Venkata Deepthi Vemuri1, Srinivas Lankalapalli2. 1. Maharajah's College of Pharmacy, Department of Pharmaceutical Technology, Vizianagaram, India. 2. GITAM (Deemed to be University), Department of Pharmacy, Andhra Pradesh, India.
Abstract
OBJECTIVES: Rosuvastatin calcium (RSC) is a synthetic biopharmaceutical classification system class-II drug with a low solubility but high permeability. The drug is used in hyperlipidemia management. In this study, the physicochemical properties of RSC were modified via crystal engineering to produce a cocrystal form. The solvent evaporation method was used to fabricate RSC cocrystals with the generally recognized as safe status coformer, L-asparagine. MATERIALS AND METHODS: The obtained cocrystals were evaluated using powder X-ray diffraction (PXRD), scanning electron microscopy, fourier-transform infrared spectroscopy, differential scanning calorimetry (DSC), and fourier-transform nuclear magnetic resonance (FT-NMR). RESULTS: The PXRD analysis revealed the presence of unique crystalline peaks, which provide details of interactions between the active pharmaceutical ingredient and coformer. The changes in the thermal behavior of the cocrystals were confirmed by DSC studies. The formation of a hydrogen bond between the drug and conformer was confirmed by a change in the chemical shift values of the FT-NMR spectra at the O-H group. Comparative studies of the solubility and dissolution rate revealed that the solubility and dissolution rate of the obtained cocrystals were almost two times higher than those of the parent drug. CONCLUSION: A new cocrystal form of RSC was obtained with a higher solubility and dissolution rate than those of the parent drug, implying new applications for these cocrystals.
OBJECTIVES: Rosuvastatin calcium (RSC) is a synthetic biopharmaceutical classification system class-II drug with a low solubility but high permeability. The drug is used in hyperlipidemia management. In this study, the physicochemical properties of RSC were modified via crystal engineering to produce a cocrystal form. The solvent evaporation method was used to fabricate RSC cocrystals with the generally recognized as safe status coformer, L-asparagine. MATERIALS AND METHODS: The obtained cocrystals were evaluated using powder X-ray diffraction (PXRD), scanning electron microscopy, fourier-transform infrared spectroscopy, differential scanning calorimetry (DSC), and fourier-transform nuclear magnetic resonance (FT-NMR). RESULTS: The PXRD analysis revealed the presence of unique crystalline peaks, which provide details of interactions between the active pharmaceutical ingredient and coformer. The changes in the thermal behavior of the cocrystals were confirmed by DSC studies. The formation of a hydrogen bond between the drug and conformer was confirmed by a change in the chemical shift values of the FT-NMR spectra at the O-H group. Comparative studies of the solubility and dissolution rate revealed that the solubility and dissolution rate of the obtained cocrystals were almost two times higher than those of the parent drug. CONCLUSION: A new cocrystal form of RSC was obtained with a higher solubility and dissolution rate than those of the parent drug, implying new applications for these cocrystals.
Authors: C Rustichelli; G Gamberini; V Ferioli; M C Gamberini; R Ficarra; S Tommasini Journal: J Pharm Biomed Anal Date: 2000-08-01 Impact factor: 3.935