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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.

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

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