药物共晶及其在改善活性药物成分固态性能中的作用

Ameera A Radhi, Iman S Jaafar, Noor S Jaafar, Sarah M Faisal
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引用次数: 0

摘要

共结晶是一种新兴的方法,用于改善活性药物成分(API)的物理化学特性,例如溶解速度,溶解度,稳定性以及机械性能,而不影响其治疗活性。当盐或多晶形成等其他方法没有遇到估计目标时,这是非常重要的。本文综述了药物共晶的发展概况,重点介绍了影响共晶的因素,包括:∆pKa、供体和受体氢键、分子识别点、合成形成官能团的灵活性、二羧酸共晶碳链长度和溶剂效应,以及共晶的制备方法。此外,还讨论了共晶表征、溶出模式以及可商品化的产品。
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Pharmaceutical cocrystal and their role in improving solid state properties of active pharmaceutical ingredients
Cocrystallization is an emerging approach for improving physico-chemical characteristics of an active pharmaceutical ingredient (API) for instance dissolution rate, solubility, stability in addition to mechanical properties without affecting their therapeutic activity. It is of great importance when other approaches like salt or polymorph formation do not encounter the estimated targets. In this review article, an outline of pharmaceutical cocrystals will be presented, with highlighting on factors affecting cocrystallization which include ∆pKa, donors and acceptors hydrogen bonds, molecular recognition point, synthon forming functional groups flexibility, dicarboxylic acid coformers carbon chain length and solvent effect, as well as and the methods for cocrystal preparation. Additionally, cocrystal characterization, dissolution pattern as well as the commercially available products were discussed.
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