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首页> 外文期刊>Crystal growth & design >Enhancing the Solubility of 6-Mercaptopurine by Formation of Ionic Cocrystal with Zinc Trifluoromethanesulfonate:Single-Crystal-to-Single-Crystal Transformation
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Enhancing the Solubility of 6-Mercaptopurine by Formation of Ionic Cocrystal with Zinc Trifluoromethanesulfonate:Single-Crystal-to-Single-Crystal Transformation

机译：通过三氟甲烷磺酸锌形成离子共晶体来增强6-巯基嘌呤的溶解度：单晶到单晶的转化

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摘要

An antitumor drug, 6-mercaptopurine monohydrate (MP?H_2O), has a low oral bioavailability due to its poor aqueous solubility. In order to improve its solubility, two ionic cocrystals of 6-mercaptopurine with zinc trifluoromethanesulfonate (Zn(CF_3SO_3)_2), [Zn(MP)_2(H_2O)_2](CF_3SO_3)_2?2H_2O (1) and [Zn(MP)_2](CF_3SO_3)_2 (2), were prepared. Slow evaporation of the methanol solution containing 1 gave the crystals of [Zn(MP)_2(H_2O)(MeOH)](CF_3SO_3)_2?H_2O (1a). Single-crystal-to-single-crystal transformation occurred under certain conditions, in which 1a transformed to 1 in the open air around 10 ℃, and 1 further transformed to [Zn(MP)_2(H_2O)](CF_3SO_3)_2 (1b) at room temperature (~25 ℃) and low RH%. The structures of 1, 1a, and 1b were determined by single crystal X-ray diffraction, in which MP and Zn(CF_3SO_3)_2 were assembled via coordination bonds and hydrogen bonds, and the coordination geometry of Zn(II) changed from octahedron in 1 and 1a to square pyramid in 1b. After the formation of ionic cocrystals of 1 and 2, both the apparent solubility and dissolution rate were increased.
机译：抗肿瘤药6-巯基嘌呤一水合物（MP2H_2O）由于水溶性差，口服生物利用度低。为了提高其溶解度，6-巯基嘌呤与三氟甲磺酸锌的两个离子共晶体（Zn（CF_3SO_3）_2），[Zn（MP）_2（H_2O）_2]（CF_3SO_3）_2？2H_2O（1）和[Zn（MP ）_2]（CF_3SO_3）_2（2）的制备。缓慢蒸发含有1的甲醇溶液，得到[Zn（MP）_2（H_2O）（MeOH）]（CF_3SO_3）_2→H_2O的晶体（1a）。在一定条件下发生单晶到单晶的转变，其中1a在大约10℃的露天环境中转变为1，然后1a进一步转变为[Zn（MP）_2（H_2O）]（CF_3SO_3）_2（1b ）在室温（〜25℃）和低RH％下。通过单晶X射线衍射确定1、1a和1b的结构，其中MP和Zn（CF_3SO_3）_2通过配位键和氢键组装，并且Zn（II）的配位几何形状从八面体变为1和1a到1b中的方形金字塔。形成离子共晶1和2后，表观溶解度和溶解速率均增加。

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