当前位置: X-MOL 学术Cryst. Growth Des. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Evidence for Halogen Bonding in Amorphous Solid Dispersions
Crystal Growth & Design ( IF 3.8 ) Pub Date : 2020-03-20 , DOI: 10.1021/acs.cgd.0c00073
Chailu Que 1 , Qingqing Qi 2 , Dmitry Y. Zemlyanov 3 , Huaping Mo 4 , Alexandru Deac 1 , Matthias Zeller 2 , Anura S. Indulkar 5 , Yi Gao 6 , Geoff G. Z. Zhang 5 , Lynne S. Taylor 1
Affiliation  

Carbon-bound halogen atoms (iodine, bromine, chlorine, and occasionally fluorine) are known to act as electron acceptors and form interactions with different species capable of acting as electron donors. This interaction is termed halogen bonding and shares some similarities with hydrogen bonding. While hydrogen bonding has been extensively studied as an important intermolecular interaction for many aspects of drug delivery and dosage form design, halogen bonding has not been investigated in these contexts. However, approximately one-third of all drug molecules contain halogen atoms. Using X-ray photoelectron spectroscopy, nuclear magnetic resonance spectroscopy, and infrared spectroscopy, it was demonstrated herein that halogen-bearing drugs that lack hydrogen bond donors form a halogen bonding interaction with the carbonyl group of a common pharmaceutical polymer, copovidone, in a solid amorphous blend. Halogen bonding thus may be a common but neglected intermolecular interaction in drug–polymer amorphous blends and is potentially important for the properties and performance of these systems which are used to enhance drug solubility and delivery. This is the first time that the occurrence of halogen bonding has been observed in drug–polymer formulations.

中文翻译:

非晶态固体分散体中卤素键的证据

已知碳键合的卤素原子(碘,溴,氯,偶尔还有氟)充当电子受体,并与能够充当电子供体的不同物种形成相互作用。这种相互作用称为卤素键,与氢键有一些相似之处。尽管氢键已被广泛研究为药物递送和剂型设计的许多方面的重要分子间相互作用,但在这些情况下尚未研究卤素键。但是,所有药物分子中约有三分之一含有卤素原子。使用X射线光电子能谱,核磁共振能谱和红外能谱,本文证明了缺乏氢键供体的含卤素药物与固体无定形共混物中的普通药物聚合物共聚维酮的羰基形成卤素键相互作用。因此,卤素键可能是药物-聚合物无定形共混物中常见但被忽略的分子间相互作用,对于这些用于增强药物溶解度和递送的系统的性能和性能而言可能非常重要。这是首次在药物-聚合物配方中观察到卤素键的出现。因此,卤素键可能是药物-聚合物无定形共混物中常见但被忽略的分子间相互作用,对于这些用于增强药物溶解度和递送的系统的性能和性能而言可能非常重要。这是首次在药物-聚合物配方中观察到卤素键的出现。因此,卤素键可能是药物-聚合物无定形共混物中常见但被忽略的分子间相互作用,并且对于这些用于增强药物溶解度和递送的系统的性能和性能可能潜在重要。这是首次在药物-聚合物配方中观察到卤素键的出现。
更新日期:2020-03-20
down
wechat
bug