Development of piroxicam mini-tablets enabled by spherical cocrystallization

We examined the potential of the spherical cocrystallization (SCC) technology in simultaneously enhancing tablet manufacturability and dissolution of poorly soluble drugs by developing a mini-tablet formulation of piroxicam. The manufacturing of mini-tablets using a direct compression (DC) process is more challenging than conventional tablets because of the much stricter requirement on the micromeritic properties of formulated powders. The SCC process in this work involved two steps: 1) preparing a new piroxicam-ferulic acid (PRX-FA) cocrystal, and 2) forming spherical agglomerates with the aid of a suitable bridging liquid.

The PRX-FA cocrystal exhibited enhanced solubility as well as improved plasticity. The bridging liquid, a mixture of chloroform and ethyl acetate (EA) (1: 2, v/v), was chosen based on the high computed adsorption energy of chloroform and EA on morphologically dominating crystal faces of PRX-FA. The improved flowability, tabletability, and dissolution rate of spherical PRX-FA enabled the successful development of a DC mini-tablet formulation with a high PRX loading (41 wt%). This example shows that SCC is a powerful enabling technology for DC tablet formulation development of challenging drugs.

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Keywords: Piroxicam, Spherical cocrystallization, Mini-tablet, Powder, Dissolution, hydroxypropylcellulose (HPC,
EF Pharm, fumed silica, microcrystalline cellulose (Avicel PH105), mannitol (Pearlitol SD200), croscarmellose sodium (CCM-Na, Ac-Di-Sol SD-711, magnesium stearate

Hongbo Chen, Chenguang Wang, Sibo Liu, Changquan Calvin Sun, Development of piroxicam mini-tablets enabled by spherical cocrystallization, International Journal of Pharmaceutics, Volume 590, 2020, 119953, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2020.119953.