Evaluation of Cocrystallization Outcomes of Multicomponent Adducts: Rapid Fabrication to Achieve Uniform Particle Size Distribution Using Thermal Inkjet Printing,Crystal Growth & Design

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Evaluation of Cocrystallization Outcomes of Multicomponent Adducts: Rapid Fabrication to Achieve Uniform Particle Size Distribution Using Thermal Inkjet Printing
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-05-20 , DOI: 10.1021/acs.cgd.0c00469
Raviteja Seera ₁ , Tayur N. Guru Row ₁

Affiliation

Multicomponent adducts such as cocrystals and eutectics have become an integral part of the pharmaceutical industry since the application potential of such products is imminent in drug design and fabrication. Cocrystallization of metronidazole, an antibiotic antiprotozoal drug, belonging to the family of nitro-imidazole, with benzoic acid and mono-, di-, tri-, hydroxybenzoic acids results in multicomponent adducts with better physicochemical properties than the drug. Cocrystallization experiments using liquid assisted grinding (LAG), melt cool, and routine solvent evaporation yielded eutectics except for the combinations 3,5-dihydroxy and 3,4,5-trihydroxybenzoic acids, which produce cocrystals. The products have been characterized and analyzed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and thermogravimetric analysis (TGA). In particular, the structures of the cocrystals were determined using single crystal X-ray diffraction, whereas those of the eutectics were identified based on PXRD, DSC, and binary phase diagram construction. Using well-known thermal inkjet printing (TIJP), organic solutions of metronidazole and substituted hydroxybenzoic acids were injected into a cartridge and printed onto the template via a jet dispensing mechanism by varying the drug–coformer stoichiometric ratio to generate the cocrystals and eutectics of the adducts in quick time. The products formed from inkjet printing show excellent consistency in the particle size distribution and can be easily subjected to scaling up in industry compared to those prepared using the conventional cocrystallization techniques such as slurry grinding, rotavapor, and routine solution evaporation, which are time-consuming and produce varying particle sizes, which is a hindrance to product development and scaling during mass production.

中文翻译：

多组分加合物共结晶结果的评估：使用热喷墨印刷快速制造以实现均匀的粒度分布

由于共晶和共晶等多组分加合物已成为制药行业不可或缺的一部分，因为此类产品的应用潜力在药物设计和制造中迫在眉睫。甲硝唑（一种属于硝基咪唑家族的抗生素抗原生动物药物）与苯甲酸和单，二，三，羟基苯甲酸的共结晶产生的多组分加合物的理化性质优于该药物。使用液体辅助研磨（LAG），熔体冷却和常规溶剂蒸发的共结晶实验产生共晶，除了3,5-二羟基和3,4,5-三羟基苯甲酸的组合产生共晶体。使用粉末X射线衍射（PXRD），差示扫描量热法（DSC）对产品进行了表征和分析，扫描电子显微镜（SEM）和热重分析（TGA）。特别是，使用单晶X射线衍射确定了共晶的结构，而基于PXRD，DSC和二元相图的结构则确定了共晶的结构。使用著名的热喷墨印刷（TIJP），将甲硝唑和取代的羟基苯甲酸的有机溶液注入药筒中，并通过喷射分配机制，通过改变药物-共聚体化学计量比以产生共晶体和共晶，通过甲乙咪唑将其印刷在模板上。快速加成。

更新日期：2020-07-01

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