Effect of Mixed Hydrotropy Approach on Solubility Enhancement of Carvedilol
摘要
In pharmaceutical formulation, poor water solubility of medicines continues to be a significant problem, frequently resulting in decreased bioavailability. An efficient and safe method of increasing drug solubility without the use of organic solvents is hydrotropic solubilization.
The goal of the current study was to assess the efficacy of hydrotropic solid dispersions and improve the water solubility of carvedilol, a weakly soluble antihypertensive and cardiovascular medication, employing the idea of mixed hydrotropy.
MethodsA variety of hydrotropic agents, such as nicotinamide, sodium citrate, and sodium benzoate, were used at varied concentrations to assess the solubility of carvedilol. To find synergistic effects on solubility enhancement, mixed hydrotropic systems were studied. The solvent evaporation method was used to create solid dispersions of carvedilol with specific mixed hydrotropic agents in various ratios. The drug content, solubility, and dissolving behavior of the produced formulations were evaluated. X-ray diffraction (XRD) and Fourier Transform Infrared Spectroscopy (FTIR) were used to examine compatibility and physicochemical characteristics.
ResultsWhen compared to individual hydrotropes and other combinations, the combination of nicotinamide and sodium benzoate showed a notable synergistic improvement in the aqueous solubility of carvedilol among the hydrotropic systems examined. Improved dissolving characteristics were demonstrated by solid dispersion formulations. While XRD investigations revealed alterations in crystallinity contributing to increased solubility, FTIR examination verified the lack of chemical interactions between carvedilol and the hydrotropic agents.
ConclusionThe study indicates that with low concentrations of hydrotropic chemicals, mixed hydrotropic solid dispersion is a practical, affordable, and eco-friendly method for improving the solubility and potential bioavailability of weakly water-soluble medications like carvedilol.