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Effect of Different Cellulose Polymers on the Crystal Growth of Celecoxib Polymorphs
Journal of Crystal Growth ( IF 1.7 ) Pub Date : 2020-06-01 , DOI: 10.1016/j.jcrysgro.2020.125638
Xiangjun Shi , Zejie Ding , Chao Wang , Shengjie Song , Xiyue Zhou

Abstract To reveal the effect of the proportions and various properties of cellulose polymers towards the stability of amorphous celecoxib (CEL), the crystallization behavior of CEL polymorphs (Form I, Form II, and Form IV) has been thoroughly investigated. The results show that the addition of cellulose polymers can induce the nucleation of Form II and Form IV instead of Form I. With an increase in the proportion of polymer addition, there was a decrease in the birefringence phenomenon of Form I, while Form II and Form IV were observed to change in the opposite direction. The crystal growth of the three polymorphs depended on the proportion of HPMC and the temperature of environment instead of the molecular weight of polymers. The crystal growth analysis suggests that the energy barrier for nucleation may be one of the key factors. The cellulose polymers with large-sized substituents exhibited a stronger inhibitory effect during the crystallization of CEL polymorphs, where the amorphous CEL remained more stable. This phenomenon can be explained by FT-IR spectroscopy and ΔTg analysis, suggesting that there may be a steric repulsion from the large-sized substituents of cellulose polymers, which affects the crystallization process of CEL polymorphs.

中文翻译:

不同纤维素聚合物对塞来昔布多晶型晶体生长的影响

摘要 为了揭示纤维素聚合物的比例和各种性质对无定形塞来昔布 (CEL) 稳定性的影响,已经彻底研究了 CEL 多晶型物(I 型、II 型和 IV 型)的结晶行为。结果表明,纤维素聚合物的加入可以诱导 Form II 和 Form IV 的成核,而不是 Form I。随着聚合物加入比例的增加,Form I 的双折射现象减少,而 Form II 和 Form II 的双折射现象减少。观察到形式IV以相反的方向变化。三种多晶型物的晶体生长取决于HPMC的比例和环境温度而不是聚合物的分子量。晶体生长分析表明,成核的能垒可能是关键因素之一。具有大尺寸取代基的纤维素聚合物在 CEL 多晶型物的结晶过程中表现出更强的抑制作用,其中无定形 CEL 保持更稳定。这种现象可以通过 FT-IR 光谱和 ΔTg 分析来解释,表明纤维素聚合物的大尺寸取代基可能存在空间排斥,这影响了 CEL 多晶型物的结晶过程。
更新日期:2020-06-01
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