Shankar Pol1*, Rajesh Nawale2, Prashant Puranik3, Hrutuja Chalak4, Harsha Pol5
1Department of Pharmacy, Research Scholar, YB Chavan College of Pharmacy, Dr. BAMU, Aurangabad - 431001, Maharashtra, India.
2Department of Pharmacology, Faculty of Pharmacy, Government College of Pharmacy, Dr. BAMU, Aurangabad - 431005, Maharashtra, India.
3Department of Pharmaceutics, Faculty of Pharmacy, University Department of Pharmaceutical Sciences, RTMNU, Nagpur- 440033, Maharashtra, India.
4,5ZIM Laboratories Limited, Nagpur- 441501, Maharashtra, India.
*Address for Corresponding Author
Shankar Dadasaheb Pol
YB Chavan College of Pharmacy, Dr. BAMU, Aurangabad - 431001, Maharashtra, India
Objective: This present study aims to screening of pharmaceutical cocrystal of Dabigatran Etexilate Mesylate (DEM) and coformers using different methods. Further the preparation and evaluation of DEM-coformer cocrystal and study the effect of cocrystallization on stability of DEM. Material and Methods: The coformers for DEM were screened using Fedor’s group solubility parameter. Compatibility study between DEM and coformer was performed. Coformer and cocrystallization method were selected based upon impurity level determination by RP-HPLC method during screening of coformers and cocrystalization methods. Further cocrystallization between selected coformer and DEM was confirmed using molecular docking study. The DEM-coformer cocrystal prepared using neat grinding method. The cocrystals produced were characterized using Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) spectroscopy and impurity level determination. Results: Cocrystal of DEM with amino acid was successfully prepared by neat grinding method. The formation of cocrystals of DEM with amino acid was evaluated by DSC, IR and impurity level determination by RP-HPLC method. Conclusion: The DEM-Leucine cocrystal exhibit enhanced stability as compared to other cocrystal. This study confirms that selection of proper coformer is very crucial step in preparation of stable, good cocrystal. Based upon above study and results it revealed that cocrystallization offers a valuable way to improve the physicochemical properties of the API.
Keywords: Pharmaceutical Cocrystal, Dabigatran Etexilate Mesylate, Coformer, Hansen (Fedor’s) solubility parameter