Improvement of Physico-mechanical and pharmacokinetic attributes of naproxen by cocrystallization with l-alanine

Review Pembuatan kokristalFarmasi Dengan Metode Mekanokimia

“…Parameter π dan polaritas pelarut yang digunakan berperan penting dalam pembentukan cocrystal. Selain itu, kemungkinan parameter π memiliki pengaruh kuat pada mekanisme, perantara, atau hasil polimorfik yang berbeda dalam reaksi kokristalisasi [55], [56], [57],.…”

Two Novel Co-Crystals of Naproxen: Comparison of Stability, Solubility and Intermolecular Interaction

“…Thus, pharmaceutical co-crystal technology has been demonstrated to be important in improving the poor solubility of NPX. NPX can form co-crystals or salts with the following CCFs or SFs, namely, nicotinamide [ 12 ], isonicotinamide [ 13 ] and picolinamide [ 14 ], duloxetine [ 15 ], and several chiral amino acids, including L-alanine [ 16 ], D-alanine, D-tyrosine, and D-tryptophan [ 17 ], arginine [ 18 ], zwitterionic prolinium [ 19 ], tramadol [ 20 ], bipyridine and piperazine [ 21 ], 4-amino pyridine and 2-amino pyridine [ 22 ], urea and thiourea [ 23 ]. SC XRD has been used to confirm the structures of most of these co-crystals or salts.…”

“…Among them, only the solubility of NPX–arginine salt was increased by 25.3 times [ 18 ]; other co-crystals have not significantly improved the solubility of naproxen. Compared with the API, the solubility of NPX–nicotinamide co-crystal was just increased by 2.8 times [ 12 ], and the intrinsic dissolution rate of NPX–L-alanine increased by two times more than NPX in phosphate buffer pH 7.4 [ 16 ]. It was necessary to carry out co-crystal research on NPX, and this prompted us to study co-crystals of NPX with better stability and solubility.…”