A novel drug–drug coamorphous system without molecular interactions: improve the physicochemical properties of tadalafil and repaglinide
Meiling Su, Yanming Xia, Yajing Shen, Weili Heng, Yuanfeng Wei, Linghe Zhang, Yuan Gao, Jianjun Zhang, Shuai Qian
Abstract
C NMR suggested the absence of intermolecular interactions in coamorphous tadalafil-repaglinide. In comparison to pure crystalline forms and their physical mixtures, both drugs in coamorphous system exhibited significant increases in intrinsic dissolution rate (1.5-3-fold) and could maintain supersaturated level for at least 4 hours in non-sink dissolution. In addition, the coamorphous tadalafil-repaglinide showed improved stability compared to the pure amorphous forms under long-term stability and accelerated storage conditions as well as under high compressing pressure. In conclusion, this study showed that co-amorphization technique is a promising approach for improving the dissolution rate of poorly water-soluble drugs and for stabilizing amorphous drugs.