (ssNMR) 已被用作探测结构细节的不可或缺的工具，但以前的研究仅限于非原位表征。我们的工作可能提供了第一个记录在案的例子，以原位方式研究酮康唑 (KTZ) 和聚丙烯酸 (PAA) 作为模型系统的共熔。它们的物理混合物在 ssNMR 转子中在高达约 400 K 的魔角旋转下熔化并混合。分子混溶和相互作用的关键结构事件已被成功鉴定。这些结果设计和评估了用于药物材料共熔实时表征的仪器和实验方案。

更新日期：2020-01-02

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