• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

在禁食条件下,通用型替格瑞洛90毫克制剂与原研产品在健康白人受试者中的药代动力学和生物等效性。

Pharmacokinetics and Bioequivalence of a Generic Ticagrelor 90-mg Formulation Versus the Innovator Product in Healthy White Subjects Under Fasting Conditions.

作者信息

Rizea-Savu Simona, Duna Simona Nicoleta, Ghita Adrian, Iordachescu Adriana, Garlea Ioana, Chirila Marinela

机构信息

3S-Pharmacological Consultation & Research GmbH, Harpstedt, Germany.

Titu Maiorescu University, Bucharest, Romania.

出版信息

Clin Pharmacol Drug Dev. 2025 Jan;14(1):59-64. doi: 10.1002/cpdd.1471. Epub 2024 Sep 10.

DOI:10.1002/cpdd.1471
PMID:39256193
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11701948/
Abstract

Ticagrelor is a key antiplatelet agent used to prevent thrombotic events in patients with acute coronary syndrome. This open-label, 2-period, crossover Phase I study assessed the pharmacokinetics and bioequivalence of a generic ticagrelor 90-mg formulation compared to the innovator product under fasting conditions. Twenty-eight healthy White adults participated in the study. Each participant received a single dose of either the test or reference formulation, followed by a 7-day washout period before switching to the alternate formulation. Plasma concentrations of ticagrelor were measured using a validated high-performance liquid chromatography-tandem mass spectrometry method. Statistical analysis of primary pharmacokinetic parameters, including maximum concentration and area under the plasma concentration-time curve from time 0 to the last quantifiable concentration, showed bioequivalence with test/reference ratios of 110.9% and 107.1%, respectively, and 90% confidence intervals within the 80%-125% regulatory range. Treatment-emergent adverse events, such as headache, dysphagia, and dizziness, were moderate and transient and resolved promptly, with no significant difference in incidence between the formulations. These results confirm that the generic ticagrelor formulation is bioequivalent to the innovator product, supporting its use as an interchangeable option in clinical practice.

摘要

替格瑞洛是一种用于预防急性冠脉综合征患者血栓形成事件的关键抗血小板药物。这项开放标签、两阶段、交叉的I期研究评估了在禁食条件下,一种替格瑞洛90毫克仿制药制剂与原研产品相比的药代动力学和生物等效性。28名健康的白人成年人参与了该研究。每位参与者接受单剂量的受试制剂或参比制剂,随后经过7天的洗脱期,再换用另一种制剂。使用经过验证的高效液相色谱 - 串联质谱法测量替格瑞洛的血浆浓度。对主要药代动力学参数进行统计分析,包括最高浓度以及从0时间点至最后可定量浓度的血浆浓度 - 时间曲线下面积,结果显示生物等效性,受试/参比比值分别为110.9%和107.1%,90%置信区间在80% - 125%的监管范围内。治疗中出现的不良事件,如头痛、吞咽困难和头晕,程度为中度且短暂,迅速缓解,两种制剂之间的发生率无显著差异。这些结果证实,替格瑞洛仿制药制剂与原研产品具有生物等效性,支持其在临床实践中作为可互换选项使用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1201/11701948/7f3e6e8081a3/CPDD-14-59-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1201/11701948/7f3e6e8081a3/CPDD-14-59-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1201/11701948/7f3e6e8081a3/CPDD-14-59-g001.jpg

相似文献

1
Pharmacokinetics and Bioequivalence of a Generic Ticagrelor 90-mg Formulation Versus the Innovator Product in Healthy White Subjects Under Fasting Conditions.在禁食条件下,通用型替格瑞洛90毫克制剂与原研产品在健康白人受试者中的药代动力学和生物等效性。
Clin Pharmacol Drug Dev. 2025 Jan;14(1):59-64. doi: 10.1002/cpdd.1471. Epub 2024 Sep 10.
2
Pharmacokinetics and Bioequivalence of Two Formulations of Azithromycin Tablets: A Randomized, Single-Dose, Three-Period, Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions.两种阿奇霉素片剂制剂的药代动力学和生物等效性:在中国健康志愿者禁食和进食条件下的随机、单剂量、三周期、交叉研究。
Drugs R D. 2024 Jun;24(2):201-209. doi: 10.1007/s40268-024-00464-8. Epub 2024 May 30.
3
Bioequivalence of a Generic Nateglinide Formulation in Healthy Chinese Volunteers under Fasting and Fed Conditions: A Randomized, Open-Label, Double-Cycle, Double-Crossover Study.在空腹和进食条件下健康中国志愿者中一种那格列奈仿制药制剂的生物等效性:一项随机、开放标签、双周期、双交叉研究。
Pharmacology. 2021;106(7-8):418-425. doi: 10.1159/000512851. Epub 2021 Apr 16.
4
Comparative bioavailability and tolerability of a single 20-mg dose of two fluoxetine hydrochloride dispersible tablet formulations in fasting, healthy Chinese male volunteers: an open-label, randomized-sequence, two-period crossover study.两种盐酸氟西汀分散片在空腹健康中国男性志愿者中的单 20mg 剂量的生物等效性和耐受性比较:一项开放标签、随机序列、两周期交叉研究。
Clin Ther. 2010 Oct;32(11):1977-86. doi: 10.1016/j.clinthera.2010.10.003.
5
Bioequivalence of two tablet formulations of clopidogrel in healthy Argentinian volunteers: a single-dose, randomized-sequence, open-label crossover study.两种氯吡格雷片剂在健康阿根廷志愿者中的生物等效性:一项单次、随机、开放标签交叉研究。
Clin Ther. 2010 Jan;32(1):161-70. doi: 10.1016/j.clinthera.2010.01.010.
6
Bioequivalence and Safety of Generic Glecaprevir/Pibrentasvir Compared to a Branded Product: A Randomized, Crossover Study in Healthy Volunteers.格卡瑞韦/哌仑他韦仿制药与参比制剂的生物等效性和安全性:一项在健康志愿者中开展的随机、交叉研究。
Clin Pharmacol Drug Dev. 2024 Dec;13(12):1331-1338. doi: 10.1002/cpdd.1463. Epub 2024 Aug 14.
7
Pharmacokinetics and bioequivalence study of three oral formulations of valsartan 160 mg: a single-dose, randomized, open-label, three-period crossover comparison in healthy Indian male volunteers.缬沙坦 160mg 三种口服制剂的药代动力学和生物等效性研究:健康印度男性志愿者单次、随机、开放、三周期交叉比较。
Clin Ther. 2010 Mar;32(3):588-96. doi: 10.1016/j.clinthera.2010.03.004.
8
Pharmacokinetics and bioavailability comparison of generic and branded citalopram 20 mg tablets: an open-label, randomized-sequence, two-period crossover study in healthy Chinese CYP2C19 extensive metabolizers.西酞普兰 20 毫克片剂的仿制药与原研药的药代动力学和生物利用度比较:在中国 CYP2C19 广泛代谢者中进行的一项开放标签、随机序列、两周期交叉研究。
Clin Drug Investig. 2013 Jan;33(1):1-9. doi: 10.1007/s40261-012-0010-8.
9
Apixaban Pharmacokinetics and Bioequivalence of Two Tablet Formulations: A Randomized, Open-Label, Crossover Study, Fasting Condition in Healthy Indonesian Volunteers.阿哌沙班两种片剂制剂的药代动力学和生物等效性:一项在健康印度尼西亚志愿者中进行的随机、开放标签、交叉研究,禁食条件。
Clin Pharmacol Drug Dev. 2024 Aug;13(8):890-896. doi: 10.1002/cpdd.1409. Epub 2024 Apr 30.
10
Mycophenolate mofetil 500-mg tablet under fasting conditions: single-dose, randomized-sequence, open-label, four-way replicate crossover, bioequivalence study in healthy subjects.在空腹条件下给予霉酚酸酯 500 毫克片剂:单次、随机、开放标签、四交叉、健康受试者的生物等效性研究。
Clin Ther. 2010 Mar;32(3):556-74. doi: 10.1016/j.clinthera.2010.03.008.

本文引用的文献

1
Pharmacokinetics, Bioequivalence and Safety Evaluation of Two Ticagrelor Tablets Under Fasting and Fed Conditions in Healthy Chinese Subjects.两种替格瑞洛片剂在健康中国受试者空腹和进食条件下的药代动力学、生物等效性和安全性评价。
Drug Des Devel Ther. 2021 Mar 15;15:1181-1193. doi: 10.2147/DDDT.S297918. eCollection 2021.
2
The Effect of Food on the Single-Dose Bioavailability and Tolerability of the Highest Marketed Strength of Duloxetine.食物对度洛西汀最高市售强度单次给药生物利用度和耐受性的影响。
Clin Pharmacol Drug Dev. 2020 Oct;9(7):797-804. doi: 10.1002/cpdd.759. Epub 2019 Dec 2.
3
Antibacterial Activity of Ticagrelor in Conventional Antiplatelet Dosages Against Antibiotic-Resistant Gram-Positive Bacteria.
替格瑞洛在常规抗血小板剂量下对耐抗生素阳性革兰氏菌的抗菌活性。
JAMA Cardiol. 2019 Jun 1;4(6):596-599. doi: 10.1001/jamacardio.2019.1189.
4
Pharmacokinetic and Pharmacogenetic Factors Contributing to Platelet Function Recovery After Single Dose of Ticagrelor in Healthy Subjects.健康受试者单次服用替格瑞洛后血小板功能恢复的药代动力学和药物遗传学因素
Front Pharmacol. 2019 Mar 18;10:209. doi: 10.3389/fphar.2019.00209. eCollection 2019.
5
Ticagrelor Use in Acute Myocardial Infarction: Insights From the National Cardiovascular Data Registry.替格瑞洛在急性心肌梗死中的应用:来自国家心血管数据注册中心的见解。
J Am Heart Assoc. 2018 Jun 9;7(12):e008125. doi: 10.1161/JAHA.117.008125.
6
Ticagrelor: Pharmacokinetic, Pharmacodynamic and Pharmacogenetic Profile: An Update.替格瑞洛:药代动力学、药效学和药物遗传学概况:最新进展
Clin Pharmacokinet. 2015 Nov;54(11):1125-38. doi: 10.1007/s40262-015-0290-2.
7
Ticagrelor: pharmacokinetics, pharmacodynamics, clinical efficacy, and safety.替格瑞洛:药代动力学、药效学、临床疗效及安全性。
Pharmacotherapy. 2014 Oct;34(10):1077-90. doi: 10.1002/phar.1477. Epub 2014 Aug 28.
8
Lower mortality following pulmonary adverse events and sepsis with ticagrelor compared to clopidogrel in the PLATO study.在PLATO研究中,与氯吡格雷相比,替格瑞洛治疗后肺部不良事件和脓毒症导致的死亡率更低。
Platelets. 2014;25(7):517-25. doi: 10.3109/09537104.2013.842965. Epub 2013 Oct 15.
9
Disposition and metabolism of ticagrelor, a novel P2Y12 receptor antagonist, in mice, rats, and marmosets.替格瑞洛在小鼠、大鼠和狨猴体内的处置和代谢。替格瑞洛,一种新型的 P2Y12 受体拮抗剂。
Drug Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.
10
Ticagrelor versus clopidogrel in patients with acute coronary syndromes undergoing coronary artery bypass surgery: results from the PLATO (Platelet Inhibition and Patient Outcomes) trial.替格瑞洛与氯吡格雷用于行冠状动脉旁路移植术的急性冠状动脉综合征患者:来自 PLATO(血小板抑制和患者结局)试验的结果。
J Am Coll Cardiol. 2011 Feb 8;57(6):672-84. doi: 10.1016/j.jacc.2010.10.029. Epub 2010 Dec 30.