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Differential Scanning Calorimetry Study of the Ibuprofen–Nicotinamide Binary Disperse System and the Anti-Inflammatory Activity of One of Its Secondary Eutectics
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-11-27 , DOI: 10.1007/s11094-020-02302-y
L. E. Zhnyakina , M. L. Tkachenko , Yu. V. Moshchenskii , I. I. Munina

Phase equilibria in the solid disperse system ibuprofen–nicotinamide were studied by differential scanning calorimetry (DSC). It was established that a cocrystal (called ibunicamide) formed at a 1:1 mole ratio of ibuprofen and nicotinamide. Ibunicamide had a melting point of 91°C and underwent a simple eutectic reaction with each of the starting compounds ibuprofen and nicotinamide. The parameters of the invariant equilibrium points were determined for the secondary systems ibuprofen–ibunicamide (E1) and ibunicamide–nicotinamide (E2). Eutectics of these secondary systems appeared at mole ratios 74:26 (±1) with a eutectic melting point of 61°C (E1) and at 82:18 (±1) with melting point 82°C (E2) for the second eutectic composition. Experimental comparison of ibuprofen and the ibuprofen–nicotinamide (ibunicamide) eutectic system showed that the new composition reduced carrageenan-induced exudation by greater than 23 times as compared to the group of animals that were not treated with the NSAID. Also, the exudation after pretreatment with pure ibuprofen at the same dose was only halved. Thus, a new anti-inflammatory and analgesic drug based on the cocrystal of the ibuprofen–nicotinamide eutectic system (ibunicamide) was obtained and tested. The test results demonstrated that the anti-inflammatory activity of ibuprofen in the eutectic composition exceeded its activity in the pure form by greater than 10 times.



中文翻译:

布洛芬-烟酰胺二元分散体系的差示扫描量热研究及其次级共晶之一的抗炎活性

通过差示扫描量热法(DSC)研究了固体分散体系布洛芬-烟酰胺的相平衡。可以确定以布洛芬和烟酰胺的摩尔比为1:1形成共晶体(称为布丁酰胺)。布丁酰胺的熔点为91℃,并且与每种起始化合物布洛芬和烟酰胺进行简单的共晶反应。确定了次级系统布洛芬-布尼酰胺(E 1)和布酰胺-烟酰胺(E 2)的恒定平衡点参数。这些次级体系的共晶以摩尔比74:26(±1)出现,共晶熔点为61°C(E 1),以82:18(±1)出现,熔点为82°C(E 2))用于第二共晶成分。布洛芬和布洛芬-烟酰胺(ibunicamide)低共熔系统的实验比较表明,与未经NSAID治疗的动物组相比,新组合物将角叉菜胶诱导的渗出减少了23倍以上。同样,用相同剂量的纯布洛芬预处理后的渗出仅减半。因此,获得并测试了一种基于布洛芬-烟酰胺共晶系统(ibunicamide)共晶的新型消炎镇痛药。试验结果表明,在低共熔组合物中,布洛芬的抗炎活性超过其纯形式的活性的10倍以上。

更新日期:2020-11-27
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