Clinical Pharmacokinetics

, Volume 41, Supplement 1, pp 7–12 | Cite as

Oral Bioavailability of Desloratadine Is Unaffected by Food

  • Samir Gupta
  • Christopher Banfield
  • Melton Affrime
  • Thomas Marbury
  • Desmond Padhi
  • Paul Glue
Original Research Article

Abstract

Objective: To determine the effect of coadministration of food on the bioavailability of oral desloratadine.

Design: A randomised, open-label, single dose crossover study in which healthy adults received a single, oral dose of desloratadine 7.5mg, 50% greater than the recommended dose of 5mg, under fed or fasted conditions and were then crossed over to receive the other treatment regimen.

Participants: 18 healthy volunteers (11 men, 7 women) aged from 18 to 43 (mean 29) years and weighing 54 to 104 (mean 76.4) kg were enrolled and completed this study.

Main outcome measures: Cmax, AUCs and AUC∞.

Results: Maximum mean plasma concentration (Cmax) was 3.53 μg/L in fed compared with 3.30 μg/L in fasted participants. Area under the plasma concentration-time curve from time 0 to time of final quantifiable sample (AUCs) mean values were 61.0 μg/L · h in fed and 61.9 μg/L · h in fasted participants. Fed individuals had mean AUC extrapolated to infinity (AUC∞) of 62.5 μg/L μ h compared with 63.5 μg/L · h in fasted participants. None of these differences between the fed and fasted state was statistically significant. The most frequently reported adverse event was headache. There were no statistically significant changes in ECG parameters.

Conclusion: The results of this study indicate that food has no effect on the oral bioavailability of a single oral dose of desloratadine 7.5mg.

Notes

Acknowledgements

Supported by a research grant from Schering-Plough Research Institute, Kenilworth, New Jersey.

References

  1. 1.
    Charman WN, Porter CJ, Mithani S, et al. Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci 1997; 86: 269–82PubMedCrossRefGoogle Scholar
  2. 2.
    Hismanal (astemizole) prescribing information. Physicians’ desk reference, 53rd ed. Montvale, NJ: Medical Economics, 1999Google Scholar
  3. 3.
    Allegra-D (fexofenadine and pseudoephedrine) prescribing information. Physicians’ desk reference, 54th ed. Montvale, NJ: Medical Economics, 2000Google Scholar
  4. 4.
    Cramer JA. Enhancing patient compliance in the elderly. Role of packaging aids and monitoring. Drugs Aging 1998; 12: 7–15PubMedCrossRefGoogle Scholar
  5. 5.
    Kreutner W, Hey JA, Anthes J, et al. Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist. 1st communication: receptor selectivity, antihistaminic activity, and antiallergenic effects. Arzneimittelforschung 2000; 50: 345–52PubMedGoogle Scholar
  6. 6.
    Meltzer EO, Prenner BM, Nayak A. Efficacy and tolerability of once-daily 5mg desloratadine, an H1-receptor antagonist, in patients with seasonal allergic rhinitis. Assessment during the spring and fall allergy seasons. Clin Drug Invest 2001; 21(1): 25–32CrossRefGoogle Scholar
  7. 7.
    Gibaldi M, Perder D. Pharmacokinetics, 2nd ed. New York: Marcel Dekker, 1982Google Scholar
  8. 8.
    Schuirmann DJ. A comparison of the two one-sided test procedure and the power approach for assessing the bioequivalence of average bioavailability. J Pharmacokinet Biopharm 1987; 15: 657–80PubMedGoogle Scholar
  9. 9.
    Gupta S, Banfield C, Affrime M, et al. Desloratadine demonstrates dose proportionality in healthy adults after single doses. Clin Pharmacokinet 2002; 41 Suppl. 1: 1–6PubMedCrossRefGoogle Scholar

Copyright information

© Adis International Limited 2002

Authors and Affiliations

  • Samir Gupta
    • 1
  • Christopher Banfield
    • 1
  • Melton Affrime
    • 1
  • Thomas Marbury
    • 2
  • Desmond Padhi
    • 1
  • Paul Glue
    • 1
  1. 1.Department of Clinical PharmacologySchering-Plough Research InstituteKenilworthUSA
  2. 2.Orlando Clinical Research CenterOrlandoUSA

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