Cocrystals have been identified as a method for ensuring the delivery of poorly soluble drugs. Development of cocrystal phases presents many challenges, with the in vivo drug delivery benefits difficult to predict robustly. Additional to this, many of the benefits seen in the literature do not use formulation strategies which are representative of the clinical dosage form. Zafirlukast has been shown to possess poor development properties. It is poorly soluble and difficult to manufacture. Here we present a case study highlighting the benefits of cocrystals in this context, outlining the discovery, formulation and improved pharmacokinetics of mixed stoichiometry cocrystals of zafirlukast. This case study outlines methods, which could be broadly applied to other drug molecules, for determination of the properties of cocrystals through a suite of in vitro experiments that display a predictive pathway from physical form discovery to enhanced in vivo activity in animal models.

中文翻译：

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扎鲁司特混合化学计量共晶体的性质预测和药代动力学评估，药物递送案例研究†

共晶已被确认为确保递送难溶性药物的方法。在体内，共晶相的发展提出了许多挑战药物输送的好处很难可靠地预测。除此之外，文献中看到的许多好处都没有使用代表临床剂型的制剂策略。扎鲁司特已显示出较差的发育特性。它溶解性差，难以制造。在这里，我们提供了一个案例研究，突出了在这种情况下共晶体的好处，概述了扎鲁司特混合化学计量共晶体的发现，配方和改进的药代动力学。本案例研究概述了可通过一系列体外实验确定共晶特性的方法，这些方法可广泛应用于其他药物分子，这些体外实验显示了从物理形式发现到体内增强的预测途径 动物模型中的活动。