Dissolution Advantage of Nitazoxanide Cocrystals in the Presence of Cellulosic Polymers

Salas-Zúñiga, Reynaldo; Rodríguez-Ruiz, Christian; Höpfl, Herbert; Morales-Rojas, Hugo; Sánchez-Guadarrama, Obdulia; Rodríguez-Cuamatzi, Patricia; Herrera-Ruiz, Dea

Because of the promising results, the performance of the powder formulation of NTZ-SUC cocrystal with Methocel ® 60 HG (5% w/w) was compared with a commercially available formulation of NTZ. Since our studies were based on a pharmaceutical powder, the commercially available reference tablets of NTZ (Daxon ® , 500 mg NTZ) were ground in an agate mortar and sifted through a sieve mesh 200. The results of the powder dissolution experiments using the USP type 1 apparatus (following the protocol detailed in Section 2.2.5) are shown in Figure 10 . Comparison of the dissolution graphs shows a statistically significant improvement of the dissolution properties for the formulated NTZ-SUC cocrystal in comparison with the commercial NTZ medicine (p < 0.05). From the polymer-cocrystal formulation with Methocel ® 60 HG (5% w/w), 57 mg of the drug were dissolved in the bulk solution after 3 h with an amount dissolved of 9046 ± 533 mg NTZ*min (AUC0-3 h), while the commercial product achieved 50 mg in the same time period, with an amount of 7287 ± 77 mg NTZ*min dissolved. Because of the promising results, the performance of the powder formulation of NTZ-SUC cocrystal with Methocel ® 60 HG (5% w/w) was compared with a commercially available formulation of NTZ. Since our studies were based on a pharmaceutical powder, the commercially available reference tablets of NTZ (Daxon ® , 500 mg NTZ) were ground in an agate mortar and sifted through a sieve mesh 200. The results of the powder dissolution experiments using the USP type 1 apparatus (following the protocol detailed in Section 2.2.5) are shown in Figure 10 . Comparison of the dissolution graphs shows a statistically significant improvement of the dissolution properties for the formulated NTZ-SUC cocrystal in comparison with the commercial NTZ medicine (p < 0.05). From the polymer-cocrystal formulation with Methocel ® 60 HG (5% w/w), 57 mg of the drug were dissolved in the bulk solution after 3 h with an amount dissolved of 9046 ± 533 mg NTZ*min (AUC 0-3 h ), while the commercial product achieved 50 mg in the same time period, with an amount of 7287 ± 77 mg NTZ*min dissolved.