Abstract
BackgroundThe meager physicochemical properties like low solubility and low dissolution rate of rosuvastatin calcium remain as an obstruction for formulation development. In the present work, we explore the evolution of rosuvastatin cocrystal, which may offer the synergetic physico-chemical properties of the drug. Cocrystal crafting depends on two possible intermolecular interactions; heteromeric and the homomeric selection of compounds with complementary functional groups are contemplated as a possible cause of supramolecular synthons in cocrystal formation. Specifically, cocrystals of rosuvastatin with l-asparagine and l-glutamine with molar ratio (1:1) were fabricated by using slow solvent evaporation and slow evaporation techniques. Novel cocrystals of rosuvastatin-asparagine (RSC-C) and rosuvastatin-glutamine (RSC-G) cocrystals obtained by slow solvent evaporation were utilized for preliminary investigation and further scale-up was done by using the solvent evaporation technique.ResultsThe novel cocrystals showed a new characteristic of powder X-ray diffraction, thermograms of differential scanning calorimetry, 1H liquid FT-NMR spectra, and scanning electron microscopy. These results signify the establishment of intermolecular interaction within the cocrystals. In both the novel cocrystals, rosuvastatin was determined to be engaged in the hydrogen bond interaction with the complementary functional groups of l-asparagine and l-glutamine. Compared with the pure rosuvastatin, RSC-C and RSC-G cocrystal showed 2.17-fold and 1.60-fold improved solubility respectively. The dissolution test showed that the RSC-C and RSC-G cocrystal exhibited 1.97-fold and 1.94-fold higher dissolution rate than the pure rosuvastatin in pH6.8 phosphate buffer respectively.ConclusionModulation in the chemical environment, improvement in the solubility, and dissolution rate demonstrated the benefit of co-crystallization to improve the physicochemical properties of the drug.Graphical abstract
Highlights
The meager physicochemical properties like low solubility and low dissolution rate of rosuvastatin calcium remain as an obstruction for formulation development
Rosuvastatin calcium (RSC)-G cocrystals showed 84.6% to 86.3% of the drug release which is of 1.74-fold enhancement of drug release in comparison to pure drug
Conclusion extensive research was dedicated to cocrystals, most of the literature reported novel cocrystal production and its modification in physicochemical properties; there is a lack of information regarding the selection of co-former and their effect on the biological system
Summary
The meager physicochemical properties like low solubility and low dissolution rate of rosuvastatin calcium remain as an obstruction for formulation development. Cocrystals of rosuvastatin with L-asparagine and L-glutamine with molar ratio (1:1) were fabricated by using slow solvent evaporation and slow evaporation techniques. Among all the physicochemical properties of the active moiety, dissolution and solubility are well deliberated to be the rate-determining step of poorly water-soluble drugs during oral absorption. Method selection for solubility and dissolution rate enhancement is crucial in attaining good oral absorption. Considering different methods, pharmaceutical cocrystals offers the most promising approach to improve physicochemical properties of the active moiety like solubility, melting point, Vemuri and Lankalapalli Future Journal of Pharmaceutical Sciences (2021) 7:64 molecule with required physicochemical properties [8, 9] and donates the right of intellectual property protection [10]. Accompanying high capability without waste products and causing co-crystallization and an influential chunk of Green chemistry [11]
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