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首页> 外文期刊>Crystal growth & design >Approach of cocrystallization to improve the solubility and photostability of tranilast
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Approach of cocrystallization to improve the solubility and photostability of tranilast

机译：共结晶法提高曲尼司特的溶解度和光稳定性

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摘要

The cocrystals and salts of an antiallergic drug, tranilast, were synthesized to improve its solubility and photostability. Two tranilast cocrystals with urea (1) and nicotinamide (2), as well as two salts with cytosine (3) and sodium ion (4), were obtained and characterized by infrared spectra, thermogravimetric analyses, differential scanning calorimetry, and powder and single crystal X-ray diffractions. The results of single crystal structure analyses of 1-3 indicate that tranilast combines amide groups in coformers via R2_2(8) synthon, resulting in a 1:1 stoichiometry. The complexes showed advantages in terms of solubility and photostability in comparison to pure tranilast. The maximum solubility values of 1-3 in phosphate buffer of pH 6.8 are approximately 1.6, 1.9, and 2.0 times as large as that of tranilast, and the residual of tranilast is 79.5, 92.9, 88.5, 86.2, and 87.4% for tranilast and 1-4, respectively, under the fluorescent lamp irradiation for 96 h.
机译：合成了抗过敏药物曲尼司特的共晶体和盐，以提高其溶解度和光稳定性。获得了两个尿素（1）和烟酰胺（2）的曲尼司特共晶体，以及胞嘧啶（3）和钠离子（4）的两种盐，并通过红外光谱，热重分析，差示扫描量热法，粉末和单相进行了表征。晶体X射线衍射。 1-3的单晶结构分析结果表明，曲尼司特通过R2_2（8）合成子在共形成体中结合了酰胺基，化学计量比为1：1。与纯曲尼司特相比，该络合物在溶解性和光稳定性方面显示出优势。在pH 6.8的磷酸盐缓冲液中1-3的最大溶解度值约为曲尼司特的1.6、1.9和2.0倍，曲尼司特和曲尼司特的残留量分别为79.5、92.9、88.5、86.2和87.4％。 1-4，分别在荧光灯照射下96小时。

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