Development and Evaluation of Cefadroxyl Monohydrate Solid Dispersion via Solvent Evaporation Method: Investigating Drug-Polymer Miscibility with Advanced Characterization

Abstract

Cefadroxil Monohydrate is a pharmaceutical drug used for the treatment of bacterial infection. The drug is characterized by poor aqueous solubility and dissolution rate leading to low bioavailability of the drug. Hence, there is a need for the improvement of the solubility and dissolution of such drugs. In this exertion, enhancement of the solubility and dissolution of the practically water insoluble drug Cefadroxil monohydrate was achieved by solid dispersion (SD) preparation using a solvent evaporation method which eventually leads to bioavailability enhancement. SD’s were formed using PEG-4000. which is a water-soluble copolymer and varying copolymer ratio. Solubility studies were carried out to establish the solubility-enhancing property of the SD’s. To support solubility analysis results, powder dissolution studies were carried out. The SD’s were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray powder diffraction studies, scanning electron microscopy. It was found that the SD’s formed showed the absence of the crystalline nature of the drug and its conversion to an amorphous state. The solubility and dissolution of the Cefadroxil monohydrate SD’s were enhanced. There is a 1.3 fold increase in solubility for the Drug:PEG-4000 in 1:4 ratios respectively. In-vitro drug release kinetics was investigated. This study demonstrates the use of solvent evaporation method for the preparation of SD’s in solubility and dissolution enhancement.