IR@PKUHSC  > 北京大学第一临床医学院  > 临床药理研究所
学科主题临床医学
Pharmacokinetics and Safety of Eszopiclone in Healthy Chinese Volunteers Data from a Single-center, Open-label, Single and Multiple Dose, Randomized, Crossover Pharmacokinetic Study of Eszopiclone under Fasting Conditions
Wu, F.1; Zhao, X. L.1; Wei, M. J.2; Wang, S. M.1; Zhou, H.1; Guo, S. J.1; Zhang, P.2
关键词eszopiclone pharmacokinetics safety tolerability
刊名ARZNEIMITTELFORSCHUNG-DRUG RESEARCH
2012-12-01
DOI10.1055/s-0032-1327570
62期:12页:561-565
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]PRIMARY INSOMNIA ; EFFICACY
英文摘要

Objective: The main objective of this study was to investigate the pharmacokinetic characters of eszopiclone (CAS: 138729-47-2) after single and multiple-dose oral administration in healthy adult Chinese volunteers.

Methods: In single-dose study, 12 subjects were given oral administrations of 1.5, 3 and 6 mg eszopiclone in an open-label, randomized, crossover fashion. In multiple-dose study, 8 subjects were given 3 mg eszopiclone once daily consecutively for 7 days. Blood samples were collected over 24 h and plasma eszopiclone were determined using a validated liquid chromatography/mass spectrometry (LC/MS/MS) assay. The safety and tolerability of eszopiclone was evaluated by adverse events recording, physical examination, laboratory testing, vital signs, and 12-lead ECG findings.

Results: The main pharmacokinetic parameters of eszopiclone after single-dose administration were as follows: doses of 1.5, 3 and 6 mg; C-max of 18.08 +/- 4.65, 38.29 +/- 15.41 and 76.38 +/- 23.34 ng/ml; T-max of 0.94 +/- 0.39, 1.04 +/- 0.63 and 1.08 +/- 0.51 h; AUC(0-24) of 110.90 +/- 23.06, 22736 +/- 62.41 and 504.10 +/- 140.13 ng*h/ml; elimination half-lives of 5.84 +/- 1.03, 5.53 +/- 1.91 and 6.17 +/- 1.23 h. After multiple-dose administration, the steady-state levels of eszopiclone were achieved by the 4th day, and the maul pharmacokinetic parameters were C-ss_max at 33.43 +/- 5.63 ng/ml and AUC(ss (0-24)) at 263.30 +/- 51.21 ng*h/ml. The most common adverse event was bitter or abnormal taste. All the adverse events were judged as mild to moderate and resolved without any medication.

Conclusion: The pharmacokinetic character of eszopiclone is linear and dose-proportional over the range of 1.5-6 mg. The systemic exposure does not accumulate with once-daily administrations. Eszopiclone appears to have good safety and is well tolerated.

语种英语
WOS记录号WOS:000321020200003
引用统计
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/67570
专题北京大学第一临床医学院_临床药理研究所
作者单位1.Capital Med Univ, Beijing Tongren Hosp, Dept Clin Pharmacol, Beijing 100730, Peoples R China
2.Peking Univ, Inst Clin Pharmacol, Beijing 100871, Peoples R China
推荐引用方式
GB/T 7714
Wu, F.,Zhao, X. L.,Wei, M. J.,et al. Pharmacokinetics and Safety of Eszopiclone in Healthy Chinese Volunteers Data from a Single-center, Open-label, Single and Multiple Dose, Randomized, Crossover Pharmacokinetic Study of Eszopiclone under Fasting Conditions[J]. ARZNEIMITTELFORSCHUNG-DRUG RESEARCH,2012,62(12):561-565.
APA Wu, F..,Zhao, X. L..,Wei, M. J..,Wang, S. M..,Zhou, H..,...&Zhang, P..(2012).Pharmacokinetics and Safety of Eszopiclone in Healthy Chinese Volunteers Data from a Single-center, Open-label, Single and Multiple Dose, Randomized, Crossover Pharmacokinetic Study of Eszopiclone under Fasting Conditions.ARZNEIMITTELFORSCHUNG-DRUG RESEARCH,62(12),561-565.
MLA Wu, F.,et al."Pharmacokinetics and Safety of Eszopiclone in Healthy Chinese Volunteers Data from a Single-center, Open-label, Single and Multiple Dose, Randomized, Crossover Pharmacokinetic Study of Eszopiclone under Fasting Conditions".ARZNEIMITTELFORSCHUNG-DRUG RESEARCH 62.12(2012):561-565.
条目包含的文件
条目无相关文件。
个性服务
推荐该条目
保存到收藏夹
查看访问统计
导出为Endnote文件
谷歌学术
谷歌学术中相似的文章
[Wu, F.]的文章
[Zhao, X. L.]的文章
[Wei, M. J.]的文章
百度学术
百度学术中相似的文章
[Wu, F.]的文章
[Zhao, X. L.]的文章
[Wei, M. J.]的文章
必应学术
必应学术中相似的文章
[Wu, F.]的文章
[Zhao, X. L.]的文章
[Wei, M. J.]的文章
相关权益政策
暂无数据
收藏/分享
所有评论 (0)
暂无评论
 

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。