Evaluating the discriminatory power of a dissolution assay for rosuvastatin calcium capsules: Solid-state properties and dissolution media

Abstract

We propose to evaluate the dissolution properties of rosuvastatin calcium (ROSC) capsules in different media to characterize the discriminatory power of the assay method. Dissolution assays were performed in media with different pH, and including the surfactant sodium dodecyl sulfate (SDS). Several immediaterelease formulations were manufactured using the commercial raw material characterized as amorphous solid. The hydrophobic adjutant magnesium stearate was employed in some formulations due to its negative effect in the wettability and dissolution efficacy of solid dosages. These formulations showed the lower dissolution efficacy values in media without surfactant; however, when SDS was added to the medium, the dissolution efficacy increased, and the discriminatory power was lost. In spite of micellar solubilization does not increase the ROSC solubility, it modifies the discriminatory power of the assay method, increasing the wettability of the powder mixtures. The crystalline form M of ROSC was recrystallized in our laboratory, and it showed lower solubility in water than amorphous solid. However, its dissolution properties were not influenced by SDS. These results are important to develop dissolution assays for other hydrophilic drugs with increased water solubility, once that dissolution media with surfactants increase the wettability of the formulations, leading to an overrated dissolution rate.

Fabrication and characterization of orodispersible films loaded with solid dispersion to enhance Rosuvastatin calcium bioavailability

“…Rosuvastatin's thermogram included an endothermic peak at about 165 °C, which corresponds to the drug's melting point ( Kapure et al, 2013 ). Also showed endothermic peaks at 50 °C up to 100 °C, correspond to the loss of water from Rosuvastatin ( Angelo et al, 2019 ). Similarly, the DSC of both poloxamer 407 and SD4 revealed endothermic peaks at 65 °C correspond to the melting point of poloxamer 407.…”

Comparison the solubility and dissolution rate effects of beta-cyclodextrin and gamma-cyclodextrin complexations of rosuvastatin calcium

“…The absence of a well-defined thermal peak versus melting point confirms the amorphous solid form of RSV. Lastly, a thermal event associated with the thermal degradation of amorphous form of RSV is observed in the range of 148-152 °C [23]. β ve g CD thermograms showed the a sharp endothermic water loss peak.…”