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Prevalence of Desloratadine Slow-metabolizer Phenotype and Food-dependent Pharmacokinetics of Desloratadine in Healthy Chinese Volunteers

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Abstract

Background and Objectives

Desloratadine, the major active metabolite of loratadine, is a non-sedating long-acting antihistamine that is widely used in the treatment of allergic rhinitis and chronic idiopathic urticaria. This study aimed to investigate the prevalence of desloratadine slow-metabolizer (DSM) phenotype and the effects of food on the pharmacokinetics of desloratadine and its active metabolite 3-OH-desloratadine in healthy Chinese volunteers.

Methods

A total of 46 healthy Chinese male volunteers were included in this investigation. All subjects received a single dose of a 5-mg desloratadine tablet under fasting or fed conditions and the plasma concentrations of desloratadine and 3-OH-desloratadine were measured by liquid chromatography-tandem mass spectrometry. The pharmacokinetic profiles were analyzed using a non-compartmental method in the Phoenix WinNonlin program. The individuals with a 3-OH-desloratadine-to-desloratadine exposure ratio lower than 10 % or a desloratadine half-life (t 1/2) of ≥50 h were supposed to be DSM.

Results

There was only one DSM among the 46 volunteers, with a prevalence of 2.2 %. Moreover, administration in a fed state resulted in 34.07 and 32.06 % decreases in maximum plasma concentration and area under the concentration-time curve from time zero to infinity for desloratadine and 47.26 and 48.46 % for 3-OH-desloratadine compared with those values under fasting conditions.

Conclusions

Taken together, these results indicated that the incidence of the DSM phenotype in the Chinese population was low and that food intake could significantly decrease the absorption rate and extent of desloratadine.

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Acknowledgments

The authors are grateful to the subjects who were involved in this study, the investigators, and research staff. The authors further appreciate the collaboration and help from Dr. Yi He, Blood Center of Chengdu (Chengdu, China).

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Authors and Affiliations

  1. Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, No.17, Block 3, Southern Renmin Road, Chengdu, 610041, China

    Ting Wang, Kun Zhang, Huiru Xie, Xuehua Jiang & Ling Wang

  2. Pharmacy Department, People’s Hospital of Xishuangbanna Dai Autonomous Prefecture, Yunnan, China

    Tingting Li

  3. Department of Pharmacy, Sichuan Provincial People’s Hospital, Sichuan, China

    Lin He

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  1. Ting Wang
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  2. Kun Zhang
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  3. Tingting Li
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  4. Lin He
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  5. Huiru Xie
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  6. Xuehua Jiang
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  7. Ling Wang
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Corresponding author

Correspondence to Ling Wang.

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The authors declare they have no conflicts of interest directly relevant to the content of this study.

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All procedures performed in studies involving human participants were in accordance with the ethical standards of the institutional and/or national research committee and with the 1964 Helsinki Declaration and its later amendments or comparable ethical standards.

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Informed consent was obtained from all individual participants included in the study.

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Wang, T., Zhang, K., Li, T. et al. Prevalence of Desloratadine Slow-metabolizer Phenotype and Food-dependent Pharmacokinetics of Desloratadine in Healthy Chinese Volunteers. Clin Drug Investig 35, 807–813 (2015). https://doi.org/10.1007/s40261-015-0343-1

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  • DOI: https://doi.org/10.1007/s40261-015-0343-1

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