Hiendrawan Stevanus, Veriansyah Bambang, Widjojokusumo Edward, Soewandhi Sundani Nurono, Wikarsa Saleh, Tjandrawinata Raymond R
Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia; School of Pharmacy, Bandung Institute of Technology, Bandung 40132, West Java, Indonesia.
Dexa Laboratories of Biomolecular Sciences, Cikarang 17550, West Java, Indonesia.
Int J Pharm. 2016 Jan 30;497(1-2):106-13. doi: 10.1016/j.ijpharm.2015.12.001. Epub 2015 Dec 4.
We report novel pharmaceutical cocrystal of a popular antipyretic drug paracetamol (PCA) with coformer 5-nitroisophhthalic acid (5NIP) to improve its tabletability. The cocrystal (PCA-5NIP at molar ratio of 1:1) was synthesized by solvent evaporation technique using methanol as solvent. The physicochemical properties of cocrystal were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetry analysis (TGA), fourier transform infrared spectroscopy (FTIR), hot stage polarized microscopy (HSPM) and scanning electron microscopy (SEM). Stability of the cocrystal was assessed by storing them at 40°C/75% RH for one month. Compared to PCA, the cocrystal displayed superior tableting performance. PCA-5NIP cocrystal showed a similar dissolution profile as compared to PCA and exhibited good stability. This study showed the utility of PCA-5NIP cocrystal for improving mechanical properties of PCA.
我们报道了一种常见的解热药物对乙酰氨基酚（PCA）与共形成物5-硝基间苯二甲酸（5NIP）形成的新型药物共晶，以改善其可压性。通过以甲醇为溶剂的溶剂蒸发技术合成了共晶（摩尔比为1:1的PCA-5NIP）。通过粉末X射线衍射（PXRD）、差示扫描量热法（DSC）、热重分析（TGA）、傅里叶变换红外光谱（FTIR）、热台偏光显微镜（HSPM）和扫描电子显微镜（SEM）对共晶的物理化学性质进行了表征。通过在40°C/75%相对湿度下储存一个月来评估共晶的稳定性。与PCA相比，共晶表现出优异的压片性能。与PCA相比，PCA-5NIP共晶显示出相似的溶出曲线，并表现出良好的稳定性。这项研究表明了PCA-5NIP共晶在改善PCA机械性能方面的实用性。
