Journal
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
Volume -, Issue -, Pages -Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10837450.2023.2194406
Keywords
Carvedilol; maleic acid; co-amorphous; molecular interaction; solubility; physical stability
Categories
Ask authors/readers for more resources
The aim of this study was to enhance the solubility and stability of the water-insoluble drug carvedilol (CAR) with maleic acid (MLE) to create a co-amorphous system. The optimal molar ratio of CAR to MLE was found to be 2:1. The co-amorphous system showed improved solubility of CAR and maintained stability in an amorphous form.
The aim of this study was to enhance the solubility and stability of the water-insoluble drug carvedilol (CAR) with maleic acid (MLE) to create a co-amorphous system by a solvent evaporation method. Phase diagrams of co-amorphous CAR-MLE, constructed from peak height in the Fourier-transform infrared (FTIR) spectra and the glass transition temperature (Tg) from differential scanning calorimetry (DSC) measurements, revealed that the optimal molar ratio of CAR to MLE was 2:1. The FTIR spectra indicated that the secondary amine-derived peak of CAR and the carboxy group-derived peak of MLE disappeared in the CAR:MLE (2:1) co-amorphous system. DSC measurements showed that the endothermic peaks associated with the melting of CAR and MLE disappeared and a Tg at 43 degrees C was apparent. Furthermore, the solubility of CAR tested using the shaking flask method for 24 h at 37 degrees C was 1.2 mu g/mL, whereas that of the co-amorphous system was approximately three times higher, at 3.5 mu g/mL. Finally, the stability was evaluated by powder- X-ray diffraction at 40 degrees C; no clear diffraction peaks originating from crystals were observed in the amorphous state until after approximately three months of storage. These results indicate that co-amorphization of CAR with MLE improved the solubility of CAR while maintaining its stability in an amorphous form.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available