SOLID DOSAGE FORM DEVELOPMENT OF DABIGATRAN ETEXILATE MESYLATE WITH INCREASED SOLUBILITY AND DISSOLUTION USING COCRYSTALLIZATIONAbstract
Dabigatran Etexilate Mesylate (DEM), an anticoagulant used to treat and prevent blood clots and to inhibit the occurrence of stroke in people with cardiac arrhythmia. The purpose of this study was to obtain DEM co-crystals by screening eight different conformers and prepare the co-crystals by evaporation technique. Molecular docking was used to identify suitable coformer. Tartaric acid DEM co-crystals have been effectively prepared in the molar ratio of 1:1, 1:2, and 1:3 by solution-based evaporation technique. A 1:1 molar mixture of DEM and tartaric acid was further characterized. Differential scanning calorimetry, Fourier Transform Infrared Spectroscopy (FTIR), Powder X-ray Diffraction (PXRD) and Scanning Electron Microscopy (SEM) were used to characterize manufactured co-crystals. The study confirmed the selection of proper coformer and exhibited enhanced solubility and stability of the DEM co-crystals. Hence, based upon the above results, it revealed that co-crystallization helps in improving the physicochemical properties of the API, altering their chemical structure.
A. R. Gawade and S. P. Boldhane *
Development Micro Labs Limited Micro Advanced Research Centre (Marc), Bangalore, Karnataka India.
18 July 2019
09 October 2019
29 February 2020
01 June 2020