Jia Yanxiao, Yang Dezhi, Wang Wenwen, Hu Kun, Yan Min, Zhang Li, Gao Li, Lu Yang
Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences, and Peking Union Medical College, Beijing, 100050, People's Republic of China.
Prescription Laboratory of Xinjiang Traditional Uyghur Medicine, Xinjiang Institute of Traditional Uyghur Medicine, Urumqi, 830000, People's Republic of China.
Nat Prod Bioprospect. 2024 Sep 14;14(1):53. doi: 10.1007/s13659-024-00470-y.
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.
目前,共结晶是一种用于调整活性药物成分物理化学性质的有前景的策略。茶碱是一种生物碱,也是咖啡因的主要初级代谢产物,是一种在茶和咖啡中常见的易得化合物。它主要起支气管扩张剂和呼吸兴奋剂的作用,使其成为哮喘等肺部疾病的主要治疗药物。茶碱的其他潜在益处,包括抗炎和抗癌特性,以及它在神经疾病中可能发挥的作用,已经引起了大量的研究兴趣。共晶形成是一种可行的方法,可以改善茶碱的物理化学性质,并有可能减轻其毒性作用。这篇综述全面探讨了几项成功的研究,这些研究利用共结晶来有利地改变茶碱或其共晶形式(CCF)的物理化学性质。值得注意的是,共晶不仅可以提高茶碱的溶解度和生物利用度,还可以与其他活性药物成分(API)表现出协同效应。该综述进一步深入研究了茶碱结构内的氢键位点以及在共晶结构中观察到的氢键网络。