Abstract

Background: Rupatadine is an antihistaminic drug that is used for the treatment of allergic rhinitis, chronic idiopathic urticarial, additionally, it can be used as safe and effective alternative to loratadine.

Aim: Development of bio-analytical method for rapid quantification of rupatadine in human plasma and its clinical application in bioequivalence study of generic and reference products of rupatadine 10mg film coated tablet.

Methods: Extracted rupatadine was chromatographed with mobile phase of methanol: 0.5% formic acid 80:20 v/v at flow rate 0.5ml/min, ESI positive mode, and m/z 416à282.1, 383à337 for rupatadine and loratadine as internal standard respectively. The bioequivalence study was conducted in a crossover design invovlving 24 volunteers and pharmacokinetic parameters AUC _0-t, AUC _0-inf, C_max, and T_max were used for assessment of bioequivalence of the two products_.

Results: The average recovery of rupatadine from human plasma was 87.567%, limit of quantitation was 0.01ng/ml, and the correlation coefficient (r²) obtained was 0.9997. Statistical analysis for the pharmacokinetic parameters using ANOVA test showed a non- significant difference between generic and reference products included in the study.

Conclusion: The developed bioanalytical LC/MS/MS method is simple, sensitive, precise, accurate and valid for rupatadine quantification in human plasma and is suitable for application in pharmacokinetic and bioavailability studies and therapeutic monitoring of rupatadine in management of allergic disease to ensure effective therapeutic drug levels and avoid potential undesired adverse events. Results of bioavailability study showed that both generic and reference products are bioequivalent and both products can be considered interchangeable in medical practice.

Keywords: Rupatadine; Bioanalytical Method Validation; LC/MS/MS; Non-Sedating Antihistamine; Allergic Rhinitis

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Citation

Citation: Nagwa A Sabri., et al. “Development of a Bio analytical Assay for the Determination of Rupatadine in Human Plasma and its Clinical Applications". Acta Scientific Pharmaceutical Sciences 5.1 (2021): 38-45.

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Copyright: © 2021 Nagwa A Sabri., et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.