Synthesis and characterization of meloxicam eutectics with mandelic acid and saccharin for enhanced solubility.

Synthesis and characterization of meloxicam eutectics with mandelic acid and saccharin for enhanced solubility. Drug Dev Ind Pharm. 2020 May 30;:1-27 Authors: Fernandes RP, de Carvalho ACS, Ekawa B, do Nascimento ALSC, Pironi AM, Chorilli M, Caires FJ Abstract Meloxicam (MLX) is a non-steroidal anti-inflammatory which is practically insoluble in water, requiring high concentrations to reach therapeutic levels and causing frequently gastrointestinal effects. In this way, the aim of this study was to synthesize two eutectic mixtures of MLX with mandelic acid (MND) and saccharin (SAC) by liquid-assisted grinding resulting in a multicomponent material with enhanced solubility. Mixtures were studied in different stoichiometric and eutectic point was found for each eutectic by Binary phase diagram and Tamman's triangle, with 0.33 molar fraction of MLX for SAC and MND. Eutectics were characterized by thermoanalytical techniques (TG-DSC, EGA, DSC and DSC-microscopy), infrared spectroscopy and X-ray powder diffraction. Thermal behaviour was studied and videos of the materials being heated was available. A polymorphic transition was discovered and studied for MLX-MND eutectic. Each new system was evaluated by solubility, dissolution and hygroscopicity tests. Eutectics showed an increase in solubility of 1.7x (MLX-MND1), 3.1x (MLX-MND2) and 1.3x (MLX-SAC) with slower dissolution profile when compared to MLX. All new solid forms showed high hygr...
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research