Randomized, Non-blinded, Two-way Crossover Study to Assess Bioequivalence Between a Rivaroxaban 10 mg Orally Disintegrating Tablet Administered With Water or Without Water and a Rivaroxaban 10 mg Film-coated Tablet in Japanese Healthy Male Adult Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Bayer
- 入组人数
- 80
- 试验地点
- 3
- 主要终点
- AUC(0-tlast) for plasma rivaroxaban concentration
研究概览
简要总结
Researchers in this study wanted to compare the effect of the formulation (orally disintegrating tablet and film-coated tablet) on the bioequivalence of drug Rivaroxaban (brand name: Xarelto) at dose of 10 mg in Japanese healthy male subjects aged 20 to 40 years. Rivaroxaban is an approved drug to be used for the prevention of events/diseases caused by blood clots. Currently, there are two formulations of Rivaroxaban available on the market in Japan and they are film-coated tablets and fine granules. To further improve patients' convenience, a new formulation, orally disintegrating tablet (ODT, a drug dosage form designed to be dissolved on the tongue rather than swallowed whole) is under development. The goal of this study was to compare the effect of this new formulation with film-coated tablets when taken with or without water.
Participants in this study received one oral dose of rivaroxaban 10 mg ODT either with or without water and one oral dose of rivaroxaban 10 mg film-tablet. There were at least 5 days between the two doses. Observation for each participant lasted about 6 weeks in total. Blood samples were collected from the participants to measure the blood level of the study drug.
研究设计
- 研究类型
- Interventional
- 分配方式
- Randomized
- 干预模型
- Crossover
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 20 Years 至 40 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Japanese healthy male subjects, aged 20 to 40 years (inclusive), with body mass index 17.6 to 26.4 kg/m²
排除标准
- •Subject with incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination, and effects of the study drugs will not be normal
- •Subject with known hypersensitivity to the study drugs (active substances or excipients of the preparations)
- •Subject with known coagulation disorders (e.g. von Willebrand disease, hemophilia)
- •Subject with febrile illness within 1 week before the first study drug administration
- •Subject with suspicion of drug or alcohol abuse
- •Subject with intake of foods or beverages containing grapefruit, pomelo, Seville orange, and tangelo within 1 week before the first study drug administration
- •Subject with therapies (e.g. physiotherapy, acupuncture, etc.) within 1 month before starting study treatment
- •Subject with clinically relevant findings in the electrocardiogram (ECG) such as a second- or third-degree atrioventricular block, prolongation of the QRS complex over 120 msec or of the corrected QT (QTc) interval over 450 msec
- •Subject with systolic blood pressure below 90 or above 130 mmHg
- •Subject with diastolic blood pressure below 45 or above 85 mmHg
- •Subject with clinically relevant deviations of the screened laboratory parameters from reference ranges
研究组 & 干预措施
Test A: 10 mg ODT with water, then 10 mg film-coated tablet
Participants received one single dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) with water in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban film-coated tablet in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in ODT form (Drug)
Test A: 10 mg ODT with water, then 10 mg film-coated tablet
Participants received one single dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) with water in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban film-coated tablet in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in film-coated form (Drug)
Test A: 10 mg film-coated tablet, then 10 mg ODT with water
Participants received one single dose of 10 mg rivaroxaban film-coated tablet in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) with water in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in ODT form (Drug)
Test A: 10 mg film-coated tablet, then 10 mg ODT with water
Participants received one single dose of 10 mg rivaroxaban film-coated tablet in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) with water in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in film-coated form (Drug)
Test B: 10 mg ODT without water, then 10 film-coated tablet
Participants received one single dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) without water in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban film-coated tablet in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in ODT form (Drug)
Test B: 10 mg ODT without water, then 10 film-coated tablet
Participants received one single dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) without water in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban film-coated tablet in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in film-coated form (Drug)
Test B: 10 mg film-coated tablet, then 10 mg ODT without water
Participants received one single dose of 10 mg rivaroxaban film-coated tablet in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) without water in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in ODT form (Drug)
Test B: 10 mg film-coated tablet, then 10 mg ODT without water
Participants received one single dose of 10 mg rivaroxaban film-coated tablet in the fasted state. After a washing period of 5 days, participants received one single oral dose of 10 mg rivaroxaban orally disintegrating tablet (ODT) without water in the fasted state
干预措施: Rivaroxaban (BAY 59-7939, Xarelto) in film-coated form (Drug)
结局指标
主要结局
AUC(0-tlast) for plasma rivaroxaban concentration
时间窗: Up to 48 hours after study medication
Area under the concentration versus time curve from time 0 to the last data point \> lower limit of quantitation
Cmax for plasma rivaroxaban concentration
时间窗: Up to 48 hours after study medication
Maximum observed concentration
次要结局
- Number of subjects with treatment-emergent adverse events(Up to 30 days after study medication)