Repeated-Dose Pharmacokinetics of Inhaled Ciclesonide (CIC-HFA) in Japanese Children with Bronchial Asthma: A Phase I Study

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Author(s)

    • Azuma Junichi
    • Clinical Pharmacology and Pharmacogenomics, School of Pharmacy, Hyogo University of Health Science
    • Nishima Sankei
    • Department of Allergy, National Hospital Organization Fukuoka Hospital
    • Matsui Eiko
    • Department of Pediatric, Gifu University Graduate School of Medicine
    • Fukao Toshiyuki
    • Department of Pediatric, Gifu University Graduate School of Medicine
    • Sakai Kazuaki
    • Pharmacokinetics Research Group, Pharmacology & Pharmacokinetics Research Department, Pharmaceutical Development Research Laboratories, Teijin Pharma Limited
    • Yonezawa Hiroshi
    • Second Department of Drug Development, Pharmaceutical Business Division, Teijin Pharma Limited
    • Kato Zenichiro
    • Department of Pediatric, Gifu University Graduate School of Medicine
    • Kaneko Hideo
    • Department of Pediatric, Gifu University Graduate School of Medicine|Department of Pediatrics, Nagara Medical Center
    • Kondo Naomi
    • Department of Pediatric, Gifu University Graduate School of Medicine

Abstract

<b>Background:</b> Ciclesonide (CIC) is a highly safe, inhaled corticosteroid (ICS) that is converted into a pharmacologically active metabolite (des-isobutyryl-ciclesonide); this metabolite, in turn, exerts a local anti-inflammatory effect on lung tissue. The present study was undertaken to analyze the pharmacokinetics of des-isobutyryl-ciclesonide in the serum of Japanese children with bronchial asthma treated by repeated doses of CIC and to compare the data thus obtained with those obtained for Caucasian children with bronchial asthma.<br> <b>Methods:</b> Eight Japanese children with bronchial asthma were treated for 7 days with CIC-hydrofluoroalkalane (CIC-HFA) 200μg/day administered by a metered-dose inhaler. The study was designed to assess the pharmacokinetics after 7-day repeated administration by which the steady state can be achieved, based on the results of an earlier study involving healthy Japanese adult males who received 7-day repeated administration of CIC-HFA. Blood was sampled at multiple time points on Day 7 of treatment for measurement of the serum des-isobutyryl-ciclesonide level.<br> <b>Results:</b> The pharmacokinetic parameters (AUC from time zero to last observed concentration [AUC<sub>t</sub>], AUC over the dosage interval τ at steady state [AUC<sub>ss</sub>], maximum concentration [C<sub>max</sub>], and terminal elimination half-life [T<sub>1/2</sub>]) and the temporal changes in the serum levels of des-isobutyryl-ciclesonide after repeated administration of CIC-HFA (200μg/day) in Japanese children with bronchial asthma differed only slightly from those in Caucasian children with bronchial asthma. No serious adverse events were noted during the study period. Additionally, no abnormalities were detected in the serum cortisol level, other laboratory parameters, or vital signs.<br> <b>Conclusions:</b> Our results suggest that there is little difference in the pharmacokinetics of des-isobutyryl-ciclesonide up on repeated administration of CIC-HFA between Japanese and Caucasian children with bronchial asthma. And our study suggests that CIC-HFA (200μg/day, once daily) can be administered safely for 7 days, without raising any safety concerns.<br>

Journal

  • Allergology International

    Allergology International 61(4), 619-624, 2012

    Japanese Society of Allergology

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