Department of Pediatric, Gifu University Graduate School of Medicine, Japan. t−tera@gifu−u.ac.jp
Allergol Int. 2012 Dec;61(4):619-24. doi: 10.2332/allergolint.11-OA-0378. Epub 2012 Sep 25.
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.
Eight Japanese children with bronchial asthma were treated for 7 days with CIC-hydrofluoroalkalane (CIC-HFA) 200 μg/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.
The pharmacokinetic parameters (AUC from time zero to last observed concentration [AUC(t)], AUC over the dosage interval τ at steady state [AUC(ss)], maximum concentration [C(max)], and terminal elimination half-life [T(1/2)]) and the temporal changes in the serum levels of des-isobutyryl-ciclesonide after repeated administration of CIC-HFA (200 μg/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.
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 (200 μg/day, once daily) can be administered safely for 7 days, without raising any safety concerns.
环索奈德（CIC）是一种高度安全的吸入性皮质类固醇（ICS），可转化为具有药理活性的代谢物（去异丁酰基环索奈德）；这种代谢物继而对肺部组织发挥局部抗炎作用。本研究旨在分析接受 CIC 重复剂量治疗的支气管哮喘日本儿童血清中去异丁酰基环索奈德的药代动力学，并将获得的数据与支气管哮喘白种人儿童的数据进行比较。
8 例支气管哮喘日本儿童接受 CIC-氢氟烷烃（CIC-HFA）200μg/天的计量吸入器治疗 7 天。该研究旨在根据之前一项涉及接受 CIC-HFA 重复 7 天治疗的健康日本成年男性的研究结果，评估达到稳态后重复 7 天给药的药代动力学。在第 7 天治疗时，多次采集血样以测量血清去异丁酰基环索奈德水平。
支气管哮喘日本儿童接受 CIC-HFA（200μg/天）重复给药后的药代动力学参数（从零时间到最后观察浓度的 AUC [AUC(t)]、稳态时剂量间隔τ的 AUC [AUC(ss)]、最大浓度 [C(max)]和终末消除半衰期 [T(1/2)])和血清去异丁酰基环索奈德水平的时间变化与支气管哮喘白种人儿童仅有轻微差异。研究期间未发现严重不良事件。此外，血清皮质醇水平、其他实验室参数或生命体征均无异常。
我们的结果表明，支气管哮喘日本儿童和白种人儿童重复给予 CIC-HFA 后，去异丁酰基环索奈德的药代动力学差异很小。我们的研究表明，CIC-HFA（200μg/天，每日一次）可安全使用 7 天，不会引起任何安全性问题。
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