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首页> 外文期刊>Acta Crystallographica, Section B. Structural science, crystal engineering and materials >First-line antituberculosis drug, pyrazinamide, its pharmaceutically relevant cocrystals and a salt
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First-line antituberculosis drug, pyrazinamide, its pharmaceutically relevant cocrystals and a salt

机译：一线抗结核剂药物，吡嗪酰胺，其药学相关的钴和盐

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摘要

A few pyrazinamide (Pyz) cocrystals involving hydroxybenzoic/cinnamic acid derivatives [2,4-dihydroxybenzoic acid (24DHBA); 2,6-dihydroxybenzoic acid (26DHBA); 3,5-dihydroxybenzoic acid (35DHBA) and nutraceutical molecule ferulic acid (FRA)] and the first example of a molecular salt with ptoluenesulfonic acid (pTSA) have been prepared and characterized using various solid-state techniques. A high-temperature cocrystal polymorph of Pyz·FRA has been characterized from the endothermic peaks observed using differential scanning calorimetry. The presence of substituent groups carrying hydrogen bond donors or acceptors and their influence on supramolecular synthon formation has been investigated using a Cambridge Structural Database search. Equilibrium solubility of all the binary complexes of Pyz follows the order of their coformer solubility, i.e. Pyz~+·pTSA~- > Pyz·35DHBA > Pyz > Pyz·26DHBA > Pyz·24DHBA > Pyz·FRA. A twofold enhancement in solubility of Pyz~+·pTSA~- molecular salt compared with the parent drug suggests a potential drug formulation for the treatment of tuberculosis.
机译：涉及羟基苯甲酸/肉桂酸衍生物的几种吡嗪酰胺（PYZ）酰基酯[2,4-二羟基苯甲酸（24dhba）; 2,6-二羟基苯甲酸（26dhba）;已经制备了3,5-二羟基苯甲酸（35dHBa）和营养素分子阿魏酸（FRA）和具有丙酮酸（PTSA）的分子盐的第一实例，并使用各种固态技术表征。使用差示扫描量热法观察到的PIZ·FRA的高温聚晶多晶型物的特征在于观察到的吸热峰。使用剑桥结构数据库搜索研究了携带氢键供体或受体的取代基或受体的影响及其对超分子合成的影响。 PYZ的所有二元络合物的平衡溶解度遵循其CoFormer溶解度的顺序，即PyZ〜+·PTSA〜 - > PYZ·35DHBA> PYZ> PYZ·26DHBA> PYZ·24DHBA> PYZ·FRA。与母体药物相比，PYZ〜+·PTSA〜 - 分子盐溶解度的两倍提高了潜在的药物制剂，用于治疗结核病。

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