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This study represents the first-time experimental analysis of lipophilicity for antidiabetic drugs from the gliflozin class using chromatographic methods alongside computational approaches. The lipophilicity of five gliflozins (canagliflozin (CANA), dapagliflozin (DAPA), empagliflozin (EMPA), ertugliflozin (ERTU), and sotagliflozin (SOTA)) was assessed using RMW and log kW parameters with RP8, RP18, and CN coatings, while methanol and acetonitrile were used as organic modifiers. To enhance the reliability, six reference substances with established lipophilicity values (0.62–3.5) were used for standardization. For computational analyses, the methods ALOGP, iLOGP, MLOGP, SILICOS-IT, WLOGP, XLOGP3, and Consensus. Log P were applied. Descriptive statistics, correlation analyses, and chemometric techniques were employed to compare the results. Experimental lipophilicity values showed strong correlations, indicating that RMW and log kW are reliable parameters for evaluating the lipophilicity of these therapeutically valuable drugs. However, computational lipophilicity values were less consistent, both among themselves and compared to experimental data. Finally, the experimental lipophilicity of gliflozins was analyzed in relation to their pharmacological properties, including protein binding, renal clearance, volume of distribution, half-life, potency (IC50), and lipophilic ligand efficiency (LLE). Our results allow for a confident proposal of a model to experimentally determine the lipophilicity of gliflozin drugs including new derivatives. [ABSTRACT FROM AUTHOR]

A comparative study of chemical stability of terfenadine (TER) and its in vivo metabolite fexofenadine (FEX) was performed. Both TER and FEX were subjected to high temperature at different pH and UV/VIS light at different pH and then quantitatively analyzed using new validated LC-UV methods. These methods were used to monitor the degradation processes and to determine the kinetics of degradation for both the compounds. As far as the effects of temperature and pH were concerned, FEX occurred more sensitive to degradation than TER. As far as the effects of UV/VIS light and pH were concerned, the both drugs were similarly sensitive to high doses of light. Using all stress conditions, the processes of degradation of TER and FEX followed the first-order kinetics. The results obtained for these two antihistaminic drugs could be helpful in developing their new derivatives with higher activity and stability at the same time. [ABSTRACT FROM AUTHOR]