Abstract

Background: Development of simple, rapid, and sensitive assay for the determination of loratadine in order to investigate its pharmacokinetic parameters in human plasma and its application in bioequivalence study of Loratadine 10mg Oral Disintegrated Tablets manufactured locally (test) and originally (Reference).

Methods: After extraction of loratadine from human plasma, it was chromatographed with mobile phase consisting of 0.5% formic acid: Acetonitrile (10:90 V/V) at flow rate 0.6ml/min, ESI positive mode, and m/z 383→337 for Loratadine. The bioequivalence study was conducted in a Two-Way Open-Label, Crossover design involving 24 volunteers. The criteria used to assess bioequivalence of the two products were AUC_0-t, AUC_0-inf, C_max, and T_max.

Results: The described method of analysis showed that the average recovery of Loratadine from human plasma was 102.685%. The limit of Quantitation was 0.05ng/ml, and the correlation coefficient (r²) was equal to 0.999893.
Statistical analysis (ANOVA) of the measured parameters showed that there was no significant difference between the two products.

Conclusion: The LC/MS/MS method presented is direct, simple, reproducible, sensitive, and linear for the determination of Loratadine in human plasma, and is adequate for clinical pharmacokinetic studies, besides the test product was found to be bioequivalent to the reference and both products can be considered interchangeable in medical practice.