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首页> 外文期刊>Crystal growth & design >Cocrystallization Enhanced TAK-441 Aqueous Solubility and Suppressed High Solvatomorphism
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Cocrystallization Enhanced TAK-441 Aqueous Solubility and Suppressed High Solvatomorphism

机译：共结晶增强了TAK-441的水溶解度并抑制了其高溶同性

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摘要

TAK-441 was cocrystallized to enhance its aqueous solubility and suppress its high solvatomorphism. A TAK-441/l-malic acid (2:1) cocrystal and a TAK-441/l-tartaric acid (2:1) cocrystal were observed, and they exhibited isomorphism. These cocrystals were 2-3 times more soluble than its free form in aqueous solutions and directly crystallized without solvate formation in various organic solvents. The cocrystals were chemically and physically stable under stress conditions and are predicted to have sufficient stability to ensure an adequate shelf life. The results demonstrated that the cocrystals had a more preferable pharmaceutical profile and that cocrystallization can both improve oral bioavailability and simplify crystal form control simultaneously.
机译：将TAK-441共结晶以增强其水溶性并抑制其高度溶剂化。观察到TAK-441 / 1-苹果酸（2：1）共晶和TAK-441 / 1-酒石酸（2：1）共晶，它们表现出同构。这些共晶体在水溶液中的溶解度为其游离形式的2-3倍，并且可以直接结晶而在各种有机溶剂中不形成溶剂化物。共晶体在应力条件下是化学和物理稳定的，预计具有足够的稳定性以确保足够的货架寿命。结果表明，共晶具有更优选的药物特性，并且共结晶既可以改善口服生物利用度，又可以同时简化晶型控制。

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