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Preparation, characterization and evaluation of aspirin: benzoic acid cocrystals with enhanced pharmaceutical properties
Future Journal of Pharmaceutical Sciences Pub Date : 2020-07-14 , DOI: 10.1186/s43094-020-00052-y
Braham Dutt , Manjusha Choudhary , Vikas Budhwar

The cocrystallization process in pharmaceuticals has gained widespread attention as a recent method of modifying physicochemical properties without altering the pharmacological characteristics of drugs. Cocrystallization provides a couple of benefits like it can be employed for a large number of APIs (acidic, basic, ionizable, or non-ionizable), and secondly, the availability of a large number of potential coformers increases the possibility of the cocrystals (CCs) that can be synthesized for an API. The main objective of this study was to investigate the effects of cocrystallization on drugs having poor aqueous solubility. Aspirin (AN) and benzoic acid (BZ) were cocrystallized by using the solvent evaporation technique. CSD (Cambridge Structure Database) software and ∆pKa value method were used for the selection of the drug and coformer and for prediction of CC formation. The analysis of CCs was performed using DSC (differential scanning calorimetry), FT-IR (Fourier transformation infra-red spectroscopy) and XRD (X-ray diffraction) techniques. In vivo anti-inflammatory studies were conducted on 24 Wistar rats divided into four groups. Here, in this study, in vitro dissolution studies revealed an improved solubility profile of CCs compared to pure drug and marketed formulation viz. 87%, 31% and 60% respectively. The in vivo anti-inflammatory studies exhibited improved anti-inflammatory activity compared to pure drug. So, on the basis of outcomes of this study, we concluded that cocrystallization process have a direct impact on the improvement of physicochemical characteristics of APIs having issues like solubility or stability without any modification and alteration of their pharmacological actions.

中文翻译:

具有增强药物特性的阿司匹林:苯甲酸共晶体的制备,表征和评价

作为改变物理化学性质而不改变药物药理学特性的最新方法,药物中的共结晶过程已引起广泛关注。共结晶提供了许多好处,例如可以用于大量的API(酸性,碱性,可电离或不可电离),其次,大量潜在的共形成物的可用性增加了共晶(CC)的可能性。 ),可以针对API进行综合。这项研究的主要目的是研究共结晶对水溶性差的药物的影响。使用溶剂蒸发技术将阿司匹林(AN)和苯甲酸(BZ)共结晶。使用CSD(剑桥结构数据库)软件和∆pKa值方法选择药物和共形成剂,并预测CC的形成。使用DSC(差示扫描量热法),FT-IR(傅里叶变换红外光谱)和XRD(X射线衍射)技术进行CC的分析。在分为四组的24只Wistar大鼠上进行了体内抗炎研究。在此,在这项研究中,体外溶出研究显示与纯药物和市售制剂相比,CC的溶出度有所改善。分别为87%,31%和60%。与纯药物相比,体内抗炎研究显示出改善的抗炎活性。因此,根据这项研究的结果,
更新日期:2020-07-14
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