Synthesis, characterization and performance evaluation of aceclofenac-urea cocrystals

Abstract

Aceclofenac is one of the commonly used Nonsteroidal anti-inflammatory drugs representing the variety of therapeutic applications including management of pain, inflammation, rheumatoid arthritis, and osteoarthritis, etc. But very low solubility and dissolution rate of aceclofenac compromise its therapeutic effectiveness. So, current work focuses on the improvement of solubility and dissolution of aceclofenac by the cocrystal approach. Aceclofenac was screened with various coformers selected from Generally Recognized as Safe and Everything Added to Foods in the United States list using Molecular orbital package 2016 software to find out novel cocrystals of aceclofenac with improved biopharmaceutical properties. Novel cocrystals of aceclofenac with urea were synthesized by mechanochemical grinding method. The synthesized cocrystals (Aceclofenac-Urea neat grinding and Aceclofenac-Urea liquid assisted grinding) were characterized carefully by Differential scanning calorimetry, infrared spectroscopy and powder X-ray diffraction to verify the formation of the cocrystals. Pharmaceutically significant properties such as powder dissolution rate, solubility, and stability of the synthesized cocrystals were evaluated. Compared to aceclofenac, the synthesized cocrystals showed improved solubility and dissolution rate. The synthesized cocrystals were found to be non-hygroscopic and stable under ambient conditions.