Acta Scientific Pharmaceutical Sciences (ASPS)(ISSN: 2581-5423)

Research Article Volume 5 Issue 1

Development of a Bio analytical Assay for the Determination of Rupatadine in Human Plasma and its Clinical Applications

Sara AS2, Mohamed Raslan1,2, Eslam MS2 and Nagwa A Sabri1*

1Department of Clinical Pharmacy, Faculty of Pharmacy- Ain Shams University, Cairo, Egypt
2Drug Research Centre, Cairo, Egypt

*Corresponding Author: Nagwa A Sabri, Department of Clinical Pharmacy, Faculty of Pharmacy- Ain Shams University, Cairo, Egypt.

Received: November 10, 2020; Published: December 14, 2020



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, Cmax, and Tmax 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



  1. British National Formulary (BNF) 78 September 2019 – March 2020, Chapter 3 Respiratory system, Allergic conditions (2019): 282.
  2. Alison Brayfield (ed.), Martindale—The Complete Drug Reference, 38th edn., Pharmaceutical Press, London, UK (2014): 640.
  3. F Saint-Martin., et al. “A randomized, double-blind, parallel-group study, comparing the efficacy and safety of rupatadine (20 and 10 mg), a new PAF and H1 receptor-specific histamine antagonist, to loratadine 10 mg in the treatment of seasonal allergic rhinitis”. Journal of Investigational Allergology and Clinical Immunology 1 (2004): 34-40.
  4. Gathsaurie Neelika Malavige., et al. “A preliminary study on efficacy of rupatadine for the treatment of acute dengue infection”. Nature, Scientific Reports 8 (2018): 3857.
  5. Keam and Plosker. “Rupatadine A Review of its Use in the Management of Allergic Disorders”. Adis Drug Evaluation3 (2007): 457-474.
  6. Summary of Product Characteristics, Rupafin 10 mg Tablets, PL 11906/0007, J. Uriach and Cía., S.A. Spain (2014).
  7. A Solans., et al. “Influence of Food on the Oral Bioavailability of Rupatadine Tablets in Healthy Volunteers: A Single-Dose, Randomized, Open-Label, Two-Way Crossover Study”. Clinical Therapeutics5 (2007).
  8. M Sudhakara Rao., et al. “Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis”. Indian Journal of Otolaryngology and Head and Neck Surgery 61 (2009): 320-332.
  9. Soja Shamizadeh., et al. “Rupatadine: Efficacy and safety of a non-sedating antihistamine with PAF-antagonist effects”. Allergo Journal International 23 (2014): 87-95.
  10. Izquierdo I., et al. “Rupatadine, a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist: a review of pharmacological profile and clinical management of allergic rhinitis”. Drugs Today (Barc) 6 (2003): 451-468.
  11. Jörg Täubel., et al. “Pharmacokinetics, Safety and Cognitive Function Profile of Rupatadine10, 20 and 40 mg in Healthy JapaneseSubjects: A Randomised Placebo-Controlled Trial”. Plos One (2016).
  12. Nogueira DR., et al. Chromatographia 66 (2007): 915.
  13. Nogueira DR., et al. 31 (2008): 3098.
  14. Shirkhedkar AA., et al. Acta Chromatography 20 (2008): 423.
  15. Tian, Y., et al. Pharmaceutical and Biomedical Analysis 47 (2007): 899.
  16. YAN Hui-juan., et al. “Determination of Plasma Concentration of Rupatadine Fumarate by HPLC-MS/MS”. 27.10 (2008): 1174-1176. 2008.
  17. J Wen., et al. “Simultaneous determination of rupatadine and its metabolite desloratadine in human plasma by a sensitive LC–MS/MS method: Application to the pharmacokinetic study in healthy Chinese volunteers”. Journal of Pharmaceutical and Biomedical Analysis 49 (2009): 347–353. (2009).
  18. A Solans., et al. “Pharmacokinetic and Safety Profile of Rupatadine When Coadministered with Azithromycin at Steady-State Levels: A Randomized, Open-Label, Two-Way, Crossover, Phase I Study”. Clinical Therapeutics9 (2008).
  19. C Sun., et al. “Development of a highly sensitive LC-MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study”. Journal of Pharmaceutical and Biomedical Analysis (2015).
  20. “Guidelines on the design of a single-dose in vivo bioavailability or bioequivalence study” (2013).
  21. Guidance for Industry Bioanalytical Method Validation (2018).
  22. Guidance for Industry. “Bioequivalence Studies with Pharmacokinetic Endpoints for Drugs Submitted Under an ANDA” (2013).
  23. C Martínez-Cócera., et al. “Rupatadine 10 mg and cetirizine 10 mg seasonal allergic rhinitis: A randomised, double-blind parallel study”. Journal of Investigational Allergology and Clinical Immunology 1 (2005): 22-29.


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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