Preparation and evaluation of pharmaceutical co-crystals for solubility enhancement of atorvastatin calcium
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Preparation and evaluation of pharmaceutical co‑crystals for solubility enhancement of atorvastatin calcium Afreen Naqvi1 · Mahmood Ahmad1 · Muhmmad Usman Minhas2 · Kifayat Ullah Khan1 · Fakhra Batool1 · Ali Rizwan1 Received: 24 April 2019 / Revised: 5 October 2019 / Accepted: 14 October 2019 © Springer-Verlag GmbH Germany, part of Springer Nature 2019
Abstract Co-crystallization is one of the methods to enhance the solubility of hydrophobic drugs that belong to BCS class II. Preparation and characterization of atorvastatin calcium co-crystals by liquid-assisted grinding method using citric acid and nicotinamide as co-formers for solubility enhancement were the objective of the current research. All the prepared formulations were characterized by powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), zeta size analysis, dissolution and solubility studies. Solubility studies were performed in distilled water, pH 1.2 and pH 6.8. PXRD revealed the structural nature of the co-crystals formulations. FTIR, TGA and DSC confirmed the complex formation and have better thermal stability than individual components. SEM images exhibited the prism-like crystals with irregular and rough surfaces. Zeta size analysis showed the small particle size having large surface area that facilitates to improve the solubility. Dissolution and solubility studies of the formulations confirmed that solubility enhanced several folds in all media as compared to the solubility of available market drug. From all these studies, it can be concluded that co-crystallization technique enhanced the solubility of atorvastatin calcium by using liquid-assisted grinding method. Keywords Atorvastatin calcium · Citric acid · Nicotinamide · Pharmaceutical co-crystals · Solubility enhancement
* Mahmood Ahmad [email protected] 1
Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur, Punjab 63100, Pakistan
2
College of Pharmacy, University of Sargodha, University Road, Sargodha City, Punjab, Pakistan
13
Vol.:(0123456789)
Polymer Bulletin
Introduction Drug’s poor aqueous solubility is one of the main arising problems in drug research and development because about 40% of the new available marketed immediate release oral drugs are practically insoluble [1]. Solubility is a phenomenon to dissolve solid in aqueous or liquid phase to form a saturated solution. At the site of absorption, drug should be available in water-soluble form to achieve maximum absorption [2, 3]. It is the interaction between two substances to produce a saturated solution at a given temperature. Solute and solvent are present in equilibrium in saturated solution. Solubility can be expressed in different ways like molality, mole fraction, molarity, parts, volume fraction and percentage. For better pharmacological activity of drugs, solubility is the important factor because weakly basic and weakly acidic
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