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Determination of some non-sedating antihistamines via their native fluorescence and derivation of some quantitative fluorescence intensity - structure relationships
Pharma Middle East
Noha M Hosny, Michael E El-Kommos, Samia M El-Gizawy and Noha N Atia
A validated simple, novel, and rapid spectro-fluorimetric method was developed for the determination of some Non-Sedating
Antihistamines (NSAs); namely Cetirizine (CTZ), Ebastine (EBS), Fexofenadine (FXD), and Loratadine (LOR). The method
is based on measuring the native fluorescence of the cited drugs after protonation in acidic media and studying their quantitative
fluorescence intensity 芒?? structure relationships. There was a linear relationship between the relative fluorescence intensity and the
concentration of the investigated drug. Under the optimal conditions, the linear ranges of calibration curves for the determination of
the studied NSAs were 0.10芒??2.0, 0.20芒??6.0, and 0.02芒??1.0 ?录g/mL for (CTZ, FXD), (EBS), and (LOR); respectively. The factors affecting
the protonation of the studied drugs were carefully studied and optimized. The method was validated according to ICH guidelines.
The suggested method is applicable for the determination of the four investigated drugs in bulk and pharmaceutical dosage forms
with excellent recoveries (97.67 - 103.80%). Quantitative relationships were found between the relative fluorescence intensities of
the protonated drugs and their physicochemical parameters namely: the pKa, log P, connectivity indexes (脧?v) and their squares.
Regression equations (76) were obtained and not previously reported. Six of these equations were highly significant and used for the
prediction of RFI of the studied NSAs.