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

  • Marilene Lopes Ângelo Federal University of Alfenas, Faculty of Pharmaceutical Sciences https://orcid.org/0000-0003-1258-8705
  • André Luís Morais Ruela Federal University of Ouro Preto, School of Pharmacy
  • Anna Clara Marques Ferreira Federal University of Alfenas, Faculty of Pharmaceutical Sciences
  • Marcus Vinicus de Faria Ramos Federal University of Alfenas, Faculty of Pharmaceutical Sciences
  • Cristina Martiniano Montanari University of São Paulo, Faculty of Pharmaceutical Sciences
  • Lucélia Magalhães da Silva Federal Institute of Paraná
  • Magali Benjamim de Araújo Federal University of Alfenas, Faculty of Pharmaceutical Sciences
Keywords: Dissolution, Crystal polymorphism, Solid dosage form, X-ray powder diffractometry, Thermal analysis, Solubility

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.

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Published
2019-11-29
How to Cite
Ângelo, M., Ruela, A. L., Ferreira, A. C., Ramos, M., Montanari, C., Silva, L., & Araújo, M. (2019). Evaluating the discriminatory power of a dissolution assay for rosuvastatin calcium capsules: Solid-state properties and dissolution media. Brazilian Journal of Pharmaceutical Sciences, 55, e17520. https://doi.org/10.1590/s2175-97902019000117520
Section
Articles