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学科主题: 临床医学
题名:
Pharmacokinetics and pharmacodynamics of single and multiple doses of prasugrel in healthy native Chinese subjects
作者: Cui, Yi-min1; Wang, Zi-ning1; Chen, Xiao-wen2; Zhang, Hui-lin1; Zhao, Xia1; Zhou, Ying1
关键词: prasugrel ; platelet aggregation ; pharmacokinetics ; pharmacodynamics ; dose regimen ; healthy Chinese subject
刊名: ACTA PHARMACOLOGICA SINICA
发表日期: 2012-11-01
DOI: 10.1038/aps.2012.120
卷: 33, 期:11, 页:1395-1400
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Chemistry ; Pharmacology & Pharmacy
关键词[WOS]: P2Y(12) RECEPTOR ANTAGONIST ; ACUTE CORONARY SYNDROMES ; ANTIPLATELET AGENT ; CLOPIDOGREL ; PHARMACOLOGY
英文摘要:

Aim: To characterize the pharmacokinetics (PKs), pharmacodynamics (PDs), and tolerability of different dose regimens of prasugrel in healthy Chinese subjects.

Methods: This was a single-centered, open-label, parallel-design study. Subjects received a single loading dose (LD) of prasugrel followed by once-daily maintenance dose (MD) for 10 d. They were enrolled into 3 groups: 60 mg LD/10 mg MD; 30 mg LD/7.5 mg MD; 30 mg LD/5 mg MD. Blood samples were collected after the first and last dose. The serum concentration of the active metabolite of prasugrel was determined using a LC/MS/MS method. Platelet aggregation was assessed using the VerifyNow-P2Y(12) assay.

Results: Thirty-six healthy native Chinese subjects (19 males) aged 18-45 were enrolled; mean age and body weight were similar across the treatment groups (n=12 for each). The metabolite AUC(0-4) and C-max increased dose-proportionally across the dose range of 5 mg to 60 mg. The median T-max was 0.5 h in all groups. The PD parameters, indicated by the inhibition of ADP-induced platelet aggregation, were met more rapidly in the 60 mg group than the 30 mg group after the LD (94%-98%). This high degree of inhibition of platelet aggregation was maintained following the 10 mg MD (87%-90%) and was lower in the 7.5 mg and 5 mg MD groups (79%-83% and 64%-67%, respectively). Prasugrel was well tolerated in healthy Chinese subjects for single doses up to 60 mg and a MD of 10 mg for 10 d.

Conclusion: The PKs and PDs of the active metabolite of prasugrel were similar to those in Chinese subjects reported by a previous bridging study, which demonstrated that the exposure to the active metabolite in Chinese subjects was higher than in Caucasians.

语种: 英语
项目资助者: Eli Lilly and Company, Indianapolis, Indiana, USA
WOS记录号: WOS:000310778400009
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61596
Appears in Collections:北京大学第一临床医学院_药剂科_期刊论文

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作者单位: 1.Peking Univ, Hosp 1, Dept Pharm, Base Clin Trial, Beijing 100034, Peoples R China
2.Lilly Suzhou Pharmaceut Co Ltd, Shanghai 200021, Peoples R China

Recommended Citation:
Cui, Yi-min,Wang, Zi-ning,Chen, Xiao-wen,et al. Pharmacokinetics and pharmacodynamics of single and multiple doses of prasugrel in healthy native Chinese subjects[J]. ACTA PHARMACOLOGICA SINICA,2012,33(11):1395-1400.
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