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The relative bioavailability of loratadine administered as a chewing gum formulation in healthy volunteers

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

Objective

The aim of this study was to investigate the pharmacokinetics of loratadine and its active metabolite desloratadine after single-dose administration of loratadine as a conventional tablet, orally disintegrating tablet (smelt tablet) and a chewing gum formulation with and without the collection of saliva.

Methods

Twelve healthy male volunteers participated in a four-period cross-over trial evaluating the effect of dosage forms on the pharmacokinetics of a single dose of loratadine. Loratadine was administered as two 10-mg conventional tablet, two 10-mg smelt tablet, a 30-mg portion of medicated chewing gum without collection of saliva and a 30-mg portion of medicated chewing gum with collection of saliva. Blood samples were taken at predefined sampling points 0–24 h after medication, and the plasma concentrations of loratadine and desloratadine were determined by high-performance liquid chromatography. Each study period was separated by a wash-out period of at least 7 days.

Results

The mean dose-corrected area under the plasma concentration-time curve extrapolated to infinity AUC(0−∞) for the chewing gum formulation was statistically significantly increased compared to the tablet formulation (geometric mean ratio: 2.68; 95%CI: 1.75–4.09). Desloratadine pharmacokinetic parameters from the chewing gum formulation were not statistically significantly different from the conventional tablet. Neither loratadine nor desloratadine pharmacokinetics of the smelt tablet formulation were statistically significantly different from the conventional tablet formulation. Plasma concentrations of desloratadine following the administration of loratadine as chewing gum with saliva collection were very low.

Conclusion

Our study showed that formulation of loratadine as a medicated chewing gum results in an almost threefold increase in relative bioavailability. This is most likely due to a bypass of first-pass metabolism as this study suggests that approximately 40% of the absorbed loratadine was absorbed via the oral mucosa.

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Acknowledgements

This study was supported by an unrestricted grant from Fertin Pharma A/S, Vejle, Denmark. The procedures in this study complied with the laws of Denmark, in which country they were performed.

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Authors and Affiliations

  1. Institute of Public Health, Clinical Pharmacology, University of Southern Denmark, Winslowparken 19, 5000, Odense C, Denmark

    Lene Noehr-Jensen, Tanja Busk Bidstrup, Rasmus Steen Pedersen, Flemming Nielsen & Kim Brosen

  2. Department of Biochemistry, Pharmacology and Genetics, Odense University Hospital, Sdr. Boulevard 29, 5000, Odense C, Denmark

    Per Damkier

Authors
  1. Lene Noehr-Jensen
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  2. Per Damkier
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  3. Tanja Busk Bidstrup
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  4. Rasmus Steen Pedersen
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  5. Flemming Nielsen
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  6. Kim Brosen
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Correspondence to Lene Noehr-Jensen.

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Noehr-Jensen, L., Damkier, P., Bidstrup, T.B. et al. The relative bioavailability of loratadine administered as a chewing gum formulation in healthy volunteers. Eur J Clin Pharmacol 62, 437–445 (2006). https://doi.org/10.1007/s00228-006-0139-6

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  • DOI: https://doi.org/10.1007/s00228-006-0139-6

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