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首页> 外文期刊>Molecular pharmaceutics >Cocrystal Transition Points: Role of Cocrystal Solubility, Drug Solubility, and Solubilizing Agents
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Cocrystal Transition Points: Role of Cocrystal Solubility, Drug Solubility, and Solubilizing Agents

机译：共晶体转变点：共晶体溶解度，药物溶解度和增溶剂的作用

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摘要

In this manuscript we bring together concepts that are relevant to the solubilization and thermodynamic stability of cocrystals in the presence of drug solubilizing agents. Simple equations are derived that allow calculation of cocrystal solubilization and transition point solubility. Analysis of 10 cocrystals in 6 different solubilizing agents shows that cocrystal solubilization is quantitatively predicted from drug solubilization. Drug solubilizing agents such as surfactants and lipid-based media are also shown to induce cocrystal transition points, where drug and cocrystal solubilities are equal, and above which the cocrystal solubility advantage over drug is eliminated. We have discovered that cocrystal solubility at the transition point (S*) is independent of solubilizing agent, and can be predicted from knowledge of only the aqueous solubilities of drug and cocrystal. For 1:1 cocrystals, S* = (S-cocrystal,S-aq)(2)/S-drug,S-aq. S* is a key indicator of cocrystal thermodynamic stability and establishes the upper solubility limit below which cocrystal is more soluble than the constituent drug. These findings have important implications to tailor cocrystal solubility and stability in pharmaceutical formulations from commonly available drug solubility descriptors.
机译：在本手稿中，我们将与在药物增溶剂存在下共结晶的增溶和热力学稳定性相关的概念归纳在一起。推导出简单的方程式，可以计算共晶体的溶解度和过渡点溶解度。对6种不同增溶剂中10种共晶体的分析表明，共晶体的增溶是从药物增溶中定量预测的。还显示了药物增溶剂，例如表面活性剂和基于脂​​质的介质，可诱导共晶转变点，此时药物和共晶的溶解度相等，并且在该点以上，共晶的溶解度优势优于药物。我们已经发现，共晶在转变点（S *）的溶解度与增溶剂无关，并且可以仅根据药物和共晶的水溶性来预测。对于1：1共结晶，S * =（S-共结晶，S-aq）（2）/ S-药物，S-aq。 S *是共晶热力学稳定性的关键指标，并确定了溶解度上限，在该上限以下，共晶比组成药物更易溶。这些发现对于根据常用的药物溶解度描述词来调整药物制剂中的共晶溶解度和稳定性具有重要意义。

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