Recent advances in pharmaceutical cocrystals of theophylline

IF 4.8 3区化学 Q1 CHEMISTRY, MEDICINAL Natural Products and Bioprospecting Pub Date : 2024-09-14 DOI:10.1007/s13659-024-00470-y

Yanxiao Jia, Dezhi Yang, Wenwen Wang, Kun Hu, Min Yan, Li Zhang, Li Gao, Yang Lu

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Abstract

Currently, cocrystallization is a promising strategy for tailoring the physicochemical properties of active pharmaceutical ingredients. Theophylline, an alkaloid and the most primary metabolite of caffeine, is a readily available compound found in tea and coffee. It functions primarily as a bronchodilator and respiratory stimulant, making it a mainstay treatment for lung diseases like asthma. Theophylline’s additional potential benefits, including anti-inflammatory and anticancer properties, and its possible role in neurological disorders, have garnered significant research interest. Cocrystal formation presents a viable approach to improve the physicochemical properties of theophylline and potentially mitigate its toxic effects. This review comprehensively explores several successful studies that utilized cocrystallization to favorably alter the physicochemical properties of theophylline or its CCF. Notably, cocrystals can not only enhance the solubility and bioavailability of theophylline but also exhibit synergistic effects with other APIs. The review further delves into the hydrogen bonding sites within the theophylline structure and the hydrogen bonding networks observed in cocrystal structures.

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茶碱药用共晶体的最新进展

目前，共晶是一种很有前途的定制活性药物成分理化特性的策略。茶碱是一种生物碱，也是咖啡因最主要的代谢产物，是一种在茶叶和咖啡中很容易找到的化合物。它的主要功能是支气管扩张剂和呼吸兴奋剂，是治疗哮喘等肺部疾病的主要药物。茶碱的其他潜在益处，包括抗炎和抗癌特性，以及在神经系统疾病中可能发挥的作用，引起了研究人员的极大兴趣。形成可可结晶是改善茶碱理化性质并减轻其毒性作用的一种可行方法。本综述全面探讨了几项成功利用共晶体化改变茶碱或其CCF理化性质的研究。值得注意的是，共晶体不仅能提高茶碱的溶解度和生物利用度，还能与其他原料药产生协同效应。本综述进一步探讨了茶碱结构中的氢键位点以及在共晶体结构中观察到的氢键网络。

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