Detailed Study on Synthesis, Characterization and Solubility Determination of 6-phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

Detailed Study on Synthesis, Characterization and Solubility Determination of 6-phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

The synthesis, characterization, determination of solubility and solution thermodynamic properties of the cardiovascular drug 6-phenylpyridazine-3(2H)-one (PPD) in 12 different pharmaceutical solvents is proposed for this analysis at temperatures ‘T = 298.2-318.2 K’ and pressure ‘p = 0.1 MPa.’ The calculated solubilities of PPD were regressed well with “van’t Hoff and Apelblat models”. Using differential scanning calorimetry and powder X-ray diffractometry, the solid phases of pure and balanced PPD were characterized and the results showed no conversion of PPD into solvates/hydrates/polymorphs after balance. Dimethyl sulfoxide [DMSO] (0.473), polyethylene glycol-400 [PEG-400] (0.412), Transcutol® (0.346), ethyl acetate [EA] (6.81 x 10-2), 2-butanol (2.18 x 10-2), 1-butanol (2.11 x 10-2), propylene glycol [PG] (1.50 x 10-2), isopropyl alcohol [IPA] (1.44 x 10-2), ethylene glycol [EG] (1.27 x 10-2), ethylene glycol [PG] (1.27 x 10-2), ethanol alcohol [IPA] (1.44 x 10-2), and ethylene glycol [EG] (1.27 x 10-2), (1.26 x 10-5). At other temperatures studied, similar trends were also reported. An endothermic and entropy-driven dissolution of PPD in all pharmaceutical solvents was observed in the results of thermodynamic evaluation. The results of the activity coefficients showed maximum molecular interaction in PPD-DMSO, PPD-PEG-400 and PPD-Transcutol relative to other solvent and solvent combinations tested. In conclusion, the findings of this study show that in the solubilization of PPD, pharmaceutical solvents such as DMSO, PEG-400 and Tarnscutol could be successfully used.

Author (s) Details

Dr. Faiyaz Shakeel
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Dr. Mohd. Imran
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, Rafha 919111, Saudi Arabia.

Dr. Nazrul Haq
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

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